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Showing drug card for Enflurane (DB00228)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-06-23 18:06:44
Primary Accession Number DB00228
Secondary Accession Number
  • APRD00234
Name Enflurane
Drug Type
  • Approved
  • Small Molecule
Description An extremely stable inhalation anesthetic that allows rapid adjustments of anesthesia depth with little change in pulse or respiratory rate. [PubChem]
Synonyms
  1. Anesthetic 347
  2. Anesthetic Compound No. 347
  3. Compound 347
  4. Enflurano [INN-Spanish]
  5. Enfluranum [INN-Latin]
  6. Methylflurether
  7. Ohio 347
Brand Names
  1. Alyrane
  2. Efrane
  3. Ethrane
Brand Mixtures Not Available
Chemical IUPAC Name 2-chloro-1-(difluoromethoxy)-1,1,2-trifluoroethane
Chemical Formula C3H2ClF5O
Chemical Structure Structure
CAS Registry Number 13838-16-9
InChI Identifier InChI=1/C3H2ClF5O/c4-1(5)3(8,9)10-2(6)7/h1-2H
InChI Key JPGQOUSTVILISH-UHFFFAOYAZ
KEGG Drug D00543 Link Image
KEGG Compound C07516 Link Image
PubChem Compound 3226 Link Image
PubChem Substance 169039 Link Image
ChEBI ID 4792 Link Image
PharmGKB ID PA449461 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 00778370 Link Image
RxList Link Not Available
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Enflurane Link Image
FDA Label Not Available
Material Safety Data Sheet (MSDS)
Synthesis Reference Not Available
Average Molecular Weight 184.4920
Monoisotopic Molecular Weight 183.9714
State Liquid
Melting Point 56 oC (boiling point)
Experimental Water Solubility Practically insoluble (5620 mg/L) Source: PhysProp
Predicted Water Solubility 3.90e+00 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 2.1 Source: PhysProp
Predicted LogP 2.24 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -1.67 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point Not Available
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID Not Available
Isomeric SMILES FC(F)OC(F)(F)[C@@H](F)Cl
Canonical SMILES FC(F)OC(F)(F)C(F)Cl
Drug Category
  • Anesthetics, Inhalation
  • General Anesthetics
ATC Codes
AHFS Codes
  • 28:04.92
Indication Used for the induction and maintenance of general anaesthesia during surgery and cesarean section and also used for analgesia during vaginal delivery.
Pharmacology Enflurane is an extremely stable halogenated ether inhalation anesthetic that allows rapid adjustments of anesthesia depth with little change in pulse or respiratory rate. Enflurane induces muscle relaxation and reduces pains sensitivity by altering tissue excitability. Induction of and recovery from anesthesia with enflurane are rapid. Enflurane may provide a mild stimulus to salivation or tracheobronchial secretions. Pharyngeal and laryngeal reflexes are readily obtunded. In the cardiovascular system, enflurane is a mild negative inotrope, causing a marked decrease in systemic vascular resistance, thus leading to a decrease in mean arterial pressure. This results in a reflex tachycardia. Enflurane also decreases coronary vascular resistance and sensitizes the myocardium to circulating catecholamines. Enflurane is a strong respiratory depressant. It decreases tidal volume but may increase respiratory rate. It also causes bronchodilatationa and inhibits pulmonary macrophage activity and mucociliary activity. Enflurane principle action in the CNS is general anaesthesia with little analgesic effect. It causes increased cerebral blood flow in concentrations and may induce tonic/clonic muscle activity and epileptiform EEG traces. It also causes a marked decrease in skeletal muscle tone. Actions in the genitourinary system include a decreased renal blood flow and glomerular filtration rate and the tone of pregnant uterus is decreased.
Mechanism of Action Enflurane induces a reduction in junctional conductance by decreasing gap junction channel opening times and increasing gap junction channel closing times. Enflurane also activates calcium dependent ATPase in the sarcoplasmic reticulum by increasing the fluidity of the lipid membrane. It also appears to bind the D subunit of ATP synthase and NADH dehydogenase. Enflurane also binds to the GABA receptor, the large conductance Ca2+ activated potassium channel, the glutamate receptor and the glycine receptor.
Absorption Rapidly absorbed into the circulation via the lungs.
Toxicity LD50=5.4 ml/kg (oral, rat). Symptoms of acute overdose include nausea, vomiting, irritation to the eyes, skin and nose/throat, headache, dizziness, and drowsiness. Symptoms of chronic overdose include hypotension, cardiac arrhythmias, respiratory depression, and liver/kidney dysfunction.
Protein Binding 97%
Biotransformation 2.4% of the dose is slowly metabolized hepatically via oxidation and dehalogenation (primarily through the actions of cytochrome P450 2E1). Leads to low levels of serum fluoride (15 µmol/L).
Half Life Not Available
Dosage Forms
Form Route
Liquid Respiratory (inhalation)
Patient Information Not Available
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions Not Available
Food Interactions Not Available
Pathways Not Available
General References
  1. Drugs.com Link Image
  2. [PubMed Link Image]
  3. Wikipedia Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. Cytochrome P450 2E1 (CYP2E1)
Targets
  1. Calcium-transporting ATPase type 2C member 1
  2. Glycine receptor subunit alpha-1
  3. ATP synthase delta chain, mitochondrial
  4. NADH-ubiquinone oxidoreductase chain 1
  5. Calcium-activated potassium channel subunit alpha 1
  6. Glutamate receptor 1
  7. Potassium voltage-gated channel subfamily A member 1
  8. Gamma-aminobutyric-acid receptor subunit alpha-1
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 2E1 (CYP2E1)
Enzyme 1 Gene Name CYP2E1
Enzyme 1 SwissProt ID P05181 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P05181|CP2E1_HUMAN Cytochrome P450 2E1 (EC 1.14.14.1)
MSALGVTVALLVWAAFLLLVSMWRQVHSSWNLPPGPFPLPIIGNLFQLELKNIPKSFTRL
AQRFGPVFTLYVGSQRMVVMHGYKAVKEALLDYKDEFSGRGDLPAFHAHRDRGIIFNNGP
TWKDIRRFSLTTLRNYGMGKQGNESRIQREAHFLLEALRKTQGQPFDPTFLIGCAPCNVI
ADILFRKHFDYNDEKFLRLMYLFNENFHLLSTPWLQLYNNFPSFLHYLPGSHRKVIKNVA
EVKEYVSERVKEHHQSLDPNCPRDLTDCLLVEMEKEKHSAERLYTMDGITVTVADLFFAG
TETTSTTLRYGLLILMKYPEIEEKLHEEIDRVIGPSRIPAIKDRQEMPYMDAVVHEIQRF
ITLVPSNLPHEATRDTIFRGYLIPKGTVVVPTLDSVLYDNQEFPDPEKFKPEHFLNENGK
FKYSDYFKPFSTGKRVCAGEGLARMELFLLLCAILQHFNLKPLVDPKDIDLSPIHIGFGC
IPPRYKLCVIPRS
Drug Target 1 [top]
Target 1 ID 241
Target 1 Name Calcium-transporting ATPase type 2C member 1
Target 1 Synonyms
  1. ATP-dependent Ca(2+
  2. ATPase 2C1
  3. EC 3.6.3.8
Target 1 Gene Name ATP2C1
Target 1 Protein Sequence >Calcium-transporting ATPase type 2C member 1
MKVARFQKIPNGENETMIPVLTSKKASELPVSEVASILQADLQNGLNKCEVSHRRAFHGW
NEFDISEDEPLWKKYISQFKNPLIMLLLASAVISVLMHQFDDAVSITVAILIVVTVAFVQ
EYRSEKSLEELSKLVPPECHCVREGKLEHTLARDLVPGDTVCLSVGDRVPADLRLFEAVD
LSIDESSLTGETTPCSKVTAPQPAATNGDLASRSNIAFMGTLVRCGKAKGVVIGTGENSE
FGEVFKMMQAEEAPKTPLQKSMDLLGKQLSFYSFGIIGIIMLVGWLLGKDILEMFTISVS
LAVAAIPEGLPIVVTVTLALGVMRMVKKRAIVKKLPIVETLGCCNVICSDKTGTLTKNEM
TVTHIFTSDGLHAEVTGVGYNQFGEVIVDGDVVHGFYNPAVSRIVEAGCVCNDAVIRNNT
LMGKPTEGALIALAMKMGLDGLQQDYIRKAEYPFSSEQKWMAVKCVHRTQQDRPEICFMK
GAYEQVIKYCTTYQSKGQTLTLTQQQRDVYQQEKARMGSAGLRVLALASGPELGQLTFLG
LVGIIDPPRTGVKEAVTTLIASGVSIKMITGDSQETAVAIASRLGLYSKTSQSVSGEEID
AMDVQQLSQIVPKVAVFYRASPRHKMKIIKSLQKNGSVVAMTGDGVNDAVALKAADIGVA
MGQTGTDVCKEAADMILVDDDFQTIMSAIEEGKGIYNNIKNFVRFQLSTSIAALTLISLA
TLMNFPNPLNAMQILWINIIMDGPPAQSLGVEPVDKDVIRKPPRNWKDSILTKNLILKIL
VSSIIIVCGTLFVFWRELRDNVITPRDTTMTFTCFVFFDMFNALSSRSQTKSVFEIGLCS
