| Version |
2.5 |
| Creation Date |
2005-06-13 13:24:05 |
| Update Date |
2009-02-19 16:05:10 |
| Primary Accession Number |
DB00709 |
| Secondary Accession Number |
|
| Name |
Lamivudine |
| Drug Type |
- Approved
- Investigational
- Small Molecule
|
| Description |
A reverse transcriptase inhibitor and zalcitabine analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat HIV disease. [PubChem] |
| Synonyms |
- Lamivudine [Usan:Ban:Inn]
- lamivudine
|
| Brand Names |
- 3TC
- Epivir
- Epivir-HBV
- Epzicom
- Hepitec
- Heptovir
- Zeffix
|
| Brand Mixtures |
- Combivir (Lamivudine + Zidovudine)
- Kivexa (Abacavir (Abacavir Sulfate) + Lamivudine)
- Trizivir (Abacavir (Abacavir Sulfate) + Lamivudine + Zidovudine)
|
| Chemical IUPAC Name |
4-amino-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one |
| Chemical Formula |
C8H11N3O3S |
| Chemical Structure |
 |
| CAS Registry Number |
134678-17-4 |
| InChI Identifier |
InChI=1/C8H11N3O3S/c9-5-1-2-11(8(13)10-5)6-4-15-7(3-12)14-6/h1-2,6-7,12H,3-4H2,(H2,9,10,13)/t6-,7+/m0/s1/f/h9H2 |
| InChI Key |
JTEGQNOMFQHVDC-IRNSGEEPDS |
| KEGG Drug |
D00353  |
| KEGG Compound |
C07065  |
| PubChem Compound |
60825  |
| PubChem Substance |
197069  |
| ChEBI ID |
Not Available |
| PharmGKB ID |
PA450163  |
| HET ID |
Not Available |
| GenBank ID |
Not Available |
| Drug ID Number [DIN] |
02239194  |
| RxList Link |
http://www.rxlist.com/cgi/generic3/lamivudine.htm  |
| PDRhealth Link |
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/com1513.shtml  |
| Wikipedia Link |
http://en.wikipedia.org/wiki/Lamivudine  |
| FDA Label |
|
| Material Safety Data Sheet (MSDS) |
|
| Synthesis Reference |
Not Available |
| Average Molecular Weight |
229.2560 |
| Monoisotopic Molecular Weight |
229.0521 |
| State |
Solid |
| Melting Point |
160-162 oC |
| Experimental Water Solubility |
70 mg/ml
Source: PhysProp
|
| Predicted Water Solubility |
2.76e+00 mg/mL
Calculated using ALOGPS
|
| Experimental LogP/Hydrophobicity |
-1.4
Source: PhysProp
|
| Predicted LogP |
-1.28
Calculated using ALOGPS
|
| Experimental LogS |
Not Available |
| Predicted LogS |
-1.92
Calculated using ALOGPS
|
| Experimental Caco2 Permeability |
Not Available |
| pKa/Isoelectric Point |
Not Available |
| Mass Spectrum |
Not Available
|
| MOL File |
Show | Download  |
| SDF File |
Show | Download  |
| PDB File |
Show | Download  |
| 2D Structure |
|
| 3D Structure |
|
| Experimental PDB ID |
Not Available |
| Isomeric SMILES |
NC1=NC(=O)N(C=C1)[C@@H]1CS[C@H](CO)O1 |
| Canonical SMILES |
NC1=NC(=O)N(C=C1)C1CSC(CO)O1 |
| Drug Category |
- Anti-HIV Agents
- Nucleoside and Nucleotide Reverse Transcriptase Inhibitors
- Reverse Transcriptase Inhibitors
|
| ATC Codes |
|
| AHFS Codes |
|
| Indication |
For the treatment of HIV infection and chronic hepatitis B (HBV). |
| Pharmacology |
Lamivudine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1) and hepatitis B (HBV). Lamivudine is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcriptase enzyme competitively and act as a chain terminator of DNA synthesis. The lack of a 3'-OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated. |
| Mechanism of Action |
Lamivudine is a synthetic nucleoside analogue and is phosphorylated intracellularly to its active 5'-triphosphate metabolite, lamivudine triphosphate (L-TP). This nucleoside analogue is incorporated into viral DNA by HIV reverse transcriptase and HBV polymerase, resulting in DNA chain termination. |
| Absorption |
Lamivudine was rapidly absorbed after oral administration in HIV-infected patients. Absolute bioavailability in adults is 86% ± 16% for the tablet and 87% ± 13% for the oral solution. |
| Toxicity |
Not Available |
| Protein Binding |
36% |
| Biotransformation |
The only detected metabolite of lamivudine is trans-sulfoxide. |
| Half Life |
5 to 7 hours |
| Dosage Forms |
| Form |
Route |
| Solution |
Oral |
| Tablet |
Oral |
|
| Patient Information |
Show  |
| Contraindications |
Show  |
| Interactions |
Show  |
| Drug Interactions |
| Drug |
Interaction |
| Zalcitabine |
Lamivudine decreases the efficacy of zalcitabine |
|
| Food Interactions |
- Take without regard to meals. Food does not decrease the extent of absorption, but it decreases the Cmax by slowing the rate of absorption.
