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Showing drug card for Temsirolimus (DB06287)

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Version 2.5
Creation Date 2008-03-19 16:22:10
Update Date 2009-02-19 16:03:54
Primary Accession Number DB06287
Secondary Accession Number Not Available
Name Temsirolimus
Drug Type
  • Approved
  • Investigational
  • Small Molecule
Description Temsirolimus is an intravenous drug for the treatment of renal cell carcinoma (RCC), developed by Wyeth Pharmaceuticals and approved by the FDA in late May 2007, and was also approved by the European Medicines Agency (EMEA) on November 2007. It is a derivative of sirolimus and is sold as Torisel.
Synonyms
  1. CCI-779
  2. temsirolimus
Brand Names
  1. Torisel
Brand Mixtures Not Available
Chemical IUPAC Name Not Available
Chemical Formula C56H87NO16
Chemical Structure Structure
CAS Registry Number 162635-04-3
InChI Identifier InChI=1/C56H87NO16/c1-33-17-13-12-14-18-34(2)45(68-9)29-41-22-20-39(7)56(67,73-41)51(63)52(64)57-24-16-15-19-42(57)53(65)71-46(30-43(60)35(3)26-38(6)49(62)50(70-11)48(61)37(5)25-33)36(4)27-40-21-23-44(47(28-40)69-10)72-54(66)55(8,31-58)32-59/h12-14,17-18,26,33,35-37,39-42,44-47,49-50,58-59,62,67H,15-16,19-25,27-32H2,1-11H3/b14-12+,17-13+,34-18+,38-26+/t33-,35-,36-,37-,39-,40+,41+,42+,44-,45+,46+,47-,49-,50+,56-/m1/s1
InChI Key CBPNZQVSJQDFBE-FUXHJELOBE
KEGG Drug D06068 Link Image
KEGG Compound C15182 Link Image
PubChem Compound 6918289 Link Image
PubChem Substance Not Available
ChEBI ID Not Available
PharmGKB ID Not Available
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] Not Available
RxList Link http://www.rxlist.com/cgi/generic/torisel.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Temsirolimus Link Image
FDA Label
Material Safety Data Sheet (MSDS) Not Available
Synthesis Reference Not Available
Average Molecular Weight 1030.2871
Monoisotopic Molecular Weight 1029.6025
State Solid
Melting Point Not Available
Experimental Water Solubility Not Available Source: PhysProp
Predicted Water Solubility 2.35e-03 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity Not Available Source: PhysProp
Predicted LogP 4.39 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -5.64 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 CO[C@@H]1C[C@@H](CC[C@H]1OC(=O)C(C)(CO)CO)C[C@@H](C)[C@@H]1CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)\[C@H](C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1)OC
Canonical SMILES COC1CC(CCC1OC(=O)C(C)(CO)CO)CC(C)C1CC(=O)C(C)C=C(C)C(O)C(OC)C(=O)C(C)CC(C)C=CC=CC=C(C)C(CC2CCC(C)C(O)(O2)C(=O)C(=O)N2CCCCC2C(=O)O1)OC
Drug Category
  • Antineoplastic Agents
  • Protein Kinase Inhibitors
ATC Codes Not Available
AHFS Codes Not Available
Indication For the treatment of renal cell carcinoma (RCC). Also investigated for use/treatment in breast cancer, lymphoma (unspecified), rheumatoid arthritis, and multiple myeloma.
Pharmacology Not Available
Mechanism of Action Temsirolimus is an inhibitor of mTOR (mammalian target of rapamycin). Temsirolimus binds to an intracellular protein (FKBP-12), and the protein-drug complex inhibits the activity of mTOR that controls cell division. Inhibition of mTOR activity resulted in a G1 growth arrest in treated tumor cells. When mTOR was inhibited, its ability to phosphorylate p70S6k and S6 ribosomal protein, which are downstream of mTOR in the PI3 kinase/AKT pathway was blocked. In in vitro studies using renal cell carcinoma cell lines, temsirolimus inhibited the activity of mTOR and resulted in reduced levels of the hypoxia-inducible factors HIF-1 and HIF-2 alpha, and the vascular endothelial growth factor.