NRMFCYAVLGSIMGQLLVIYFPPLQKVFQTESLSILDLLFLLGLTSSVCIVAEIIKKVER
SREKIQKHVSSTSSSFLEV
Target 1 Number of Residues 934
Target 1 Molecular Weight 100579
Target 1 Theoretical pI 6.72
Target 1 GO Classification
Function
hydrolase activity
hydrolase activity, acting on acid anhydrides
hydrolase activity, acting on acid anhydrides, catalyzing transmembrane movement of substances
catalytic activity
ATPase activity, coupled to transmembrane movement of ions, phosphorylative mechanism
binding
nucleotide binding
purine nucleotide binding
adenyl nucleotide binding
ATP binding
transporter activity
ion transporter activity
cation transporter activity
di-, tri-valent inorganic cation transporter activity
calcium ion transporter activity
calcium-transporting ATPase activity
Process
metabolism
physiological process
cellular physiological process
transport
ion transport
cation transport
di-, tri-valent inorganic cation transport
calcium ion transport
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 1 General Function Inorganic ion transport and metabolism
Target 1 Specific Function This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of the calcium
Target 1 Pathways Not Available
Target 1 Reactions
  • ATP + H2O + Ca2+cis = ADP + phosphate + Ca2+trans
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 71-91
  • 105-123
  • 263-282
  • 295-312
  • 700-719
  • 730-750
  • 771-793
  • 809-828
  • 842-860
  • 876-896
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 6715131 Link Image
Target 1 UniProtKB/Swiss-Prot ID P98194 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name AT2C1_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Golgi apparatus
  • Golgi apparatus membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >2760 bp
ATGAAGGTTGCACGTTTTCAAAAAATACCTAATGGTGAAAATGAGACAATGATTCCTGTA
TTGACATCAAAAAAAGCAAGTGAATTACCAGTCAGTGAAGTTGCAAGCATTCTCCAAGCT
GATCTTCAGAATGGTCTAAACAAATGTGAAGTTAGTCATAGGCGAGCCTTTCATGGCTGG
AATAAGTTTGATATTAGTGAAGATGAGCCACTGTGGAAGAAGTATATTTCTCAGTTTAAA
AATCCCCTTATTATGCTGCTTCTGGCTTCTGCAGTCATCAGTGTTTTAATGCATCAGTTT
GATGATGCCGTCAGTATCACTGTGGCAATACTTATCGTTGTTACAGTTGCCTTTGTTCAG
GAATATCGTTCAGAAAAATCTCTTGAAGAATTGAGTAAACTTGTGCCACCAGAATGCCAT
TGTGTGCGTGAAGGAAAATTGGAGCATACACTTGCCCGAGACTTGGTTCCAGGTGATACA
GTTTGCCTTTCTGTTGGGGATAGAGTTCCTGCTGACTTACGCTTGTTTGAGGCTGTGGAT
CTTTCCATTGATGAGTCCAGCTTGACAGGTGAGACAACGCCTTGTTCTAAGGTGACAGCT
CCTCAGCCAGCTGCAACTAATGGAGATCTTGCATCGAGAAGTAACATTGCCTTTATGGGA
ACACTGGTCAGATGTGGCAAAGCAAAGGGTGTTGTCATTGGAACAGGAGAAAATTCTGAA
TTTGGGGAGGTTTTTAAAATGATGCAAGCAGAAGAGGCACCAAAAACCCCTCTGCAGAAG
AGCATGGACCTCTTAGGAAAACAACTTTCCTTTTACTCCTTTGGTATAATAGGAATCATC
ATGTTGGTTGGCTGGTTACTGGGAAAAGATATCCTGGAAATGTTTACTATTAGTGTAAGT
TTGGCTGTAGCAGCAATTCCTGAAGGTCTCCCCATTGTGGTCACAGTGACGCTAGCTCTT
GGTGTTATGAGAATGGTGAAGAAAAGGGCCATTGTGAAAAAGCTGCCTATTGTTGAAACT
CTGGGCTGCTGTAATGTGATTTGTTCAGATAAAACTGGAACACTGACGAAGAATGAAATG
ACTGTTACTCACATATTTACTTCAGATGGTCTGCATACTGAGGTTACTGGAGTTGGCTAT
AATCAATTTGGGGAAGTGATTGTTGATGGTGATGTTGTTCATGGATTCTATAACCCAGCT
GTTAGCAGAATTGTTGAGGCGGGCTGTGTGTGCAATGATGCTGTAATTAGAAACAATACT
CTAATGGGGAAGCCAACAGAAGGGGCCTTAATTGCTCTTGCAATGAAGATGGGTCTTGAT
GGACTTCAACAAGACTACATCAGAAAAGCTGAATACCCTTTTAGCTCTGAGCAAAAGTGG
ATGGCTGTTAAGTGTGTACACCGAACACAGCAGGACAGACCAGAGATTTGTTTTATGAAA
GGTGCTTACGAACAAGTAATTAAGTACTGTACTACATACCAGAGCAAAGGGCAGACCTTG
ACACTTACTCAGCAGCAGAGAGATGTGTACCAACAAGAGAAGGCACGCATGGGCTCAGCG
GGACTCAGAGTTCTTGCTTTGGCTTCTGGTCCTGAACTGGGACAGCTGACATTTCTTGGC
TTGGTGGGAATCATTGATCCACCTAGAACTGGTGTGAAAGAAGCTGTTACAACACTCATT
GCCTCAGGAGTATCAATAAAAATGATTACTGGAGATTCACAGGAGACTGCAGTTGCAATC
GCCAGTCGTCTGGGATTGTATTCCAAAACTTCCCAGTCAGTCTCAGGAGAAGAAATAGAT
GCAATGGATGTTCAGCAGCTTTCACAAATAGTACCAAAGGTTGCAGTATTTTACAGAGCT
AGCCCAAGGCACAAGATGAAAATTATTAAGTCGCTACAGAAGAACGGTTCAGTTGTAGCC
ATGACAGGAGATGGAGTAAATGATGCAGTTGCTCTGAAGGCTGCAGACATTGGAGTTGCG
ATGGGCCAGACTGGTACAGATGTTTGCAAAGAGGCAGCAGACATGATCCTAGTGGATGAT
GATTTTCAAACCATAATGTCTGCAATCGAAGAGGGTAAAGGGATTTATAATAACATTAAA
AATTTCGTTAGATTCCAGCTGAGCACGAGTATAGCAGCATTAACTTTAATCTCATTGGCT
ACATTAATGAACTTTCCTAATCCTCTCAATGCCATGCAGATTTTGTGGATCAATATTATT
ATGGATGGACCCCCAGCTCAGAGCCTTGGAGTAGAACCAGTGGATAAAGATGTCATTCGT
AAACCTCCTCGCAACTGGAAAGACAGCATTTTGACTAAAAACTTGATACTTAAAATACTT
GTTTCATCAATAATCATTGTTTGTGGGACTTTGTTTGTCTTCTGGCGTGAGCTACGAGAC
AATGTGATTACACCTCGAGACACAACAATGACCTTCACATGCTTTGTGTTTTTTGACATG
TTCAATGCACTAAGTTCCAGATCCCAGACCAAGTCTGTGTTTGAGATTGGACTCTGCAGT
AATAGAATGTTTTGCTATGCAGTTCTTGGATCCATCATGGGACAATTACTAGTTATTTAC
TTTCCTCCGCTTCAGAAGGTTTTTCAGACTGAGAGCCTAAGCATACTGGATCTGTTGTTT
CTTTTGGGTCTCACCTCATCAGTGTGCATAGTGGCAGAAATTATAAAGAAGGTTGAAAGG
AGCAGGGAAAAGATCCAGAAGCATGTTAGTTCGACATCATCATCTTTTCTTGAAGTATGA
Target 1 GenBank Gene ID
Target 1 GeneCard ID ATP2C1 Link Image
Target 1 GenAtlas ID ATP2C1 Link Image
Target 1 HGNC ID HGNC:13211 Link Image
Target 1 Chromosome Location 3
Target 1 Locus 3q22.1
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Hu Z, Bonifas JM, Beech J, Bench G, Shigihara T, Ogawa H, Ikeda S, Mauro T, Epstein EH Jr: Mutations in ATP2C1, encoding a calcium pump, cause Hailey-Hailey disease. Nat Genet. 2000 Jan;24(1):61-5. [PubMed Link Image]
  2. Nagase T, Kikuno R, Ishikawa KI, Hirosawa M, Ohara O: Prediction of the coding sequences of unidentified human genes. XVI. The complete sequences of 150 new cDNA clones from brain which code for large proteins in vitro. DNA Res. 2000 Feb 28;7(1):65-73. [PubMed Link Image]
  3. Sudbrak R, Brown J, Dobson-Stone C, Carter S, Ramser J, White J, Healy E, Dissanayake M, Larregue M, Perrussel M, Lehrach H, Munro CS, Strachan T, Burge S, Hovnanian A, Monaco AP: Hailey-Hailey disease is caused by mutations in ATP2C1 encoding a novel Ca(2+) pump. Hum Mol Genet. 2000 Apr 12;9(7):1131-40. [PubMed Link Image]
  4. Stanchi F, Bertocco E, Toppo S, Dioguardi R, Simionati B, Cannata N, Zimbello R, Lanfranchi G, Valle G: Characterization of 16 novel human genes showing high similarity to yeast sequences. Yeast. 2001 Jan 15;18(1):69-80. [PubMed Link Image]
  5. Fairclough RJ, Dode L, Vanoevelen J, Andersen JP, Missiaen L, Raeymaekers L, Wuytack F, Hovnanian A: Effect of Hailey-Hailey Disease mutations on the function of a new variant of human secretory pathway Ca2+/Mn2+-ATPase (hSPCA1). J Biol Chem. 2003 Jul 4;278(27):24721-30. Epub 2003 Apr 21. [PubMed Link Image]
Target 1 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 482
Target 2 Name Glycine receptor subunit alpha-1
Target 2 Synonyms
  1. Glycine receptor 48 kDa subunit
  2. Glycine receptor strychnine-binding subunit
  3. Glycine receptor subunit alpha-1 precursor
Target 2 Gene Name GLRA1
Target 2 Protein Sequence >Glycine receptor subunit alpha-1 precursor
MYSFNTLRLYLWETIVFFSLAASKEAEAARSAPKPMSPSDFLDKLMGRTSGYDARIRPNF
KGPPVNVSCNIFINSFGSIAETTMDYRVNIFLRQQWNDPRLAYNEYPDDSLDLDPSMLDS
IWKPDLFFANEKGAHFHEITTDNKLLRISRNGNVLYSIRITLTLACPMDLKNFPMDVQTC
IMQLESFGYTMNDLIFEWQEQGAVQVADGLTLPQFILKEEKDLRYCTKHYNTGKFTCIEA
RFHLERQMGYYLIQMYIPSLLIVILSWISFWINMDAAPARVGLGITTVLTMTTQSSGSRA
SLPKVSYVKAIDIWMAVCLLFVFSALLEYAAVNFVSRQHKELLRFRRKRRHHKSPMLNLF
QEDEAGEGRFNFSAYGMGPACLQAKDGISVKGANNSNTTNPPPAPSKSPEEMRKLFIQRA
KKIDKISRIGFPMAFLIFNMFYWIIYKIVRREDVHNQ
Target 2 Number of Residues 464
Target 2 Molecular Weight 52625
Target 2 Theoretical pI 9.04
Target 2 GO Classification
Function
neurotransmitter receptor activity
anion channel activity
chloride channel activity
glycine-gated chloride channel activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
GABA receptor activity
GABA-A receptor activity
Process
anion transport
inorganic anion transport
chloride transport
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 2 General Function Involved in GABA-A receptor activity