|
| Pathways |
Not Available
|
| General References |
- Fox Z, Dragsted UB, Gerstoft J, Phillips AN, Kjaer J, Mathiesen L, Youle M, Katlama C, Hill A, Bruun JN, Clumeck N, Dellamonica P, Lundgren JD: A randomized trial to evaluate continuation versus discontinuation of lamivudine in individuals failing a lamivudine-containing regimen: the COLATE trial. Antivir Ther. 2006;11(6):761-70. [PubMed
]
- Drugs.com

- Wikipedia

- RxList

- PDRhealth

|
| Organisms Affected |
- Hepatitis B virus
- Human Immunodeficiency Virus
|
| Targets |
- P protein [Includes: DNA-directed DNA polymerase
- Gag-Pol polyprotein
- DNA
|
|
Drug Target 1
[top]
|
| Target 1 ID |
612 |
| Target 1 Name |
P protein [Includes: DNA-directed DNA polymerase |
| Target 1 Synonyms |
- EC 3.1.26.4]
- RNA- directed DNA polymerase
- Ribonuclease H
|
| Target 1 Gene Name |
P |
| Target 1 Protein Sequence |
>P protein [Includes: DNA-directed DNA polymerase
MPLSYPHFRKLLLLDDEAGPLEEELPRLADEDLNRRVAADLNLQLPNVSIPWTHKVGNFT
GLYSSTVPAFNPNWSTPSFPDIHLHQDLISKCEQFVGPLTKNELRRLKLVMPARFYPKVT
KYFPMDKGIKPYYPEHAVNHYFKTRHYLHTLWKAGILYKRESTRSASFCGSPYSWEQELQ
HGSTSLNDTKRHGTESLCAQSSGILSRPSAGSAIQSKFQQSRLGLQHKQGQLANGKQGRS
GRLRSRVHTPTRWPAGVEPSSTRCVNNLASRSASCFHQSAVREKANPSLSTSKRHTSTGN
AVELNPVPPSSVGSQGKGSVLPCWWLQFRDTEPCSDYCLSHIINLLEDWGPCYEHGQHYI
RTPRTPARVTGGVFLVDKNPHNTTESRLVVDFSQFSRGTTRVSWPKFAVPNLQSLTNLLS
SNLSWLSLDVSAAFYHLPLHPAAMPHLLVGSSGLSRYVARLSSTSRIHDHQHGTLQNLHN
SCTRNLYVSLLLLFQTLGRKLHLYSHPIILGFRKIPMGVGLSPFLLAQFTSAICSVVRRA
FPHCLAFSYMDDLVLGAKSVQHLESLYTAVTNFLLSVGIHLNTSKTKRWGYSLHFMGYVI
GSWGSLPQDHIVHKIKECFRKLPVNRPIDWKVCQRIVGLLGFAAPFTQCGYPALMPLYAC
ITAKQAFVFSPTYKAFLCKQYMNLYPVARQRPGLCQVFADATPTGWGLAIGHQRMRGTFV
APLPIHTAELLAACFARSRSGATLIGTDNSVVLSRKYTSFPWLLGCAANWILRGTSFVYV
PSALNPADDPSRGRLGLYRPLLRLPFQPTTGRTSLYADSPSVPSHLPDRVHFASPLHVAW
RPP
|
| Target 1 Number of Residues |
857 |
| Target 1 Molecular Weight |
94259 |
| Target 1 Theoretical pI |
10.12 |
| Target 1 GO Classification |
|
Function
|
RNA-directed DNA polymerase activity
RNA binding
transferase activity
transferase activity, transferring phosphorus-containing groups
nucleotidyltransferase activity
DNA-directed DNA polymerase activity
binding
nucleic acid binding
DNA binding
catalytic activity
hydrolase activity
hydrolase activity, acting on ester bonds
nuclease activity
endonuclease activity
endoribonuclease activity
endoribonuclease activity, producing 5'-phosphomonoesters
ribonuclease H activity |
|
Process
|
RNA-dependent DNA replication
physiological process
metabolism
cellular metabolism
nucleobase, nucleoside, nucleotide and nucleic acid metabolism
DNA metabolism
DNA replication |
|
Component
|
| Not Available |
|
| Target 1 General Function |
Involved in RNA binding |
| Target 1 Specific Function |
Not Available |