Absorption Not Available
Toxicity Temsirolimus has been administered to patients with cancer in phase 1 and 2 trials with repeated intravenous doses as high as 220 mg/m2. The risk of several serious adverse events, including thrombosis, bowel perforation, interstitial lung disease (ILD), seizure, and psychosis, is increased with doses of temsirolimus greater than 25 mg.
Protein Binding Not Available
Biotransformation Hepatic, primarily cytochrome P450 (CYP) 3A4/5.
Half Life Temsirolimus exhibits a bi-exponential decline in whole blood concentrations and the mean half-lives of temsirolimus and sirolimus were 17.3 hr and 54.6 hr, respectively.
Dosage Forms
Form Route
Solution Intravenous
Patient Information Not Available
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions
Drug Interaction
Aminoglutethimide Aminoglutethimide may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Amprenavir Amprenavir may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Atazanavir Atazanavir may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Bosentan Bosentan may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Carbamazepine Carbamazepine may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Clarithromycin Clarithromycin may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Conivaptan Conivaptan may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Darunavir Darunavir may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Delavirdine Delavirdine may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Dexamethasone Dexamethasone may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Efavirenz Efavirenz may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Fluorouracil Co-administration of Temsirolimus and Fluorouracil may result in serious adverse drug reactions.
Fosamprenavir Fosamprenavir may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Fosphenytoin Fosphenytoin may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Gemcitabine Co-administration of Temsirolimus and Gemcitabine may result in serious adverse drug reactions.
Imatinib Imatinib may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Indinavir Indinavir may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Isoniazid Isoniazid may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Itraconazole Itraconazole may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Ketoconazole Ketoconazole may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Lopinavir Lopinavir may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Miconazole Miconazole may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Nafcillin Nafcillin may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Natalizumab Temsirolimus may increase the toxicity of Natalizumab. Concomitant therapy should be avoided.