Target 2 Specific Function The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing)
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • 1-28
Target 2 Transmembrane Regions
  • 248-274
  • 281-298
  • 313-336
  • 429-446
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 31851 Link Image
Target 2 UniProtKB/Swiss-Prot ID P23415 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name GLRA1_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 2 Gene Sequence >1350 bp
ATGTACAGCTTCAATACTCTTCGACTCTACCTTTCGGGAGCCATTGTATTCTTCAGCCTT
GCTGCTTCTAAGGAGGCTGAAGCTGCTCGCTCCGCAACCAAGCCTATGTCACCCTCGGAT
TTCCTGGATAAGCTAATGGGGAGAACCTCCGGATATGATGCCAGGATCAGGCCCAATTTT
AAAGGTCCCCCAGTGAACGTGAGCTGCAACATTTTCATCAACAGCTTTGGTTCCATTGCT
GAGACAACCATGGACTATAGGGTCAACATCTTCCTGCGGCAGCAATGGAACGACCCCCGC
CTGGCCTATAATGAATACCCTGACGACTCTCTGGACCTGGACCCATCCATGCTGGACTCC
ATCTGGAAACCTGACCTGTTCTTTGCCAACGAGAAGGGGGCCCACTTCCATGAGATCACC
ACAGACAACAAATTGCTAAGGATCTCCCGGAATGGGAATGTCCTCTACAGCATCAGAATC
ACCCTGACACTGGCCTGCCCCATGGACTTGAAGAATTTCCCCATGGATGTCCAGACATGT
ATCATGCAACTGGAAAGCTTTGGATATACGATGAATGACCTCATCTTTGAGTGGCAGGAA
CAGGGAGCCGTGCAGGTAGCAGATGGACTAACTCTGCCCCAGTTTATCTTGAAGGAAGAG
AAGGACTTGAGATACTGCACCAAGCACTACAACACAGGTAAATTCACCTGCATTGAGGCC
CGGTTCCACCTGGAGCGGCAGATGGGTTACTACCTGATTCAGATGTATATTCCCAGCCTG
CTCATTGTCATCCTCTCATGGATCTCCTTCTGGATCAACATGGATGCTGCACCTGCTCGT
GTGGGCCTAGGCATCACCACTGTGCTCACCATGACCACCCAGAGCTCCGGCTCTCGAGCA
TCTCTGCCCAAGGTGTCCTATGTGAAAGCCATTGACATTTGGATGGCAGTTTGCCTGCTC
TTTGTGTTCTCAGCCCTATTAGAATATGCTGCCGTTAACTTTGTGTCTCGGCAACATAAG
GAGCTGCTCCGATTCAGGAGGAAGCGGAGACATCACAAGGAGGATGAAGCTGGAGAAGGC
CGCTTTAACTTCTCTGCCTATGGGATGGGCCCAGCCTGTCTACAGGCCAAGGATGGCATC
TCAGTCAAGGGCGCCAACAACAGTAACACCACCAACCCCCCTCCTGCACCATCTAAGTCC
CCAGAGGAGATGCGAAAACTCTTCATCCAGAGGGCCAAGAAGATCGACAAAATATCCCGC
ATTGGCTTCCCCATGGCCTTCCTCATTTTCAACATGTTCTACTGGATCATCTACAAGATT
GTCCGTAGAGAGGACGTCCACAACCAGTGA
Target 2 GenBank Gene ID
Target 2 GeneCard ID GLRA1 Link Image
Target 2 GenAtlas ID GLRA1 Link Image
Target 2 HGNC ID HGNC:4326 Link Image
Target 2 Chromosome Location 5
Target 2 Locus 5q32
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Vergouwe MN, Tijssen MA, Peters AC, Wielaard R, Frants RR: Hyperekplexia phenotype due to compound heterozygosity for GLRA1 gene mutations. Ann Neurol. 1999 Oct;46(4):634-8. [PubMed Link Image]
  2. Grenningloh G, Schmieden V, Schofield PR, Seeburg PH, Siddique T, Mohandas TK, Becker CM, Betz H: Alpha subunit variants of the human glycine receptor: primary structures, functional expression and chromosomal localization of the corresponding genes. EMBO J. 1990 Mar;9(3):771-6. [PubMed Link Image]
  3. Shiang R, Ryan SG, Zhu YZ, Fielder TJ, Allen RJ, Fryer A, Yamashita S, O'Connell P, Wasmuth JJ: Mutational analysis of familial and sporadic hyperekplexia. Ann Neurol. 1995 Jul;38(1):85-91. [PubMed Link Image]
  4. Rees MI, Andrew M, Jawad S, Owen MJ: Evidence for recessive as well as dominant forms of startle disease (hyperekplexia) caused by mutations in the alpha 1 subunit of the inhibitory glycine receptor. Hum Mol Genet. 1994 Dec;3(12):2175-9. [PubMed Link Image]
  5. Langosch D, Laube B, Rundstrom N, Schmieden V, Bormann J, Betz H: Decreased agonist affinity and chloride conductance of mutant glycine receptors associated with human hereditary hyperekplexia. EMBO J. 1994 Sep 15;13(18):4223-8. [PubMed Link Image]
  6. Schorderet DF, Pescia G, Bernasconi A, Regli F: An additional family with Startle disease and a G1192A mutation at the alpha 1 subunit of the inhibitory glycine receptor gene. Hum Mol Genet. 1994 Jul;3(7):1201. [PubMed Link Image]
  7. Shiang R, Ryan SG, Zhu YZ, Hahn AF, O'Connell P, Wasmuth JJ: Mutations in the alpha 1 subunit of the inhibitory glycine receptor cause the dominant neurologic disorder, hyperekplexia. Nat Genet. 1993 Dec;5(4):351-8. [PubMed Link Image]
  8. Milani N, Dalpra L, del Prete A, Zanini R, Larizza L: A novel mutation (Gln266-->His) in the alpha 1 subunit of the inhibitory glycine-receptor gene (GLRA1) in hereditary hyperekplexia. Am J Hum Genet. 1996 Feb;58(2):420-2. [PubMed Link Image]
  9. Elmslie FV, Hutchings SM, Spencer V, Curtis A, Covanis T, Gardiner RM, Rees M: Analysis of GLRA1 in hereditary and sporadic hyperekplexia: a novel mutation in a family cosegregating for hyperekplexia and spastic paraparesis. J Med Genet. 1996 May;33(5):435-6. [PubMed Link Image]
  10. Seri M, Bolino A, Galietta LJ, Lerone M, Silengo M, Romeo G: Startle disease in an Italian family by mutation (K276E): The alpha-subunit of the inhibiting glycine receptor. Hum Mutat. 1997;9(2):185-7. [PubMed Link Image]
  11. 9920650 Saul B, Kuner T, Sobetzko D, Brune W, Hanefeld F, Meinck HM, Becker CM: Novel GLRA1 missense mutation (P250T) in dominant hyperekplexia defines an intracellular determinant of glycine receptor channel gating. J Neurosci. 1999 Feb 1;19(3):869-77.
Target 2 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 3 [top]
Target 3 ID 537
Target 3 Name ATP synthase delta chain, mitochondrial
Target 3 Synonyms
  1. ATP synthase delta chain, mitochondrial precursor
  2. EC 3.6.3.14
Target 3 Gene Name ATP5D
Target 3 Protein Sequence >ATP synthase delta chain, mitochondrial precursor
MLPAALLRRPGLGRLVRHARAYAEAAAAPAAASGPNQMSFTFASPTQVFFNGANVRQVDV
PTLTGAFGILAAHVPTLQVLRPGLVVVHAEDGTTSKYFVSSGSIAVNADSSVQLLAEEAV
TLDMLDLGAAKANLEKAQAELVGTADEATRAEIQIRIEANEALVKALE
Target 3 Number of Residues 170
Target 3 Molecular Weight 17490
Target 3 Theoretical pI 5.19
Target 3 GO Classification
Function
hydrogen-transporting ATPase activity, rotational mechanism
transporter activity
ion transporter activity
cation transporter activity
monovalent inorganic cation transporter activity
hydrogen ion transporter activity
hydrogen-transporting ATP synthase activity, rotational mechanism
Process
physiological process
metabolism
cellular metabolism
cofactor metabolism
coenzyme metabolism
group transfer coenzyme metabolism
nucleoside phosphate metabolism
ATP biosynthesis
ATP synthesis coupled proton transport
Component
cell
membrane
intrinsic to membrane
integral to membrane
proton-transporting two-sector ATPase complex
Target 3 General Function Energy production and conversion
Target 3 Specific Function Produces ATP from ADP in the presence of a proton gradient across the membrane
Target 3 Pathways
Name SMPDB Link KEGG Link
ATP synthesis map00193 Link Image
Flagellar assembly map02040 Link Image
Oxidative phosphorylation map00190 Link Image
Photosynthesis map00195 Link Image
Type III secretion system map03070 Link Image
Target 3 Reactions
  • ATP + H2O + H+in = ADP + phosphate + H+out
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • None
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 12586 Link Image
Target 3 UniProtKB/Swiss-Prot ID P30049 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name ATPD_HUMAN Link Image
Target 3 PDB ID 1E79 Link Image
Target 3 PDB File Show
Target 3 3D Structure
Target 3 Cellular Location
  • Mitochondrion
Target 3 Gene Sequence >507 bp
ATGCTGCCCGCCGCGCTGCTCCGCCGCCCGGGACTTGGCCGCCTCGTCCGCCACGCCCGT
GCCTATGCCGAGGCCGCCGCCGCCCCGGCTGCCGCCTCTGGCCCCAACCAGATGTCCTTC
ACCTTCGCCTCTCCCACGCAGGTGTTCTTCAACGGTGCCAACGTCCGGCAGGTGGACGTG
CCCACGCTGACCGGAGCCTTCGGCATCCTGGCGGCCCACGTGCCCACGCTGCAGGTCCTG
CGGCCGGGGCTGGTCGTGGTGCATGCAGAGGACGGCACCACCTCCAAATACTTTGTGAGC
AGCGGTTCCATCGCAGTGAACGCCGACTCTTCGGTGCAGTTGTTGGCCGAAGAGGCCGTG
ACGCTGGACATGTTGGACCTGGGGGCAGCCAAGGCAAACTTGGAGAAGGCCCAGGCGGAG
CTGGTGGGGACAGCTGACGAGGCCACGCGGGCAGAGATCCAGATCCGAATCGAGGCCAAC