| Target 1 Pathways |
|
| Target 1 Reactions |
- deoxynucleoside triphosphate + DNAn = diphosphate + DNAn+1
|
| Target 1 Pfam Domain Function |
|
| Target 1 Signals |
|
| Target 1 Transmembrane Regions |
|
| Target 1 Essentiality |
Essential |
| Target 1 GenBank ID Protein |
59427  |
| Target 1 UniProtKB/Swiss-Prot ID |
Q05486  |
| Target 1 UniProtKB/Swiss-Prot Entry Name |
DPOL_HBVA4  |
| Target 1 PDB ID |
Not Available |
| Target 1 Cellular Location |
|
| Target 1 Gene Sequence |
>2532 bp
ATGCCCCTATCCTATCCACACTTCCGGAAACTACTGTTGTTAGACGACGAGGCAGGTCCC
CTAGAAGAAGAACTCCCTCGCCTCGCAGACGAAGATCTCAATCGCCGCGTCGCCGCAGAT
CTCAATCTCCAGCTTCCCAATGTTAGTATTCCTTGGACTCATAAGGTGGGAAACTTTACG
GGGCTTTACTCTTCTACTGTGCCTGCTTTTAATCCTAACTGGTCCACTCCTTCTTTTCCT
GATATTCATTTGCATCAAGACCTGATTTCTAAATGTGAACAATTTGTAGGCCCACTTACT
AAAAATGAATTACGAAGATTAAAATTGGTTATGCCAGCTAGATTTTATCCTAAGGTTACC
AAATATTTTCCCATGGATAAAGGCATCAAACCCTATTATCCTGAGCATGCAGTTAATCAT
TACTTTAAAACCAGACATTATTTGCATACTTTATGGAAGGCGGGAATTTTATATAAGAGA
GAATCCACACGTAGCGCCTCATTTTGTGGGTCACCATATTCCTGGGAACAAGAGCTACAG
CATGGGAGCACCTCTCTCAACGACACGAAGAGGCATGGGACAGAATCTCTCTGTGCCCAA
TCCTCTGGGATTCTTTCCAGACCATCAGCTGGATCCGCTATTCAGAGCAAATTCCAGCAG
TCCCGACTGGGACTTCAACACAAACAAGGACAGTTGGCCAATGGCAAACAAGGTAGGAGT
GGGAGGCTACGGTCCAGGGTTCACACCCCCACACGGTGGCCTGCTGGGGTGGAGCCCTCA
AGCACAAGGTGTGTTAACAACCTTGCCAGCAGATCCGCCTCCTGCTTCCACCAATCGGCG
GTCCGGGAGAAAGCCAACCCCAGTCTCTCCACCTCTAAGAGACACACATCCACAGGCAAT
GCAGTGGAACTCAACCCAGTTCCACCAAGCTCTGTTGGATCCCAGGGTAAGGGCTCTGTA
CTTCCCTGCTGGTGGCTCCAGTTCAGGGACACAGAACCCTGCTCCGACTATTGCCTCTCT
CACATCATCAATCTTCTCGAAGACTGGGGGCCCTGCTATGAACATGGACAACATTACATC
AGGACTCCTAGGACCCCTGCTCGTGTTACAGGCGGTGTGTTTCTTGTTGACAAAAATCCT
CACAATACCACAGAGTCTAGACTCGTGGTGGACTTCTCTCAATTTTCTAGGGGGACTACC
CGGGTGTCCTGGCCAAAATTCGCAGTCCCCAACCTCCAATCACTTACCAACCTCCTGTCC
TCCAACTTGTCCTGGCTATCGTTGGATGTGTCTGCGGCGTTTTATCATCTTCCTCTTCAT
CCTGCTGCTATGCCTCATCTTCTTGTTGGTTCTTCTGGACTATCAAGGTATGTTGCCCGT
TTGTCCTCTACTTCCAGGATCCACGACCACCAGCACGGGACCCTGCAAAACCTGCACAAC
TCTTGCACAAGGAACCTCTATGTTTCCCTCCTGTTGCTGTTCCAAACCCTCGGACGGAAA
CTGCACTTGTATTCCCATCCCATCATCCTGGGCTTTAGGAAAATACCTATGGGAGTGGGC
CTCAGCCCGTTTCTCCTGGCTCAGTTTACTAGTGCAATTTGTTCAGTGGTGCGTCGGGCT
TTCCCCCACTGTTTGGCTTTTAGTTATATGGATGATCTGGTATTGGGGGCCAAATCTGTG
CAGCATCTTGAGTCCCTTTATACCGCTGTTACCAATTTTCTGTTATCTGTGGGTATCCAT
TTAAATACCTCTAAAACAAAAAGATGGGGTTACTCCCTACATTTTATGGGTTATGTCATT
GGTAGTTGGGGATCATTACCCCAAGATCACATTGTACACAAAATCAAGGAATGCTTTCGA
AAACTGCCTGTAAATCGTCCAATTGATTGGAAAGTTTGTCAACGCATAGTGGGTCTTTTG
GGCTTTGCTGCCCCTTTCACCCAATGCGGTTATCCTGCTCTCATGCCTCTGTATGCCTGT
ATTACTGCTAAACAGGCTTTTGTCTTCTCGCCAACCTACAAGGCCTTTCTGTGTAAACAA
TACATGAACCTTTACCCGGTTGCTCGGCAACGGCCAGGCCTGTGCCAAGTGTTTGCTGAC
GCAACCCCCACTGGTTGGGGCTTGGCCATTGGCCATCAGCGCATGCGTGGAACCTTTGTG
GCTCCTCTGCCGATCCATACTGCGGAACTCCTAGCAGCTTGTTTCGCTCGCAGCAGGTCT