Nefazodone Nefazodone may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Nelfinavir Nelfinavir may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Nevirapine Nevirapine may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Nicardipine Nicardipine may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Oxcarbazepine Oxcarbamazepine may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Pentobarbital Pentobarbital may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Phenobarbital Phenobarbital may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Phenytoin Phenytoin may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Posaconazole Posaconazole may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Primidone Primidone may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Quinidine Quinidine may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Rifabutin Rifabutin may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Rifampin Rifampin may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Rifapentine Rifapentine may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Ritonavir Ritonavir may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Saquinavir Saquinavir may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
St. John's Wort St. John's Wort may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Sunitinib Co-administration of Temsirolimus and Sunitinib may result in serious adverse drug reactions.
Telithromycin Telithromycin may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Voriconazole Voriconzole may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Food Interactions Not Available
Pathways Not Available
General References
  1. Boni J, Leister C, Burns J, Cincotta M, Hug B, Moore L: Pharmacokinetic profile of temsirolimus with concomitant administration of cytochrome p450-inducing medications. J Clin Pharmacol. 2007 Nov;47(11):1430-9. Epub 2007 Oct 3. [PubMed Link Image]
  2. Wikipedia Link Image
  3. RxList Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. Cytochrome P450 3A5 (CYP3A5)
  2. Cytochrome P450 3A4 (CYP3A4)
Targets
  1. FKBP12-rapamycin complex-associated protein
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 3A5 (CYP3A5)
Enzyme 1 Gene Name CYP3A5
Enzyme 1 SwissProt ID P20815 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P20815|CP3A5_HUMAN Cytochrome P450 3A5 
MDLIPNLAVETWLLLAVSLVLLYLYGTRTHGLFKRLGIPGPTPLPLLGNVLSYRQGLWKF
DTECYKKYGKMWGTYEGQLPVLAITDPDVIRTVLVKECYSVFTNRRSLGPVGFMKSAISL
AEDEEWKRIRSLLSPTFTSGKLKEMFPIIAQYGDVLVRNLRREAEKGKPVTLKDIFGAYS
MDVITGTSFGVNIDSLNNPQDPFVESTKKFLKFGFLDPLFLSIILFPFLTPVFEALNVSL
FPKDTINFLSKSVNRMKKSRLNDKQKHRLDFLQLMIDSQNSKETESHKALSDLELAAQSI
IFIFAGYETTSSVLSFTLYELATHPDVQQKLQKEIDAVLPNKAPPTYDAVVQMEYLDMVV