GAGGCCCTGGTGAAGGCCCTGGAGTAG
Target 3 GenBank Gene ID
Target 3 GeneCard ID ATP5D Link Image
Target 3 GenAtlas ID ATP5D Link Image
Target 3 HGNC ID HGNC:837 Link Image
Target 3 Chromosome Location 19
Target 3 Locus 19p13.3
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Hochstrasser DF, Frutiger S, Paquet N, Bairoch A, Ravier F, Pasquali C, Sanchez JC, Tissot JD, Bjellqvist B, Vargas R, et al.: Human liver protein map: a reference database established by microsequencing and gel comparison. Electrophoresis. 1992 Dec;13(12):992-1001. [PubMed Link Image]
  2. Jordan EM, Breen GA: Molecular cloning of an import precursor of the delta-subunit of the human mitochondrial ATP synthase complex. Biochim Biophys Acta. 1992 Feb 28;1130(1):123-6. [PubMed Link Image]
Target 3 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 4 [top]
Target 4 ID 559
Target 4 Name NADH-ubiquinone oxidoreductase chain 1
Target 4 Synonyms
  1. EC 1.6.5.3
  2. NADH dehydrogenase subunit 1
Target 4 Gene Name MT-ND1
Target 4 Protein Sequence >NADH-ubiquinone oxidoreductase chain 1
MPMANLLLLIVPILIAMAFLMLTERKILGYMQLRKGPNVVGPYGLLQPFADAMKLFTKEP
LKPATSTITLYITAPTLALTIALLLWTPLPMPNPLVNLNLGLLFILATSSLAVYSILWSG
WASNSNYALIGALRAVAQTISYEVTLAIILLSTLLMSGSFNLSTLITTQEHLWLLLPSWP
LAMMWFISTLAETNRTPFDLAEGESELVSGFNIEYAAGPFALFFMAEYTNIIMMNTLTTT
IFLGTTYDALSPELYTTYFVTKTLLLTSLFLWIRTAYPRFRYDQLMHLLWKNFLPLTLAL
LMWYVSMPITISSIPPQT
Target 4 Number of Residues 323
Target 4 Molecular Weight 35661
Target 4 Theoretical pI 6.53
Target 4 GO Classification
Function
Not Available
Process
metabolism
cellular metabolism
generation of precursor metabolites and energy
electron transport
physiological process
cellular physiological process
transport
Component
cell
membrane
Target 4 General Function Energy production and conversion
Target 4 Specific Function Not Available
Target 4 Pathways
Name SMPDB Link KEGG Link
Oxidative phosphorylation map00190 Link Image
Ubiquinone biosynthesis SMP00065 Link Image map00130 Link Image
Target 4 Reactions
  • NADH + H+ + ubiquinone = NAD+ + ubiquinol
Target 4 Pfam Domain Function
Target 4 Signals
  • None
Target 4 Transmembrane Regions
  • 4-23; 68-90; 100-122; 135-157; 172-191; 222-244; 254-273; 293-315
Target 4 Essentiality Non-Essential
Target 4 GenBank ID Protein 13004 Link Image
Target 4 UniProtKB/Swiss-Prot ID P03886 Link Image
Target 4 UniProtKB/Swiss-Prot Entry Name NU1M_HUMAN Link Image
Target 4 PDB ID Not Available
Target 4 Cellular Location
  • Mitochondrion
  • mitochondrial inner membrane
  • multi-pass membrane protein (Probable)
Target 4 Gene Sequence >957 bp
ATACCCATGGCCAACCTCCTACTCCTCATTGTACCCATTCTAATCGCAATGGCATTCCTA
ATGCTTACCGAACGAAAAATTCTAGGCTATATACAACTACGCAAAGGCCCCAACGTGGTA
GGCCCCTACGGGCTACTACAACCCTTCGCTGACGCCATAAAACTCTTCACCAAAGAGCCC
CTAAAACCCGCCACATCTACCATCACCCTCTACATCACCGCCCCGACCTTAGCTCTCACC
ATCGCTCTTCTACTATGAACCCCCCTCCCCATACCCAACCCCCTGGTCAACCTCAACCTA
GGCCTCCTATTTATTCTAGCCACCTCTAGCCTAGCCGTTTACTCAATCCTCTGATCAGGG
TGAGCATCAAACTCAAACTACGCCCTGATCGGCGCACTGCGAGCAGTAGCCCAAACAATC
TCATATGAAGTCACCCTAGCCATCATTCTACTATCAACATTACTAATAAGTGGCTCCTTT
AACCTCTCCACCCTTATCACAACACAAGAACACCTCTGATTACTCCTGCCATCATGACCC
TTGGCCATAATATGATTTATCTCCACACTAGCAGAGACCAACCGAACCCCCTTCGACCTT
GCCGAAGGGGAGTCCGAACTAGTCTCAGGCTTCAACATCGAATACGCCGCAGGCCCCTTC
GCCCTATTCTTCATAGCCGAATACACAAACATTATTATAATAAACACCCTCACCACTACA
ATCTTCCTAGGAACAACATATGACGCACTCTCCCCTGAACTCTACACAACATATTTTGTC
ACCAAGACCCTACTTCTAACCTCCCTGTTCTTATGAATTCGAACAGCATACCCCCGATTC
CGCTACGACCAACTCATACACCTCCTATGAAAAAACTTCCTACCACTCACCCTAGCATTA
CTTATATGATATGTCTCCATACCCATTACAATCTCCAGCATTCCCCCTCAAACCTAA
Target 4 GenBank Gene ID
Target 4 GeneCard ID MT-ND1 Link Image
Target 4 GenAtlas ID MT-ND1 Link Image
Target 4 HGNC ID HGNC:7455 Link Image
Target 4 Chromosome Location MT
Target 4 Locus -
Target 4 SNPs SNPJam Report Link Image
Target 4 General References
  1. Ingman M, Kaessmann H, Paabo S, Gyllensten U: Mitochondrial genome variation and the origin of modern humans. Nature. 2000 Dec 7;408(6813):708-13. [PubMed Link Image]
  2. Ingman M, Gyllensten U: Mitochondrial genome variation and evolutionary history of Australian and New Guinean aborigines. Genome Res. 2003 Jul;13(7):1600-6. [PubMed Link Image]
  3. Johns DR, Neufeld MJ, Park RD: An ND-6 mitochondrial DNA mutation associated with Leber hereditary optic neuropathy. Biochem Biophys Res Commun. 1992 Sep 30;187(3):1551-7. [PubMed Link Image]
  4. Huoponen K, Vilkki J, Aula P, Nikoskelainen EK, Savontaus ML: A new mtDNA mutation associated with Leber hereditary optic neuroretinopathy. Am J Hum Genet. 1991 Jun;48(6):1147-53. [PubMed Link Image]
  5. Marzuki S, Noer AS, Lertrit P, Thyagarajan D, Kapsa R, Utthanaphol P, Byrne E: Normal variants of human mitochondrial DNA and translation products: the building of a reference data base. Hum Genet. 1991 Dec;88(2):139-45. [PubMed Link Image]
  6. Johns DR, Berman J: Alternative, simultaneous complex I mitochondrial DNA mutations in Leber's hereditary optic neuropathy. Biochem Biophys Res Commun. 1991 Feb 14;174(3):1324-30. [PubMed Link Image]
  7. Howell N, Bindoff LA, McCullough DA, Kubacka I, Poulton J, Mackey D, Taylor L, Turnbull DM: Leber hereditary optic neuropathy: identification of the same mitochondrial ND1 mutation in six pedigrees. Am J Hum Genet. 1991 Nov;49(5):939-50. [PubMed Link Image]
  8. Majander A, Huoponen K, Savontaus ML, Nikoskelainen E, Wikstrom M: Electron transfer properties of NADH:ubiquinone reductase in the ND1/3460 and the ND4/11778 mutations of the Leber hereditary optic neuroretinopathy (LHON). FEBS Lett. 1991 Nov 4;292(1-2):289-92. [PubMed Link Image]
  9. Howell N, Kubacka I, Xu M, McCullough DA: Leber hereditary optic neuropathy: involvement of the mitochondrial ND1 gene and evidence for an intragenic suppressor mutation. Am J Hum Genet. 1991 May;48(5):935-42. [PubMed Link Image]
  10. Chomyn A, Mariottini P, Cleeter MW, Ragan CI, Matsuno-Yagi A, Hatefi Y, Doolittle RF, Attardi G: Six unidentified reading frames of human mitochondrial DNA encode components of the respiratory-chain NADH dehydrogenase. Nature. 1985 Apr 18-24;314(6012):592-7. [PubMed Link Image]
  11. 6260957 Sanger F, Coulson AR, Barrell BG, Smith AJ, Roe BA: Cloning in single-stranded bacteriophage as an aid to rapid DNA sequencing. J Mol Biol. 1980 Oct 25;143(2):161-78.
  12. 7219534 Anderson S, Bankier AT, Barrell BG, de Bruijn MH, Coulson AR, Drouin J, Eperon IC, Nierlich DP, Roe BA, Sanger F, Schreier PH, Smith AJ, Staden R, Young IG: Sequence and organization of the human mitochondrial genome. Nature. 1981 Apr 9;290(5806):457-65.
  13. 7530363 Horai S, Hayasaka K, Kondo R, Tsugane K, Takahata N: Recent African origin of modern humans revealed by complete sequences of hominoid mitochondrial DNAs. Proc Natl Acad Sci U S A. 1995 Jan 17;92(2):532-6.
  14. 7733935 Nakagawa Y, Ikegami H, Yamato E, Takekawa K, Fujisawa T, Hamada Y, Ueda H, Uchigata Y, Miki T, Kumahara Y, et al.: A new mitochondrial DNA mutation associated with non-insulin-dependent diabetes mellitus. Biochem Biophys Res Commun. 1995 Apr 17;209(2):664-8.
  15. 8104867 Shoffner JM, Brown MD, Torroni A, Lott MT, Cabell MF, Mirra SS, Beal MF, Yang CC, Gearing M, Salvo R, et al.: Mitochondrial DNA variants observed in Alzheimer disease and Parkinson disease patients. Genomics. 1993 Jul;17(1):171-84.
  16. 8723687 Jaksch M, Hofmann S, Kaufhold P, Obermaier-Kusser B, Zierz S, Gerbitz KD: A novel combination of mitochondrial tRNA and ND1 gene mutations in a syndrome with MELAS, cardiomyopathy, and diabetes mellitus. Hum Mutat. 1996;7(4):358-60.