GGAGCGACTCTCATCGGCACGGACAATTCTGTTGTCCTCTCTAGGAAGTACACCTCCTTT
CCATGGCTGCTCGGATGTGCTGCAAACTGGATCCTGCGCGGGACGTCCTTTGTTTACGTC
CCATCGGCGCTGAATCCCGCGGACGACCCCTCCCGGGGCCGCTTGGGGCTGTACCGCCCT
CTTCTCCGTCTGCCGTTCCAGCCGACGACGGGTCGCACCTCTCTTTACGCGGACTCCCCG
TCTGTTCCTTCTCATCTGCCGGACCGTGTGCACTTCGCTTCACCTCTGCACGTCGCATGG
AGACCACCGTGA
|
| Target 1 GenBank Gene ID |
|
| Target 1 GeneCard ID |
Not Available |
| Target 1 GenAtlas ID |
Not Available |
| Target 1 HGNC ID |
Not Available |
| Target 1 Chromosome Location |
Not Available |
| Target 1 Locus |
Not Available |
| Target 1 SNPs |
SNPJam Report  |
| Target 1 General References |
- Naumann H, Schaefer S, Yoshida CF, Gaspar AM, Repp R, Gerlich WH: Identification of a new hepatitis B virus (HBV) genotype from Brazil that expresses HBV surface antigen subtype adw4. J Gen Virol. 1993 Aug;74 ( Pt 8):1627-32. [PubMed
]
|
| Target 1 Drug References |
- Stuyver LJ, Locarnini SA, Lok A, Richman DD, Carman WF, Dienstag JL, Schinazi RF: Nomenclature for antiviral-resistant human hepatitis B virus mutations in the polymerase region. Hepatology. 2001 Mar;33(3):751-7. [PubMed
]
- 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
]
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed
]
|
|
Drug Target 2
[top]
|
| Target 2 ID |
864 |
| Target 2 Name |
Gag-Pol polyprotein |
| Target 2 Synonyms |
- Pr160Gag-Pol
|
| Target 2 Gene Name |
gag |
| Target 2 Protein Sequence |
>Gag-Pol polyprotein
GARASVLSGGELDKWEKIRLRPGGKKKYKLKHIVWASRELERFAVNPGLLETSEGCRQIL
GQLQPSLQTGSEELRSLYNTVATLYCVHQRIDVKDTKEALEKIEEEQNKSKKKAQQAAAA
AGTGNSSQVSQNYPIVQNLQGQMVHQAISPRTLNAWVKVVEEKAFSPEVIPMFSALSEGA
TPQDLNTMLNTVGGHQAAMQMLKETINEEAAEWDRVHPVHAGPIAPGQMREPRGSDIAGT
TSTLQEQIGWMTNNPPIPVGEIYKRWIILGLNKIVRMYSPTSILDIRQGPKEPFRDYVDR
FYKTLRAEQASQDVKNWMTETLLVQNANPDCKTILKALGPAATLEEMMTACQGVGGPGHK
ARVLAEAMSQVTNPANIMMQRGNFRNQRKTVKCFNCGKEGHIAKNCRAPRKKGCWRCGRE
GHQMKDCTERQANFLREDLAFLQGKAREFSSEQTRANSPTRRELQVWGGENNSLSEAGAD
RQGTVSFNFPQITLWQRPLVTIRIGGQLKEALLDTGADDTVLEEMNLPGKWKPKMIGGIG
GFIKVRQYDQIPVEICGHKAIGTVLVGPTPVNIIGRNLLTQIGCTLNFPISPIETVPVKL
KPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPVFAIKKKDSTKWR
KLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPLDKDFRKYTAFTI
PSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFRKQNPDIVIYQYMDDLYVGSD
LEIGQHRTKIEELRQHLLRWGFTTPDKKHQKEPPFLWMGYELHPDKWTVQPIMLPEKDSW
TVNDIQKLVGKLNWASQIYAGIKVKQLCKLLRGTKALTEVIPLTEEAELELAENREILKE
PVHEVYYDPSKDLVAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGAHTNDVKQLTEAV
QKVSTESIVIWGKIPKFKLPIQKETWEAWWMEYWQATWIPEWEFVNTPPLVKLWYQLEKE
PIVGAETFYVDGAANRETKLGKAGYVTDRGRQKVVSIADTTNQKTELQAIHLALQDSGLE
VNIVTDSQYALGIIQAQPDKSESELVSQIIEQLIKKEKVYLAWVPAHKGIGGNEQVDKLV
SAGIRKVLFLNGIDKAQEEHEKYHSNWRAMASDFNLPPVVAKEIVASCDKCQLKGEAMHG