NETLRLFPVAIRLERTCKKDVEINGVFIPKGSMVVIPTYALHHDPKYWTEPEEFRPERFS
KKKDSIDPYIYTPFGTGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLDTQG
LLQPEKPIVLKVDSRDGTLSGE
Phase 1 Metabolizing Enzyme 2 [top]
Enzyme 2 Name Cytochrome P450 3A4 (CYP3A4)
Enzyme 2 Gene Name CYP3A4
Enzyme 2 SwissProt ID P08684 Link Image
Enzyme 2 SNPs SNPJam Report Link Image
Enzyme 2 Protein Sequence >sp|P08684|CP3A4_HUMAN Cytochrome P450 3A4 (EC 1.14.13.67) 
ALIPDLAMETWLLLAVSLVLLYLYGTHSHGLFKKLGIPGPTPLPFLGNILSYHKGFCMFD
MECHKKYGKVWGFYDGQQPVLAITDPDMIKTVLVKECYSVFTNRRPFGPVGFMKSAISIA
EDEEWKRLRSLLSPTFTSGKLKEMVPIIAQYGDVLVRNLRREAETGKPVTLKDVFGAYSM
DVITSTSFGVNIDSLNNPQDPFVENTKKLLRFDFLDPFFLSITVFPFLIPILEVLNICVF
PREVTNFLRKSVKRMKESRLEDTQKHRVDFLQLMIDSQNSKETESHKALSDLELVAQSII
FIFAGYETTSSVLSFIMYELATHPDVQQKLQEEIDAVLPNKAPPTYDTVLQMEYLDMVVN
ETLRLFPIAMRLERVCKKDVEINGMFIPKGWVVMIPSYALHRDPKYWTEPEKFLPERFSK
KNKDNIDPYIYTPFGSGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLSLGG
LLQPEKPVVLKVESRDGTVSGA
Drug Target 1 [top]
Target 1 ID 4148
Target 1 Name FKBP12-rapamycin complex-associated protein
Target 1 Synonyms
  1. FK506-binding protein 12- rapamycin complex-associated protein 1
  2. Mammalian target of rapamycin
  3. RAPT1
  4. Rapamycin target protein
  5. mTOR
Target 1 Gene Name FRAP1
Target 1 Protein Sequence >FKBP12-rapamycin complex-associated protein 
MLGTGPAAATTAATTSSNVSVLQQFASGLKSRNEETRAKAAKELQHYVTMELREMSQEES
TRFYDQLNHHIFELVSSSDANERKGGILAIASLIGVEGGNATRIGRFANYLRNLLPSNDP
VVMEMASKAIGRLAMAGDTFTAEYVEFEVKRALEWLGADRNEGRRHAAVLVLRELAISVP
TFFFQQVQPFFDNIFVAVWDPKQAIREGAVAALRACLILTTQREPKEMQKPQWYRHTFEE
AEKGFDETLAKEKGMNRDDRIHGALLILNELVRISSMEGERLREEMEEITQQQLVHDKYC
KDLMGFGTKPRHITPFTSFQAVQPQQSNALVGLLGYSSHQGLMGFGTSPSPAKSTLVESR
CCRDLMEEKFDQVCQWVLKCRNSKNSLIQMTILNLLPRLAAFRPSAFTDTQYLQDTMNHV
LSCVKKEKERTAAFQALGLLSVAVRSEFKVYLPRVLDIIRAALPPKDFAHKRQKAMQVDA
TVFTCISMLARAMGPGIQQDIKELLEPMLAVGLSPALTAVLYDLSRQIPQLKKDIQDGLL
KMLSLVLMHKPLRHPGMPKGLAHQLASPGLTTLPEASDVGSITLALRTLGSFEFEGHSLT
QFVRHCADHFLNSEHKEIRMEAARTCSRLLTPSIHLISGHAHVVSQTAVQVVADVLSKLL
VVGITDPDPDIRYCVLASLDERFDAHLAQAENLQALFVALNDQVFEIRELAICTVGRLSS
MNPAFVMPFLRKMLIQILTELEHSGIGRIKEQSARMLGHLVSNAPRLIRPYMEPILKALI
LKLKDPDPDPNPGVINNVLATIGELAQVSGLEMRKWVDELFIIIMDMLQDSSLLAKRQVA
LWTLGQLVASTGYVVEPYRKYPTLLEVLLNFLKTEQNQGTRREAIRVLGLLGALDPYKHK
VNIGMIDQSRDASAVSLSESKSSQDSSDYSTSEMLVNMGNLPLDEFYPAVSMVALMRIFR
DQSLSHHHTMVVQAITFIFKSLGLKCVQFLPQVMPTFLNVIRVCDGAIREFLFQQLGMLV
SFVKSHIRPYMDEIVTLMREFWVMNTSIQSTIILLIEQIVVALGGEFKLYLPQLIPHMLR
VFMHDNSPGRIVSIKLLAAIQLFGANLDDYLHLLLPPIVKLFDAPEAPLPSRKAALETVD
RLTESLDFTDYASRIIHPIVRTLDQSPELRSTAMDTLSSLVFQLGKKYQIFIPMVNKVLV
RHRINHQRYDVLICRIVKGYTLADEEEDPLIYQHRMLRSGQGDALASGPVETGPMKKLHV
STINLQKAWGAARRVSKDDWLEWLRRLSLELLKDSSSPSLRSCWALAQAYNPMARDLFNA
AFVSCWSELNEDQQDELIRSIELALTSQDIAEVTQTLLNLAEFMEHSDKGPLPLRDDNGI
VLLGERAAKCRAYAKALHYKELEFQKGPTPAILESLISINNKLQQPEAAAGVLEYAMKHF