Target 4 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 5 [top]
Target 5 ID 610
Target 5 Name Calcium-activated potassium channel subunit alpha 1
Target 5 Synonyms
  1. BK channel
  2. BKCA alpha
  3. Calcium-activated potassium channel, subfamily M subunit alpha 1
  4. K(VCA)alpha
  5. KCa1.1
  6. Maxi K channel
  7. MaxiK
  8. Slo homolog
  9. Slo-alpha
  10. Slo1
  11. Slowpoke homolog
  12. hSlo
Target 5 Gene Name KCNMA1
Target 5 Protein Sequence >Calcium-activated potassium channel subunit alpha 1
MANGGGGGGGSSGGGGGGGGSSLRMSSNIHANHLSLDASSSSSSSSSSSSSSSSSSSSSS
VHEPKMDALIIPVTMEVPCDSRGQRMWWAFLASSMVTFFGGLFIILLWRTLKYLWTVCCH
CGGKTKEAQKINNGSSQADGTLKPVDEKEEAVAAEVGWMTSVKDWAGVMISAQTLTGRVL
VVLVFALSIGALVIYFIDSSNPIESCQNFYKDFTLQIDMAFNVFFLLYFGLRFIAANDKL
WFWLEVNSVVDFFTVPPVFVSVYLNRSWLGLRFLRALRLIQFSEILQFLNILKTSNSIKL
VNLLSIFISTWLTAAGFIHLVENSGDPWENFQNNQALTYWECVYLLMVTMSTVGYGDVYA
KTTLGRLFMVFFILGGLAMFASYVPEIIELIGNRKKYGGSYSAVSGRKHIVVCGHITLES
VSNFLKDFLHKDRDDVNVEIVFLHNISPNLELEALFKRHFTQVEFYQGSVLNPHDLARVK
IESADACLILANKYCADPDAEDASNIMRVISIKNYHPKIRIITQMLQYHNKAHLLNIPSW
NWKEGDDAICLAELKLGFIAQSCLAQGLSTMLANLFSMRSFIKIEEDTWQKYYLEGVSNE
MYTEYLSSAFVGLSFPTVCELCFVKLKLLMIAIEYKSANRESRILINPGNHLKIQEGTLG
FFIASDAKEVKRAFFYCKACHDDITDPKRIKKCGCKRPKMSIYKRMRRACCFDCGRSERD
CSCMSGRVRGNVDTLERAFPLSSVSVNDCSTSFRAFEDEQPSTLSPKKKQRNGGMRNSPN
TSPKLMRHDPLLIPGNDQIDNMDSNVKKYDSTGMFHWCAPKEIEKVILTRSEAAMTVLSG
HVVVCIFGDVSSALIGLRNLVMPLRASNFHYHELKHIVFVGSIEYLKREWETLHNFPKVS
ILPGTPLSRADLRAVNINLCDMCVILSANQNNIDDTSLQDKECILASLNIKSMQFDDSIG
VLQANSQGFTPPGMDRSSPDNSPVHGMLRQPSITTGVNIPIITELVNDTNVQFLDQDDDD
DPDTELYLTQPFACGTAFAVSVLDSLMSATYFNDNILTLIRTLVTGGATPELEALIAEEN
ALRGGYSTPQTLANRDRCRVAQLALLDGPFADLGDGGCYGDLFCKALKTYNMLCFGIYRL
RDAHLSTPSQCTKRYVITNPPYEFELVPTDLIFCLMQFDHNAGQSRASLSHSSHSSQSSS
KKSSSVHSIPSTANRQNRPKSRESRDKQKYVQEERL
Target 5 Number of Residues 1256
Target 5 Molecular Weight 137561
Target 5 Theoretical pI 7.07
Target 5 GO Classification
Function
voltage-gated ion channel activity
voltage-gated potassium channel activity
transporter activity
ion transporter activity
ion channel activity
cation channel activity
potassium channel activity
calcium-activated potassium channel activity
Process
physiological process
cellular physiological process
transport
ion transport
cation transport
monovalent inorganic cation transport
potassium ion transport
Component
protein complex
voltage-gated potassium channel complex
cell
membrane
Target 5 General Function Inorganic ion transport and metabolism
Target 5 Specific Function Potassium channel activated by both membrane depolarization or increase in cytosolic Ca(2+) that mediates export of K(+). It is also activated by the concentration of cytosolic Mg(2+). Its activation dampens the excitatory events that elevate the cytosolic Ca(2+) concentration and/or depolarize the cell membrane. It therefore contributes to repolarization of the membrane potential. Plays a key role in controlling excitability in a number of systems, such as regulation of the contraction of smooth muscle, the tuning of hair cells in the cochlea, regulation of transmitter release, and innate immunity. In smooth muscles, its activation by high level of Ca(2+), caused by ryanodine receptors in the sarcoplasmic reticulum, regulates the membrane potential. In cochlea cells, its number and kinetic properties partly determine the characteristic frequency of each hair cell and thereby helps to establish a tonotopic map. Kinetics of KCNMA1 channels are determined by alternative splicing, phosphorylation status and its combination with modulating beta subunits. Highly sensitive to both iberiotoxin (IbTx) and charybdotoxin (CTX)
Target 5 Pathways Not Available
Target 5 Reactions Not Available
Target 5 Pfam Domain Function
Target 5 Signals
  • None
Target 5 Transmembrane Regions
  • 87-107
  • 179-199
  • 215-235
  • 240-260
  • 265-285
  • 301-321
  • 368-388
Target 5 Essentiality Non-Essential
Target 5 GenBank ID Protein 537439 Link Image
Target 5 UniProtKB/Swiss-Prot ID Q12791 Link Image
Target 5 UniProtKB/Swiss-Prot Entry Name KCMA1_HUMAN Link Image
Target 5 PDB ID Not Available
Target 5 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 5 Gene Sequence >3639 bp
ATGAGTAGCAATATCCACGCGAACCATCTCAGCCTAGACGCGTCCTCCTCCTCCTCCTCC
TCCTCTTCCTCTTCTTCTTCTTCCTCCTCCTCTTCCTCCTCGTCCTCGGTCCACGAGCCC
AAGATGGATGCGCTCATCATCCCGGTGACCATGGAGGTGCCGTGCGACAGCCGGGGCCAA
CGCATGTGGTGGGCTTTCCTGGCCTCCTCCATGGTGACTTTCTTCGGGGGCCTCTTCATC
ATCTTGCTCTGGCGGACGCTCAAGTACCTGTGGACCGTGTGCTGCCACTGCGGGGGCAAG
ACGAAGGAGGCCCAGAAGATTAACAATGGCTCAAGCCAGGCGGATGGCACTCTCAAACCA
GTGGATGAAAAAGAGGAGGCAGTGGCCGCCGAGGTCGGCTGGATGACCTCCGTGAAGGAC
TGGGCGGGGGTGATGATATCCGCCCAGACACTGACTGGCAGAGTCCTGGTTGTCTTAGTC
TTTGCTCTCAGCATCGGTGCACTTGTAATATACTTCATAGATTCATCAAACCCAATAGAA
TCCTGCCAGAATTTCTACAAAGATTTCACATTACAGATCGACATGGCTTTCAACGTGTTC
TTCCTTCTCTACTTCGGCTTGCGGTTTATTGCAGCCAACGATAAATTGTGGTTCTGGCTG
GAAGTGAACTCTGTAGTGGATTTCTTCACGGTGCCCCCCGTGTTTGTGTCTGTGTACTTA
AACAGAAGTTGGCTTGGTTTGAGATTTTTAAGAGCTCTGAGACTGATACAGTTTTCAGAA
ATTTTGCAGTTTCTGAATATTCTTAAAACAAGTAATTCCATCAAGCTGGTGAATCTGCTC
TCCATATTTATCAGCACGTGGCTGACTGCAGCCGGGTTCATCCATTTGGTGGAGAATTCA
GGGGACCCATGGGAAAATTTCCAAAACAACCAGGCTCTCACCTACTGGGAATGTGTCTAT
TTACTCATGGTCACAATGTCCACCGTTGGTTATGGGGATGTTTATGCAAAAACCACACTT
GGGCGCCTCTTCATGGTCTTCTTCATCCTCGGGGGACTGGCCATGTTTGCCAGCTACGTC
CCTGAAATCATAGAGTTAATAGGAAACCGCAAGAAATACGGGGGCTCCTATAGTGCGGTT
AGTGGAAGAAAGCACATTGTGGTCTGCGGACACATCACTCTGGAGAGTGTTTCCAACTTC
CTGAAGGACTTTCTGCACAAGGACCGGGATGACGTCAATGTGGAGATCGTTTTTCTTCAC
AACATCTCCCCCAACCTGGAGCTTGAAGCTCTGTTCAAACGACATTTTACTCAGGTGGAA
TTTTATCAGGGTTCCGTCCTCAATCCACATGATCTTGCAAGAGTCAAGATAGAGTCAGCA
GATGCATGCCTGATCCTTGCCAACAAGTACTGCGCTGACCCGGATGCGGAGGATGCCTCG
AATATCATGAGAGTAATCTCCATAAAGAACTACCATCCGAAGATAAGAATCATCACTCAA
ATGCTGCAGTATCACAACAAGGCCCATCTGCTAAACATCCCGAGCTGGAATTGGAAAGAA
GGTGATGACGCAATCTGCCTCGCAGAGTTGAAGTTGGGCTTCATAGCCCAGAGCTGCCTG
GCTCAAGGCCTCTCCACCATGCTTGCCAACCTCTTCTCCATGAGGTCATTCATAAAGATT
GAGGAAGACACATGGCAGAAATACTACTTGGAAGGAGTCTCAAATGAAATGTACACAGAA
TATCTCTCCAGTGCCTTCGTGGGTCTGTCCTTCCCTACTGTTTGTGAGCTGTGTTTTGTG
AAGCTCAAGCTCCTAATGATAGCCATTGAGTACAAGTCTGCCAACCGAGAGAGCCGTATA
TTAATTAATCCTGGAAACCATCTTAAGATCCAAGAAGGTACTTTAGGATTTTTCATCGCA
AGTGATGCCAAAGAAGTTAAAAGGGCATTTTTTTACTGCAAGGCCTGTCATGATGACATC
ACAGATCCCAAAAGAATAAAAAAATGTGGCTGCAAACGGCCCAAGATGTCCATCTACAAG
AGAATGAGACGGGCATGTTGTTTTGATTGCGGACGTTCTGAGCGTGACTGCTCATGCATG
TCAGGCCGTGTGCGTGGTAACGTGGACACCCTTGAGAGAGCCTTCCCACTTTCTTCTGTC
TCTGTTAATGATTGCTCCACCAGTTTCCGTGCCTTTGAAGATGAGCAGCCGTCAACACTA
TCACCAAAAAAAAAGCAACGGAATGGAGGCATGCGGAACTCACCCAACACCTCGCCTAAG
CTGATGAGGCATGACCCCTTGTTAATTCCTGGCAATGATCAGATTGACAACATGGACTCC
AATGTGAAGAAGTACGACTCTACTGGGATGTTTCACTGGTGTGCACCCAAGGAGATAGAG