QVDCSPGIWQLDCTHLEGKIILVAVHVASGYIEAEVIPAETGQETAYFLLKLAGRWPVKT
IHTDNGSNFTSTTVKAACWWAGIKQEFGIPYNPQSQGVVESMNNELKKIIGQVRDQAEHL
KTAVQMAVFIHNFKRKGGIGGYSAGERIVDIIATDIQTKELQKQITKIQNFRVYYRDNKD
PLWKGPAKLLWKGEGAVVIQDNSDIKVVPRRKAKIIRDYGKQMAGDDCVASRQDED
|
| Target 2 Number of Residues |
1459 |
| Target 2 Molecular Weight |
161886 |
| Target 2 Theoretical pI |
9.02 |
| Target 2 GO Classification |
|
Function
|
RNA binding
transferase activity
transferase activity, transferring phosphorus-containing groups
nucleotidyltransferase activity
RNA-directed DNA polymerase activity
DNA binding
hydrolase activity, acting on ester bonds
nuclease activity
endonuclease activity
endoribonuclease activity
endoribonuclease activity, producing 5'-phosphomonoesters
ribonuclease H activity
nucleic acid binding
hydrolase activity
peptidase activity
endopeptidase activity
aspartic-type endopeptidase activity
structural molecule activity
binding
ion binding
cation binding
transition metal ion binding
zinc ion binding
catalytic activity
integrase activity |
|
Process
|
DNA replication
RNA-dependent DNA replication
DNA recombination
macromolecule metabolism
protein metabolism
cellular protein metabolism
proteolysis
physiological process
metabolism
cellular metabolism
nucleobase, nucleoside, nucleotide and nucleic acid metabolism
DNA metabolism
DNA integration
viral life cycle |
|
Component
|
| Not Available |
|
| Target 2 General Function |
Involved in RNA binding |
| Target 2 Specific Function |
Integrase performs the integration of the newly synthesized dsDNA copy of the viral genome into the host chromosome. The integrated DNA is called provirus |
| Target 2 Pathways |
|
| Target 2 Reactions |
- deoxynucleoside triphosphate + DNAn = diphosphate + DNAn+1
|
| Target 2 Pfam Domain Function |
|
| Target 2 Signals |
|
| Target 2 Transmembrane Regions |
|
| Target 2 Essentiality |
Non-Essential |
| Target 2 GenBank ID Protein |
328661  |
| Target 2 UniProtKB/Swiss-Prot ID |
P03369  |
| Target 2 UniProtKB/Swiss-Prot Entry Name |
POL_HV1A2  |
| Target 2 PDB ID |
1VRU  |
| Target 2 PDB File |
Show |
| Target 2 3D Structure |
|
| Target 2 Cellular Location |
- Nucleus. Cytoplasm (By similarity). Following virus entry, the nuclear localization signal (NLS) of
|
| Target 2 Gene Sequence |
>3012 bp
TTTTTTAGGGAAGATCTGGCCTTCCTACAAGGGAAGGCCAGGGAATTTTCTTCAGAGCAG
ACCAGAGCCAACAGCCCCACCAGAAGAGAGCTTCAGGTTTGGGGAGGAGAAAACAACTCC
CTCTCAGAAGCAGGAGCCGATAGACAAGGAACTGTATCCTTTAACTTCCCTCAGATCACT
CTTTGGCAACGACCCCTCGTCACAATAAGGATAGGGGGGCAACTAAAGGAAGCTCTATTA
GATACAGGAGCAGATGATACAGTATTAGAAGAAATGAATTTGCCAGGAAAATGGAAACCA
AAAATGATAGGGGGAATTGGAGGTTTTATCAAAGTAAGACAGTACGATCAGATACCTGTA
GAAATCTGTGGACATAAAGCTATAGGTACAGTATTAGTAGGACCTACACCTGTCAACATA