GELEIQATWYEKLHEWEDALVAYDKKMDTNKDDPELMLGRMRCLEALGEWGQLHQQCCEK
WTLVNDETQAKMARMAAAAAWGLGQWDSMEEYTCMIPRDTHDGAFYRAVLALHQDLFSLA
QQCIDKARDLLDAELTAMAGESYSRAYGAMVSCHMLSELEEVIQYKLVPERREIIRQIWW
ERLQGCQRIVEDWQKILMVRSLVVSPHEDMRTWLKYASLCGKSGRLALAHKTLVLLLGVD
PSRQLDHPLPTVHPQVTYAYMKNMWKSARKIDAFQHMQHFVQTMQQQAQHAIATEDQQHK
QELHKLMARCFLKLGEWQLNLQGINESTIPKVLQYYSAATEHDRSWYKAWHAWAVMNFEA
VLHYKHQNQARDEKKKLRHASGANITNATTAATTAATATTTASTEGSNSESEAESTENSP
TPSPLQKKVTEDLSKTLLMYTVPAVQGFFRSISLSRGNNLQDTLRVLTLWFDYGHWPDVN
EALVEGVKAIQIDTWLQVIPQLIARIDTPRPLVGRLIHQLLTDIGRYHPQALIYPLTVAS
KSTTTARHNAANKILKNMCEHSNTLVQQAMMVSEELIRVAILWHEMWHEGLEEASRLYFG
ERNVKGMFEVLEPLHAMMERGPQTLKETSFNQAYGRDLMEAQEWCRKYMKSGNVKDLTQA
WDLYYHVFRRISKQLPQLTSLELQYVSPKLLMCRDLELAVPGTYDPNQPIIRIQSIAPSL
QVITSKQRPRKLTLMGSNGHEFVFLLKGHEDLRQDERVMQLFGLVNTLLANDPTSLRKNL
SIQRYAVIPLSTNSGLIGWVPHCDTLHALIRDYREKKKILLNIEHRIMLRMAPDYDHLTL
MQKVEVFEHAVNNTAGDDLAKLLWLKSPSSEVWFDRRTNYTRSLAVMSMVGYILGLGDRH
PSNLMLDRLSGKILHIDFGDCFEVAMTREKFPEKIPFRLTRMLTNAMEVTGLDGNYRITC
HTVMEVLREHKDSVMAVLEAFVYDPLLNWRLMDTNTKGNKRSRTRTDSYSAGQSVEILDG
VELGEPAHKKTGTTVPESIHSFIGDGLVKPEALNKKAIQIINRVRDKLTGRDFSHDDTLD
VPTQVELLIKQATSHENLCQCYIGWCPFW
Target 1 Number of Residues 2591
Target 1 Molecular Weight 288896
Target 1 Theoretical pI 7.17
Target 1 GO Classification
Function
catalytic activity
transferase activity
transferase activity, transferring phosphorus-containing groups
phosphotransferase activity, alcohol group as acceptor
binding
Process
Not Available
Component
Not Available
Target 1 General Function Involved in binding
Target 1 Specific Function Acts as the target for the cell-cycle arrest and immunosuppressive effects of the FKBP12-rapamycin complex
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • None
Target 1 Essentiality Non Essential
Target 1 GenBank ID Protein Not Available
Target 1 UniProtKB/Swiss-Prot ID P42345 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name FRAP_HUMAN Link Image
Target 1 PDB ID 1AUE Link Image
Target 1 PDB File Show
Target 1 3D Structure
Target 1 Cellular Location Not Available
Target 1 Gene Sequence >7650 bp 
ATGCTTGGAACCGGACCTGCCGCCGCCACCACCGCTGCCACCACATCTAGCAATGTGAGC
GTCCTGCAGCAGTTTGCCAGTGGCCTAAAGAGCCGGAATGAGGAAACCAGGGCCAAAGCC
GCCAAGGAGCTCCAGCACTATGTCACCATGGAACTCCGAGAGATGAGTCAAGAGGAGTCT
ACTCGCTTCTATGACCAACTGAACCATCACATTTTTGAATTGGTTTCCAGCTCAGATGCC
AATGAGAGGAAAGGTGGCATCTTGGCCATAGCTAGCCTCATAGGAGTGGAAGGTGGGAAT
GCCACCCGAATTGGCAGATTTGCCAACTATCTTCGGAACCTCCTCCCCTCCAATGACCCA
GTTGTCATGGAAATGGCATCCAAGGCCATTGGCCGTCTTGCCATGGCAGGGGACACTTTT
ACCGCTGAGTACGTGGAATTTGAGGTGAAGCGAGCCCTGGAATGGCTGGGTGCTGACCGC
AATGAGGGCCGGAGACATGCAGCTGTCCTGGTTCTCCGTGAGCTGGCCATCAGCGTCCCT
ACCTTCTTCTTCCAGCAAGTGCAACCCTTCTTTGACAACATTTTTGTGGCCGTGTGGGAC
CCCAAACAGGCCATCCGTGAGGGAGCTGTAGCCGCCCTTCGTGCCTGTCTGATTCTCACA
ACCCAGCGTGAGCCGAAGGAGATGCAGAAGCCTCAGTGGTACAGGCACACATTTGAAGAA