AAAGTCATCCTGACTCGAAGTGAAGCTGCCATGACCGTCCTGAGTGGCCATGTCGTGGTC
TGCATCTTTGGCGACGTCAGCTCAGCCCTGATCGGCCTCCGGAACCTGGTGATGCCGCTC
CGTGCCAGCAACTTTCATTACCATGAGCTCAAGCACATTGTGTTTGTGGGCTCTATTGAG
TACCTCAAGCGGGAATGGGAGACGCTTCATAACTTCCCCAAAGTGTCCATATTGCCTGGT
ACGCCATTAAGTCGGGCTGATTTAAGGGCTGTCAACATCAACCTCTGTGACATGTGCGTT
ATCCTGTCAGCCAATCAGAATAATATTGATGATACTTCGCTGCAGGACAAGGAATGCATC
TTGGCGTCACTCAACATCAAATCTATGCAGTTTGATGACAGCATCGGAGTCTTGCAGGCT
AATTCCCAAGGGTTCACACCTCCAGGAATGGATAGATCCTCTCCAGATAACAGCCCAGTG
CACGGGATGTTACGTCAACCATCCATCACAACTGGGGTCAACATCCCCATCATCACTGAA
CTAGTGAACGATACTAATGTTCAGTTTTTGGACCAAGACGATGATGATGACCCTGATACA
GAACTGTACCTCACGCAGCCCTTTGCCTGTGGGACAGCATTTGCCGTCAGTGTCCTGGAC
TCACTCATGAGCGCGACGTACTTCAATGACAATATCCTCACCCTGATACGGACCCTGGTG
ACCGGAGGAGCCACGCCGGAGCTGGAGGCTCTGATTGCTGAGGAAAACGCCCTTAGAGGT
GGCTACAGCACCCCGCAGACACTGGCCAATAGGGACCGCTGCCGCGTGGCCCAGTTAGCT
CTGCTCGATGGGCCATTTGCGGACTTAGGGGATGGTGGTTGTTATGGTGATCTGTTCTGC
AAAGCTCTGAAAACATATAATATGCTTTGTTTTGGAATTTACCGGCTGAGAGATGCTCAC
CTCAGCACCCCCAGTCAGTGCACAAAGAGGTATGTCATCACCAACCCGCCCTATGAGTTT
GAGCTCGTGCCGACGGACCTGATCTTCTGCTTAATGCAGTTTGACCACAATGCCGGCCAG
TCCCGGGCCAGCCTGTCCCATTCCTCCCACTCGTCGCAGTCCTCCAGCAAGAAGAGCTCC
TCTGTTCACTCCATCCCATCCACAGCAAACCGACAGAACCGGCCCAAGTCCAGGGAGTCC
CGGGACAAACAGAAGTACGTGCAGGAAGAGCGGCTTTGA
Target 5 GenBank Gene ID
Target 5 GeneCard ID KCNMA1 Link Image
Target 5 GenAtlas ID KCNMA1 Link Image
Target 5 HGNC ID HGNC:6284 Link Image
Target 5 Chromosome Location 10
Target 5 Locus 10q22.3
Target 5 SNPs SNPJam Report Link Image
Target 5 General References
  1. Wallner M, Meera P, Toro L: Molecular basis of fast inactivation in voltage and Ca2+-activated K+ channels: a transmembrane beta-subunit homolog. Proc Natl Acad Sci U S A. 1999 Mar 30;96(7):4137-42. [PubMed Link Image]
  2. Brenner R, Jegla TJ, Wickenden A, Liu Y, Aldrich RW: Cloning and functional characterization of novel large conductance calcium-activated potassium channel beta subunits, hKCNMB3 and hKCNMB4. J Biol Chem. 2000 Mar 3;275(9):6453-61. [PubMed Link Image]
  3. McCobb DP, Fowler NL, Featherstone T, Lingle CJ, Saito M, Krause JE, Salkoff L: A human calcium-activated potassium channel gene expressed in vascular smooth muscle. Am J Physiol. 1995 Sep;269(3 Pt 2):H767-77. [PubMed Link Image]
  4. Dworetzky SI, Trojnacki JT, Gribkoff VK: Cloning and expression of a human large-conductance calcium-activated potassium channel. Brain Res Mol Brain Res. 1994 Nov;27(1):189-93. [PubMed Link Image]
  5. Pallanck L, Ganetzky B: Cloning and characterization of human and mouse homologs of the Drosophila calcium-activated potassium channel gene, slowpoke. Hum Mol Genet. 1994 Aug;3(8):1239-43. [PubMed Link Image]
  6. Tseng-Crank J, Foster CD, Krause JD, Mertz R, Godinot N, DiChiara TJ, Reinhart PH: Cloning, expression, and distribution of functionally distinct Ca(2+)-activated K+ channel isoforms from human brain. Neuron. 1994 Dec;13(6):1315-30. [PubMed Link Image]
  7. Wallner M, Meera P, Ottolia M, Kaczorowski GJ, Latorre R, Garcia ML, Stefani E, Toro L: Characterization of and modulation by a beta-subunit of a human maxi KCa channel cloned from myometrium. Receptors Channels. 1995;3(3):185-99. [PubMed Link Image]
  8. Wallner M, Meera P, Toro L: Determinant for beta-subunit regulation in high-conductance voltage-activated and Ca(2+)-sensitive K+ channels: an additional transmembrane region at the N terminus. Proc Natl Acad Sci U S A. 1996 Dec 10;93(25):14922-7. [PubMed Link Image]
  9. Meera P, Wallner M, Song M, Toro L: Large conductance voltage- and calcium-dependent K+ channel, a distinct member of voltage-dependent ion channels with seven N-terminal transmembrane segments (S0-S6), an extracellular N terminus, and an intracellular (S9-S10) C terminus. Proc Natl Acad Sci U S A. 1997 Dec 9;94(25):14066-71. [PubMed Link Image]
Target 5 Drug References
  1. Namba T, Ishii TM, Ikeda M, Hisano T, Itoh T, Hirota K, Adelman JP, Fukuda K: Inhibition of the human intermediate conductance Ca(2+)-activated K(+) channel, hIK1, by volatile anesthetics. Eur J Pharmacol. 2000 Apr 28;395(2):95-101. [PubMed Link Image]
  2. Antkowiak B, Kirschfeld K: Enflurane is a potent inhibitor of high conductance Ca(2+)-activated K+ channels of Chara australis. FEBS Lett. 1992 Nov 30;313(3):281-4. [PubMed Link Image]
Drug Target 6 [top]
Target 6 ID 705
Target 6 Name Glutamate receptor 1
Target 6 Synonyms
  1. AMPA-selective glutamate receptor 1
  2. GluR-1
  3. GluR-A
  4. GluR-K1
  5. Glutamate receptor 1 precursor
  6. Glutamate receptor ionotropic, AMPA 1
Target 6 Gene Name GRIA1
Target 6 Protein Sequence >Glutamate receptor 1 precursor
MQHIFAFFCTGFLGAVVGANFPNNIQIGGLFPNQQSQEHAAFRFALSQLTEPPKLLPQID
IVNISDSFEMTYRFCSQFSKGVYAIFGFYERRTVNMLTSFCGALHVCFITPSFPVDTSNQ
FVLQLRPELQDALISIIDHYKWQKFVYIYDADRGLSVLQKVLDTAAEKNWQVTAVNILTT
TEEGYRMLFQDLEKKKERLVVVDCESERLNAILGQIIKLEKNGIGYHYILANLGFMDIDL
NKFKESGANVTGFQLVNYTDTIPAKIMQQWKNSDARDHTRVDWKRPKYTSALTYDGVKVM
AEAFQSLRRQRIDISRRGNAGDCLANPAVPWGQGIDIQRALQQVRFEGLTGNVQFNEKGR
RTNYTLHVIEMKHDGIRKIGYWNEDDKFVPAATDAQAGGDNSSVQNRTYIVTTILEDPYV
MLKKNANQFEGNDRYEGYCVELAAEIAKHVGYSYRLEIVSDGKYGARDPDTKAWNGMVGE
LVYGRADVAVAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLDPLAYEIW
MCIVFAYIGVSVVLFLVSRFSPYEWHSEEFEEGRDQTTSDQSNEFGIFNSLWFSLGAFMQ
QGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDLAKQTEIA
YGTLEAGSTKEFFRRSKIAVFEKMWTYMKSAEPSVFVRTTEEGMIRVRKSKGKYAYLLES
TMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSALRNPVNLAVLKLNEQGLLDKLKNKW
WYDKGECGSGGGDSKDKTSALSLSNVAGVFYILIGGLGLAMLVALIEFCYKSRSESKRMK
GFCLIPQQSINEAIRTSTLPRNSGAGASSGGSGENGRVVSHDFPKSMQSIPCMSHSSGMP
LGATGL
Target 6 Number of Residues 921
Target 6 Molecular Weight 101507
Target 6 Theoretical pI 7.78
Target 6 GO Classification
Function
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
excitatory extracellular ligand-gated ion channel activity
glutamate-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
glutamate receptor activity
ionotropic glutamate receptor activity
Process
physiological process
cellular physiological process
transport
ion transport
Component
cell
membrane
Target 6 General Function Involved in ionotropic glutamate receptor activity
Target 6 Specific Function L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. The postsynaptic actions of Glu are mediated by a variety of receptors that are named according to their selective agonists
Target 6 Pathways Not Available
Target 6 Reactions Not Available
Target 6 Pfam Domain Function
Target 6 Signals
  • 1-18
Target 6 Transmembrane Regions
  • 537-557
  • 585-605
  • 618-638
  • 806-826
Target 6 Essentiality Non-Essential