ATTGGAAGAAATCTGTTGACTCAGATTGGTTGTACTTTAAATTTCCCCATTAGTCCTATT
GAAACTGTACCAGTAAAATTAAAGCCAGGAATGGATGGCCCAAAAGTTAAGCAATGGCCA
TTGACAGAAGAAAAAATAAAAGCATTAGTAGAGATATGTACAGAAATGGAAAAGGAAGGG
AAAATTTCAAAAATTGGGCCTGAAAATCCATACAATACTCCAGTATTTGCTATAAAGAAA
AAAGACAGTACTAAATGGAGAAAACTAGTAGATTTCAGAGAACTTAATAAAAGAACTCAA
GACTTCTGGGAAGTTCAGTTAGGAATACCACACCCCGCAGGGTTAAAAAAGAAAAAATCA
GTAACAGTATTGGATGTGGGTGATGCATACTTTTCAGTTCCCTTAGATAAAGACTTTAGA
AAGTATACTGCATTTACCATACCTAGTATAAACAATGAGACACCAGGGATTAGATATCAG
TACAATGTGCTGCCACAGGGATGGAAAGGATCACCAGCAATATTCCAAAGTAGCATGACA
AAAATCTTAGAGCCTTTTAGAAAACAGAATCCAGACATAGTTATCTATCAATACATGGAT
GATTTGTATGTAGGATCTGACTTAGAAATAGGGCAGCATAGAACAAAAATAGAGGAACTG
AGACAGCATCTGTTGAGGTGGGGATTTACCACACCAGACAAAAAACATCAGAAAGAACCT
CCATTCCTTTGGATGGGTTATGAACTCCATCCTGATAAATGGACAGTACAGCCTATAATG
CTGCCAGAAAAAGACAGCTGGACTGTCAATGACATACAGAAGTTAGTGGGAAAATTGAAT
TGGGCAAGTCAGATTTATGCAGGGATTAAAGTAAAGCAGTTATGTAAACTCCTTAGAGGA
ACCAAAGCACTAACAGAAGTAATACCACTAACAGAAGAAGCAGAGCTAGAACTGGCAGAA
AACAGGGAGATTCTAAAAGAACCAGTACATGAAGTATATTATGACCCATCAAAAGACTTA
GTAGCAGAAATACAGAAGCAGGGGCAAGGCCAATGGACATATCAAATTTATCAAGAGCCA
TTTAAAAATCTGAAAACAGGAAAGTATGCAAGGATGAGGGGTGCCCACACTAATGATGTA
AAACAGTTAACAGAGGCAGTGCAAAAAGTATCCACAGAAAGCATAGTAATATGGGGAAAG
ATTCCTAAATTTAAACTACCCATACAAAAGGAAACATGGGAAGCATGGTGGATGGAGTAT
TGGCAAGCTACCTGGATTCCTGAGTGGGAGTTTGTCAATACCCCTCCCTTAGTGAAATTA
TGGTACCAGTTAGAGAAAGAACCCATAGTAGGAGCAGAAACTTTCTATGTAGATGGGGCA
GCTAATAGGGAGACTAAATTAGGAAAAGCAGGATATGTTACTGACAGAGGAAGACAAAAA
GTTGTCTCCATAGCTGACACAACAAATCAGAAGACTGAATTACAAGCAATTCATCTAGCT
TTGCAGGATTCGGGATTAGAAGTAAACATAGTAACAGACTCACAATATGCATTAGGAATC
ATTCAAGCACAACCAGATAAGAGTGAATCAGAGTTAGTCAGTCAAATAATAGAGCAGTTA
ATAAAAAAGGAAAAGGTCTACCTGGCATGGGTACCAGCACACAAAGGAATTGGAGGAAAT
GAACAAGTAGATAAATTAGTCAGTGCTGGAATCAGGAAAGTACTATTTTTGAATGGAATA
GATAAGGCCCAAGAAGAACATGAGAAATATCACAGTAATTGGAGAGCAATGGCTAGTGAT
TTTAACCTGCCACCTGTAGTAGCAAAAGAAATAGTAGCCAGCTGTGATAAATGTCAGCTA
AAAGGAGAAGCCATGCATGGACAAGTAGACTGTAGTCCAGGAATATGGCAACTAGATTGT
ACACATCTAGAAGGAAAAATTATCCTGGTAGCAGTTCATGTAGCCAGTGGATATATAGAA
GCAGAAGTTATTCCAGCAGAGACAGGGCAGGAAACAGCATATTTTCTCTTAAAATTAGCA
GGAAGATGGCCAGTAAAAACAATACATACAGACAATGGCAGCAATTTCACCAGTACTACG
GTTAAGGCCGCCTGTTGGTGGGCAGGGATCAAGCAGGAATTTGGCATTCCCTACAATCCC
CAAAGTCAAGGAGTAGTAGAATCTATGAATAATGAATTAAAGAAAATTATAGGACAGGTA
AGAGATCAGGCTGAACACCTTAAGACAGCAGTACAAATGGCAGTATTCATCCACAATTTT
AAAAGAAAAGGGGGGATTGGGGGATACAGTGCAGGGGAAAGAATAGTAGACATAATAGCA
ACAGACATACAAACTAAAGAACTACAAAAGCAAATTACAAAAATTCAAAATTTTCGGGTT
TATTACAGGGACAACAAAGATCCCCTTTGGAAAGGACCAGCAAAGCTTCTCTGGAAAGGT
GAAGGGGCAGTAGTAATACAAGATAATAGTGACATAAAAGTAGTGCCAAGAAGAAAAGCA
AAAATCATTAGGGATTATGGAAAACAGATGGCAGGTGATGATTGTGTGGCAAGTAGACAG
GATGAGGATTAG
|
| Target 2 GenBank Gene ID |
|
| Target 2 GeneCard ID |
Not Available |
| Target 2 GenAtlas ID |
Not Available |
| Target 2 HGNC ID |