Target 6 GenBank ID Protein 183281 Link Image
Target 6 UniProtKB/Swiss-Prot ID P42261 Link Image
Target 6 UniProtKB/Swiss-Prot Entry Name GRIA1_HUMAN Link Image
Target 6 PDB ID 1WVJ Link Image
Target 6 PDB File Show
Target 6 3D Structure
Target 6 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 6 Gene Sequence >2724 bp
ATGCAGCACATTTTTGCCTTCTTCTGCACCGGTTTCCTAGGCGCGGTAGTAGGTGCCAAT
TTCCCCAACAATATCCAGATCGGGGGATTATTTCCAAACCAGCAGTCACAGGAACATGCT
GCTTTTAGATTTGCTTTGTCGCAACTCACAGAGCCCCCGAAGCTGCTCCCCCAGATTGAT
ATTGTGAACATCAGCGACAGCTTTGAGATGACCTATAGATTCTGTTCCCAGTTCTCCAAA
GGAGTCTATGCCATCTTTGGGTTTTATGAACGTAGGACTGTCAACATGCTGACCTCCTTT
TGTGGGGCCCTCCACGTCTGCTTCATTACGCCGAGCTTTCCCGTTGATACATCCAATCAG
TTTGTCCTTCAGCTGCGCCCTGAACTGCAGGATGCCCTCATCAGCATCATTGACCATTAC
AAGTGGCAGAAATTTGTCTACATTTATGATGCCGACCGGGGCTTATCCGTCCTGCAGAAA
GTCCTGGATACAGCTGCTGAGAAGAACTGGCAGGTGACAGCAGTCAACATCTTGACAACC
ACAGAGGAGGGATACCGGATGCTCTTTCAGGACCTGGAGAAGAAAAAGGAGCGGCTGGTG
GTGGTGGACTGTGAATCAGAACGCCTCAATGCTATCTTGGGCCAGATTATAAAGCTAGAG
AAGAATGGCATCGGCTACCACTACATTCTTGCAAATCTGGGCTTCATGGACATTGACTTA
AACAAATTCAAGGAGAGTGGCGCCAATGTGACAGGTTTCCAGCTGGTGAACTACACAGAC
ACTATTCCGGCCAAGATCATGCAGCAGTGGAAGAATAGTGATGCTCGAGACCACACACGG
GTGGACTGGAAGAGACCCAAGTACACCTCTGCGCTCACCTACGATGGGGTGAAGGTGATG
GCTGAGGCTTTCCAGAGCCTGCGGAGGCAGAGAATTGATATATCTCGCCGGGGGAATGCT
GGGGATTGTCTGGCTAACCCAGCTGTTCCCTGGGGCCAAGGGATCGACATCCAGAGAGCT
CTGCAGCAGGTGCGATTTGAAGGTTTAACAGGAAACGTGCAGTTTAATGAGAAAGGACGC
CGGACCAACTACACGCTCCACGTGATTGAAATGAAACATGACGGCATCCGAAAGATTGGT
TACTGGAATGAAGATGATAAGTTTGTCCCTGCAGCCACCGATGCCCAAGCTGGGGGCGAT
AATTCAAGTGTTCAGAACAGAACATACATCGTCACAACAATCCTAGAAGATCCTTATGTG
ATGCTCAAGAAGAACGCCAATCAGTTTGAGGGCAATGACCGTTACGAGGGCTACTGTGTA
GAGCTGGCGGCAGAGATTGCCAAGCACGTGGGCTACTCCTACCGTCTGGAGATTGTCAGT
GATGGAAAATACGGAGCCCGAGACCCTGACACGAAGGCCTGGAATGGCATGGTGGGAGAG
CTGGTCTATGGAAGAGCAGATGTGGCTGTGGCTCCCTTAACTATCACTTTGGTCCGGGAA
GAAGTTATAGATTTCTCCAAACCATTTATGAGTTTGGGGATCTCCATCATGATTAAAAAA
CCACAGAAATCCAAGCCGGGTGTCTTCTCCTTCCTTGATCCTTTGGCTTATGAGATTTGG
ATGTGCATTGTTTTTGCCTACATTGGAGTGAGTGTTGTCCTCTTCCTGGTCAGCCGCTTC
AGTCCCTATGAATGGCACAGTGAAGAGTTTGAGGAAGGACGGGACCAGACAACCAGTGAC
CAGTCCAATGAGTTTGGGATATTCAACAGTTTGTGGTTCTCCCTGGGAGCCTTCATGCAG
CAAGGATGTGACATTTCTCCCAGGTCCCTGTCTGGTCGCATCGTTGGTGGCGTCTGGTGG
TTCTTCACCTTAATCATCATCTCCTCATATACAGCCAATCTGGCCGCCTTCCTGACCGTG
GAGAGGATGGTGTCTCCCATTGAGAGTGCAGAGGACCTAGCGAAGCAGACAGAAATTGCC
TACGGGACGCTGGAAGCAGGATCTACTAAGGAGTTCTTCAGGAGGTCTAAAATTGCTGTG
TTTGAGAAGATGTGGACATACATGAAGTCAGCAGAGCCATCAGTTTTTGTGCGGACCACA
GAGGAGGGGATGATTCGAGTGAGGAAATCCAAAGGCAAATATGCCTACCTCCTGGAGTCC
ACCATGAATGAGTACATTGAGCAGCGGAAACCCTGTGACACCATGAAGGTGGGAGGTAAC
TTGGATTCCAAAGGCTATGGCATTGCAACACCCAAGGGGTCTGCCCTGAGAGGTCCCGTA
AACCTAGCGGTTTTGAAACTCAGTGAGCAAGGCGTCTTAGACAAGCTGAAAAGCAAATGG
TGGTACGATAAAGGGGAATGTGGAAGCAAGGACTCCGGAAGTAAGGACAAGACAAGCGCT
CTGAGCCTCAGCAATGTGGCAGGCGTGTTCTACATCCTGATCGGAGGACTTGGACTAGCC
ATGCTGGTTGCCTTAATCGAGTTCTGCTACAAATCCCGTAGTGAATCCAAGCGGATGAAG
GGTTTTTGTTTGATCCCACAGCAATCCATCAACGAAGCCATACGGACATCGACCCTCCCC
CGCAACAGCGCGGGCACGGCACCGAGCAGCGGCGGCAGTGGAGAGAATGGTCGGGTGGTC
AGCCATGACTTCCCCAAGTCCATGCAATCGATTCCTTGCATGAGCCACAGTTCAGGGATG
CCCTTGGGAGCCACGGGATTGTAA
Target 6 GenBank Gene ID
Target 6 GeneCard ID GRIA1 Link Image
Target 6 GenAtlas ID GRIA1 Link Image
Target 6 HGNC ID HGNC:4571 Link Image
Target 6 Chromosome Location 5
Target 6 Locus 5q33|5q31.1
Target 6 SNPs SNPJam Report Link Image
Target 6 General References
  1. Sun W, Ferrer-Montiel AV, Schinder AF, McPherson JP, Evans GA, Montal M: Molecular cloning, chromosomal mapping, and functional expression of human brain glutamate receptors. Proc Natl Acad Sci U S A. 1992 Feb 15;89(4):1443-7. [PubMed Link Image]
  2. Potier MC, Spillantini MG, Carter NP: The human glutamate receptor cDNA GluR1: cloning, sequencing, expression and localization to chromosome 5. DNA Seq. 1992;2(4):211-8. [PubMed Link Image]
  3. Puckett C, Gomez CM, Korenberg JR, Tung H, Meier TJ, Chen XN, Hood L: Molecular cloning and chromosomal localization of one of the human glutamate receptor genes. Proc Natl Acad Sci U S A. 1991 Sep 1;88(17):7557-61. [PubMed Link Image]
Target 6 Drug References
  1. Dildy-Mayfield JE, Eger EI 2nd, Harris RA: Anesthetics produce subunit-selective actions on glutamate receptors. J Pharmacol Exp Ther. 1996 Mar;276(3):1058-65. [PubMed Link Image]
Drug Target 7 [top]
Target 7 ID 858
Target 7 Name Potassium voltage-gated channel subfamily A member 1
Target 7 Synonyms
  1. HBK1
  2. HUKI
  3. Voltage-gated potassium channel subunit Kv1.1
Target 7 Gene Name KCNA1
Target 7 Protein Sequence >Potassium voltage-gated channel subfamily A member 1
MTVMSGENVDEASAAPGHPQDGSYPRQADHDDHECCERVVINISGLRFETQLKTLAQFPN
TLLGNPKKRMRYFDPLRNEYFFDRNRPSFDAILYYYQSGGRLRRPVNVPLDMFSEEIKFY
ELGEEAMEKFREDEGFIKEEERPLPEKEYQRQVWLLFEYPESSGPARVIAIVSVMVILIS
IVIFCLETLPELKDDKDFTGTVHRIDNTTVIYNSNIFTDPFFIVETLCIIWFSFELVVRF
FACPSKTDFFKNIMNFIDIVAIIPYFITLGTEIAEQEGNQKGEQATSLAILRVIRLVRVF
RIFKLSRHSKGLQILGQTLKASMRELGLLIFFLFIGVILFSSAVYFAEAEEAESHFSSIP
DAFWWAVVSMTTVGYGDMYPVTIGGKIVGSLCAIAGVLTIALPVPVIVSNFNYFYHRETE
GEEQAQLLHVSSPNLASDSDLSRRSSSTMSKYEYMEIEEDMNNSIAHYRQVNIRTANCTT
ANQNCVNKSKLLTDV
Target 7 Number of Residues 503
Target 7 Molecular Weight 56542
Target 7 Theoretical pI 4.82
Target 7 GO Classification
Function
voltage-gated ion channel activity
voltage-gated potassium channel activity
transporter activity
ion transporter activity
ion channel activity
binding
protein binding
Process
cation transport
monovalent inorganic cation transport
potassium ion transport
physiological process
cellular physiological process
transport
ion transport
Component
protein complex
voltage-gated potassium channel complex
cell
membrane
Target 7 General Function Inorganic ion transport and metabolism
Target 7 Specific Function Mediates the voltage-dependent potassium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a potassium-selective channel through which potassium ions may pass in accordance with their electrochemical gradient
Target 7 Pathways Not Available
Target 7 Reactions Not Available
Target 7 Pfam Domain Function
Target 7 Signals
  • None
Target 7 Transmembrane Regions
  • 168-186
  • 221-242
  • 254-274
  • 290-309
  • 326-345
  • 387-408
Target 7 Essentiality Non-Essential
Target 7 GenBank ID Protein 186663 Link Image
Target 7 UniProtKB/Swiss-Prot ID Q09470 Link Image
Target 7 UniProtKB/Swiss-Prot Entry Name KCNA1_HUMAN Link Image
Target 7 PDB ID 1EXB Link Image
Target 7 PDB File Show
Target 7 3D Structure
Target 7 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 7 Gene Sequence >1488 bp
ATGACGGTGATGTCTGGGGAGAACGTGGACGAGGCTTCGGCCGCCCCGGGCCACCCCCAG
GATGGCAGCTACCCCCGCCAGGCCGACCACGACGACCACGAGTGCTGCGAGCGCGTGGTG
ATCAACATCTCCGGGCTGCGCTTCGAGACGCAGCTCAAGACCCTGGCGCAGTTCCCCAAC
ACGCTGCTGGGCAACCCTAAGAAACGCATGCGCTACTTCGACCCCCTGAGGAACGAGTAC
TTCTTCGACCGCAACCGGCCCAGCTTCGACGCCATCCTCTACTACTACCAGTCCGGCGGC
CGCCTGCGGAGGCCGGTCAACGTGCCCCTGGACATGTTCTCCGAGGAGATCAAGTTTTAC
GAGTTGGGCGAGGAGGCCATGGAGAAGTTCCGGGAGGACGAGGGCTTCATCAAGGAGGAG
GAGCGCCCTCTGCCCGAGAAGGAGTACCAGCGCCAGGTGTGGCTGCTCTTCGAGTACCCC
GAGAGCTCGGGGCCCGCCAGGGTCATCGCCATCGTCTCCGTCATGGTCATCCTCATCTCC
ATCGTCATCTTTTGCCTGGAGACGCTCCCCGAGCTGAAGGATGACAAGGACTTCACGGGC
ACCGTCCACCGCATCGACAACACCACGGTCATCTACAATTCCAACATCTTCACAGACCCC
TTCTTCATCGTGGAAACGCTGTGCATCATCTGGTTCTCCTTCGAGCTGGTGGTGCGCTTC
TTCGCCTGCCCCAGCAAGACGGACTTCTTCAAAAACATCATGAACTTCATAGACATTGTG
GCCATCATTCCTTATTTCATCACCCTGGGCACCGAGATAGCTGAGCAGGAAGGAAACCAG
AAGGGCGAGCAGGCCACCTCCCTGGCCATCCTCAGGGTCATCCGCTTGGTAAGGGTTTTT
AGAATCTTCAAGCTCTCCCGCCACTCTAAGGGCCTCCAGATCCTGGGCCAGACCCTCAAA
GCTAGTATGAGAGAGCTAGGGCTGCTCATCTTTTTCCTCTTCATCGGGGTCATCCTGTTT
TCTAGTGCAGTGTACTTTGCCGAGGCGGAAGAAGCTGAGTCGCACTTCTCCAGTATCCCC
GATGCTTTCTGGTGGGCGGTGGTGTCCATGACCACTGTAGGATACGGTGACATGTACCCT
GTGACAATTGGAGGCAAGATCGTGGGCTCCTTGTGTGCCATCGCTGGTGTGCTAACAATT
GCCCTGCCCGTACCTGTCATTGTGTCCAATTTCAACTATTTCTACCACCGAGAAACTGAG
GGGGAAGAGCAGGCTCAGTTGCTCCACGTCAGTTCCCCTAACTTAGCCTCTGACAGTGAC
CTCAGTCGCCGCAGTTCCTCTACTATGAGCAAGTATGAGTACATGGAGATCGAAGAGGAT
ATGAATAATAGCATAGCCCATTATAGACAGGTCAATATCAGAACTGCCAATTGCACCACA
GCTAACCAAAACTGCGTTAATAAGAGCAAGCTACTGACCGATGTTTAA
Target 7 GenBank Gene ID
Target 7 GeneCard ID KCNA1 Link Image
Target 7 GenAtlas ID KCNA1 Link Image
Target 7 HGNC ID HGNC:6218 Link Image
Target 7 Chromosome Location 12
Target 7 Locus 12p13
Target 7 SNPs SNPJam Report Link Image
Target 7 General References
  1. Hoopengardner B, Bhalla T, Staber C, Reenan R: Nervous system targets of RNA editing identified by comparative genomics. Science. 2003 Aug 8;301(5634):832-6. [PubMed Link Image]
  2. Browne DL, Gancher ST, Nutt JG, Brunt ER, Smith EA, Kramer P, Litt M: Episodic ataxia/myokymia syndrome is associated with point mutations in the human potassium channel gene, KCNA1. Nat Genet. 1994 Oct;8(2):136-40. [PubMed Link Image]
  3. Scheffer H, Brunt ER, Mol GJ, van der Vlies P, Stulp RP, Verlind E, Mantel G, Averyanov YN, Hofstra RM, Buys CH: Three novel KCNA1 mutations in episodic ataxia type I families. Hum Genet. 1998 Apr;102(4):464-6. [PubMed Link Image]
Target 7 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 8 [top]
Target 8 ID 872
Target 8 Name Gamma-aminobutyric-acid receptor subunit alpha-1
Target 8 Synonyms
  1. Gamma-aminobutyric-acid receptor subunit alpha-1 precursor
Target 8 Gene Name GABRA1
Target 8 Protein Sequence >Gamma-aminobutyric-acid receptor subunit alpha-1 precursor
MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPG
LGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHAC
PLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVM
TTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDP
LIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKID
RLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
Target 8 Number of Residues 463
Target 8 Molecular Weight 51802
Target 8 Theoretical pI 9.61
Target 8 GO Classification
Function
neurotransmitter receptor activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
GABA receptor activity
GABA-A receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
gamma-aminobutyric acid signaling pathway
anion transport
inorganic anion transport
chloride transport
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 8 General Function Involved in GABA-A receptor activity
Target 8 Specific Function GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel
Target 8 Pathways Not Available
Target 8 Reactions Not Available
Target 8 Pfam Domain Function
Target 8 Signals
  • 1-27
Target 8 Transmembrane Regions
  • 252-273
  • 279-300
  • 313-334
  • 422-443
Target 8 Essentiality Non-Essential
Target 8 GenBank ID Protein 31631 Link Image
Target 8 UniProtKB/Swiss-Prot ID P14867 Link Image
Target 8 UniProtKB/Swiss-Prot Entry Name GBRA1_HUMAN Link Image
Target 8 PDB ID Not Available
Target 8 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 8 Gene Sequence >1371 bp
ATGAGGAAAAGTCCAGGTCTGTCTGACTGTCTTTGGGCCTGGATCCTCCTTCTGAGCACA
CTGACTGGAAGAAGCTATGGACAGCCGTCATTACAAGATGAACTTAAAGACAATACCACT
GTCTTCACCAGGATTTTGGACAGACTCCTAGATGGTTATGACAATCGCCTGAGACCAGGA
TTGGGAGAGCGTGTAACCGAAGTGAAGACTGATATCTTCGTCACCAGTTTCGGACCCGTT
TCAGACCATGATATGGAATATACAATAGATGTATTTTTCCGTCAAAGCTGGAAGGATGAA
AGGTTAAAATTTAAAGGACCTATGACAGTCCTCCGGTTAAATAACCTAATGGCAAGTAAA
ATCTGGACTCCGGACACATTTTTCCACAATGGAAAGAAGTCAGTGGCCCACAACATGACC
ATGCCCAACAAACTCCTGCGGATCACAGAGGATGGCACCTTGCTGTACACCATGAGGCTG
ACAGTGAGAGCTGAATGTCCGATGCATTTGGAGGACTTCCCTATGGATGCCCATGCTTGC
CCACTAAAATTTGGAAGTTATGCTTATACAAGAGCAGAAGTTGTTTATGAATGGACCAGA
GAGCCAGCACGCTCAGTGGTTGTAGCAGAAGATGGATCACGTCTAAACCAGTATGACCTT
CTTGGACAAACAGTAGACTCTGGAATTGTCCAGTCAAGTACAGGAGAATATGTTGTTATG
ACCACTCATTTCCACTTGAAGAGAAAGATTGGCTACTTTGTTATTCAAACATACCTGCCA
TGCATAATGACAGTGATTCTCTCACAAGTCTCCTTCTGGCTCAACAGAGAGTCTGTACCA
GCAAGAACTGTCTTTGGAGTAACAACTGTGCTCACCATGACAACATTGAGCATCAGTGCC
AGAAACTCCCTCCCTAAGGTGGCTTATGCAACAGCTATGGATTGGTTTATTGCCGTGTGC
TATGCCTTTGTGTTCTCAGCTCTGATTGAGTTTGCCACAGTAAACTATTTCACTAAGAGA
GGTTATGCATGGGATGGCAAAAGTGTGGTTCCAGAAAAGCCAAAGAAAGTAAAGGATCCT
CTTATTAAGAAAAACAACACTTACGCTCCAACAGCAACCAGCTACACCCCTAATTTGGCC
AGGGGCGACCCGGGCTTAGCCACCATTGCTAAAAGTGCAACCATAGAACCTAAAGAGGTC
AAGCCCGAAACAAAACCACCAGAACCCAAGAAAACCTTTAACAGTGTCAGCAAAATTGAC
CGACTGTCAAGAATAGCCTTCCCGCTGCTATTTGGAATCTTTAACTTAGTCTACTGGGCT
ACGTATTTAAACAGAGAGCCTCAGCTAAAAGCCCCCACACCACATCAATAG
Target 8 GenBank Gene ID
Target 8 GeneCard ID GABRA1 Link Image
Target 8 GenAtlas ID GABRA1 Link Image
Target 8 HGNC ID HGNC:4075 Link Image
Target 8 Chromosome Location 5
Target 8 Locus 5q34-q35
Target 8 SNPs SNPJam Report Link Image
Target 8 General References
  1. Cossette P, Liu L, Brisebois K, Dong H, Lortie A, Vanasse M, Saint-Hilaire JM, Carmant L, Verner A, Lu WY, Wang YT, Rouleau GA: Mutation of GABRA1 in an autosomal dominant form of juvenile myoclonic epilepsy. Nat Genet. 2002 Jun;31(2):184-9. Epub 2002 May 6. [PubMed Link Image]
  2. Schofield PR, Pritchett DB, Sontheimer H, Kettenmann H, Seeburg PH: Sequence and expression of human GABAA receptor alpha 1 and beta 1 subunits. FEBS Lett. 1989 Feb 27;244(2):361-4. [PubMed Link Image]
  3. Garrett KM, Duman RS, Saito N, Blume AJ, Vitek MP, Tallman JF: Isolation of a cDNA clone for the alpha subunit of the human GABA-A receptor. Biochem Biophys Res Commun. 1988 Oct 31;156(2):1039-45. [PubMed Link Image]
Target 8 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.