Not Available |
| Target 2 Chromosome Location |
Not Available |
| Target 2 Locus |
Not Available |
| Target 2 SNPs |
SNPJam Report  |
| Target 2 General References |
- Tyndall JD, Reid RC, Tyssen DP, Jardine DK, Todd B, Passmore M, March DR, Pattenden LK, Bergman DA, Alewood D, Hu SH, Alewood PF, Birch CJ, Martin JL, Fairlie DP: Synthesis, stability, antiviral activity, and protease-bound structures of substrate-mimicking constrained macrocyclic inhibitors of HIV-1 protease. J Med Chem. 2000 Sep 21;43(19):3495-504. [PubMed
]
- Prabu-Jeyabalan M, Nalivaika E, Schiffer CA: Substrate shape determines specificity of recognition for HIV-1 protease: analysis of crystal structures of six substrate complexes. Structure. 2002 Mar;10(3):369-81. [PubMed
]
- Jacks T, Power MD, Masiarz FR, Luciw PA, Barr PJ, Varmus HE: Characterization of ribosomal frameshifting in HIV-1 gag-pol expression. Nature. 1988 Jan 21;331(6153):280-3. [PubMed
]
- Wlodawer A, Miller M, Jaskolski M, Sathyanarayana BK, Baldwin E, Weber IT, Selk LM, Clawson L, Schneider J, Kent SB: Conserved folding in retroviral proteases: crystal structure of a synthetic HIV-1 protease. Science. 1989 Aug 11;245(4918):616-21. [PubMed
]
- Sanchez-Pescador R, Power MD, Barr PJ, Steimer KS, Stempien MM, Brown-Shimer SL, Gee WW, Renard A, Randolph A, Levy JA, et al.: Nucleotide sequence and expression of an AIDS-associated retrovirus (ARV-2). Science. 1985 Feb 1;227(4686):484-92. [PubMed
]
- Rose RB, Craik CS, Douglas NL, Stroud RM: Three-dimensional structures of HIV-1 and SIV protease product complexes. Biochemistry. 1996 Oct 1;35(39):12933-44. [PubMed
]
- Rutenber EE, McPhee F, Kaplan AP, Gallion SL, Hogan JC Jr, Craik CS, Stroud RM: A new class of HIV-1 protease inhibitor: the crystallographic structure, inhibition and chemical synthesis of an aminimide peptide isostere. Bioorg Med Chem. 1996 Sep;4(9):1545-58. [PubMed
]
- Turner BG, Summers MF: Structural biology of HIV. J Mol Biol. 1999 Jan 8;285(1):1-32. [PubMed
]
|
| Target 2 Drug References |
- 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
]
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed
]
|
|
Drug Target 3
[top]
|
| Target 3 ID |
874 |
| Target 3 Name |
DNA |
| Target 3 Synonyms |
- Deoxyribonucleic acid
|
| Target 3 Gene Name |
Not Available |
| Target 3 Protein Sequence |
Not Available |
| Target 3 Number of Residues |
0 |
| Target 3 Molecular Weight |
7656 (double strand) |
| Target 3 Theoretical pI |
Not Available |
| Target 3 GO Classification |
|
Function
|
information storage
information transfer
|
|
Process
|
DNA replication and chromosomal cycle
DNA replication
DNA-dependent DNA replication
DNA replication, synthesis of RNA primer
transcription
transcription, DNA dependent
|
|
Component
|
cell
intracellular
nucleus
mitochondria |
|
| Target 3 General Function |
Biological information storage and information transfer |
| Target 3 Specific Function |
DNA is the molecule of heredity, as it is responsible for the genetic propagation of most inherited traits. It is a polynucleic acid that carries genetic information on cell growth, division, and function. DNA consists of two long strands of nucleotides twisted into a double helix and held together by hydrogen bonds. The sequence of nucleotides determines hereditary characteristics. Each strand serves as the template for subsequent DNA replication and as a template for mRNA production, leading to protein synthesis via ribosomes. |
| Target 3 Pathways |
|
| Target 3 Reactions |
- DNA + DNA polymerase + nNTP = 2 DNA + nNDP; DNA + RNA polymerase + NTP = mRNA + nNDP
|
| Target 3 Pfam Domain Function |
Not Available |
| Target 3 Signals |
|
| Target 3 Transmembrane Regions |
|
| Target 3 Essentiality |
Essential |
| Target 3 GenBank ID Protein |
Not Available |
| Target 3 UniProtKB/Swiss-Prot ID |
Not Available |
| Target 3 UniProtKB/Swiss-Prot Entry Name |
Not Available |
| Target 3 PDB ID |
1BNA  |
| Target 3 PDB File |
Show |
| Target 3 3D Structure |
|
| Target 3 Cellular Location |
|
| Target 3 Gene Sequence |
>Example: Dickerson dodecamer
CGCGAATTCGCG
|
| Target 3 GenBank Gene ID |
|
| Target 3 GeneCard ID |
Not Available |
| Target 3 GenAtlas ID |
Not Available |
| Target 3 HGNC ID |
Not Available |
| Target 3 Chromosome Location |
Not Available |
| Target 3 Locus |
All loci |
| Target 3 SNPs |
Not Available |
| Target 3 General References |
- Nadeau D, Marchand C: Change in the kinetics of sulphacetamide tissue distribution in Walker tumor-bearing rats. Drug Metab Dispos. 1975 Nov-Dec;3(6):565-76. [PubMed
]
|
| Target 3 Drug References |
- 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
]
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed
]
- Dai CY, Yu ML, Hsieh MY, Lee LP, Hou NJ, Huang JF, Chen SC, Lin ZY, Hsieh MY, Wang LY, Tsai JF, Chang WY, Chuang WL: Early response to lamivudine therapy in clinically non-cirrhotic chronic hepatitis B patients with decompensation. Liver Int. 2007 Sep 27;. [PubMed
]
- Ma H, Guo F, Wei L, Sun Y, Wang H: [The prospective study of the clinical features and outcome of HBeAg-negative and HBeAg-positive cirrhosis in patients with chronic type B hepatitis] Zhonghua Yi Xue Za Zhi. 2007 Jul 10;87(26):1832-5. [PubMed
]
- Pan XP, Li LJ, Du WB, Li MW, Cao HC, Sheng JF: Differences of YMDD mutational patterns, precore/core promoter mutations, serum HBV DNA levels in lamivudine-resistant hepatitis B genotypes B and C. J Viral Hepat. 2007 Nov;14(11):767-74. [PubMed
]
|