GCAGAGAAGGGATTTGATGAGACCTTGGCCAAAGAGAAGGGCATGAATCGGGATGATCGG
ATCCATGGAGCCTTGTTGATCCTTAACGAGCTGGTCCGAATCAGCAGCATGGAGGGAGAG
CGTCTGAGAGAAGAAATGGAAGAAATCACACAGCAGCAGCTGGTACACGACAAGTACTGC
AAAGATCTCATGGGCTTCGGAACAAAACCTCGTCACATTACCCCCTTCACCAGTTTCCAG
GCTGTACAGCCCCAGCAGTCAAATGCCTTGGTGGGGCTGCTGGGGTACAGCTCTCACCAA
GGCCTCATGGGATTTGGGACCTCCCCCAGTCCAGCTAAGTCCACCCTGGTGGAGAGCCGG
TGTTGCAGAGACTTGATGGAGGAGAAATTTGATCAGGTGTGCCAGTGGGTGCTGAAATGC
AGGAATAGCAAGAACTCGCTGATCCAAATGACAATCCTTAATTTGTTGCCCCGCTTGGCT
GCATTCCGACCTTCTGCCTTCACAGATACCCAGTATCTCCAAGATACCATGAACCATGTC
CTAAGCTGTGTCAAGAAGGAGAAGGAACGTACAGCGGCCTTCCAAGCCCTGGGGCTACTT
TCTGTGGCTGTGAGGTCTGAGTTTAAGGTCTATTTGCCTCGCGTGCTGGACATCATCCGA
GCGGCCCTGCCCCCAAAGGACTTCGCCCATAAGAGGCAGAAGGCAATGCAGGTGGACGCC
ACAGTCTTCACTTGCATCAGCATGCTGGCTCGAGCAATGGGGCCAGGCATCCAGCAGGAT
ATCAAGGAGCTGCTGGAGCCCATGCTGGCAGTGGGACTAAGCCCTGCCCTCACTGCAGTG
CTCTACGACCTGAGCCGTCAGATTCCACAGCTAAAGAAGGACATTCAAGATGGGCTACTG
AAAATGCTGTCCCTGGTCCTTATGCACAAACCCCTTCGCCACCCAGGCATGCCCAAGGGC
CTGGCCCATCAGCTGGCCTCTCCTGGCCTCACGACCCTCCCTGAGGCCAGCGATGTGGGC
AGCATCACTCTTGCCCTCCGAACGCTTGGCAGCTTTGAATTTGAAGGCCACTCTCTGACC
CAATTTGTTCGCCACTGTGCGGATCATTTCCTGAACAGTGAGCACAAGGAGATCCGCATG
GAGGCTGCCCGCACCTGCTCCCGCCTGCTCACACCCTCCATCCACCTCATCAGTGGCCAT
GCTCATGTGGTTAGCCAGACCGCAGTGCAAGTGGTGGCAGATGTGCTTAGCAAACTGCTC
GTAGTTGGGATAACAGATCCTGACCCTGACATTCGCTACTGTGTCTTGGCGTCCCTGGAC
GAGCGCTTTGATGCACACCTGGCCCAGGCGGAGAACTTGCAGGCCTTGTTTGTGGCTCTG
AATGACCAGGTGTTTGAGATCCGGGAGCTGGCCATCTGCACTGTGGGCCGACTCAGTAGC
ATGAACCCTGCCTTTGTCATGCCTTTCCTGCGCAAGATGCTCATCCAGATTTTGACAGAG
TTGGAGCACAGTGGGATTGGAAGAATCAAAGAGCAGAGTGCCCGCATGCTGGGGCACCTG
GTCTCCAATGCCCCCCGACTCATCCGCCCCTACATGGAGCCTATTCTGAAGGCATTAATT
TTGAAACTGAAAGATCCAGACCCTGATCCAAACCCAGGTGTGATCAATAATGTCCTGGCA
ACAATAGGAGAATTGGCACAGGTTAGTGGCCTGGAAATGAGGAAATGGGTTGATGAACTT
TTTATTATCATCATGGACATGCTCCAGGATTCCTCTTTGTTGGCCAAAAGGCAGGTGGCT
CTGTGGACCCTGGGACAGTTGGTGGCCAGCACTGGCTATGTAGTAGAGCCCTACAGGAAG
TACCCTACTTTGCTTGAGGTGCTACTGAATTTTCTGAAGACTGAGCAGAACCAGGGTACA
CGCAGAGAGGCCATCCGTGTGTTAGGGCTTTTAGGGGCTTTGGATCCTTACAAGCACAAA
GTGAACATTGGCATGATAGACCAGTCCCGGGATGCCTCTGCTGTCAGCCTGTCAGAATCC
AAGTCAAGTCAGGATTCCTCTGACTATAGCACTAGTGAAATGCTGGTCAACATGGGAAAC
TTGCCTCTGGATGAGTTCTACCCAGCTGTGTCCATGGTGGCCCTGATGCGGATCTTCCGA
GACCAGTCACTCTCTCATCATCACACCATGGTTGTCCAGGCCATCACCTTCATCTTCAAG
TCCCTGGGACTCAAATGTGTGCAGTTCCTGCCCCAGGTCATGCCCACGTTCCTTAATGTC
ATTCGAGTCTGTGATGGGGCCATCCGGGAATTTTTGTTCCAGCAGCTGGGAATGTTGGTG
TCCTTTGTGAAGAGCCACATCAGACCTTATATGGATGAAATAGTCACCCTCATGAGAGAA
TTCTGGGTCATGAACACCTCAATTCAGAGCACGATCATTCTTCTCATTGAGCAAATTGTG
GTAGCTCTTGGGGGTGAATTTAAGCTCTACCTGCCCCAGCTGATCCCACACATGCTGCGT
GTCTTCATGCATGACAACAGCCCAGGCCGCATTGTCTCTATCAAGTTACTGGCTGCAATC
CAGCTGTTTGGCGCCAACCTGGATGACTACCTGCATTTACTGCTGCCTCCTATTGTTAAG
TTGTTTGATGCCCCTGAAGCTCCACTGCCATCTCGAAAGGCAGCGCTAGAGACTGTGGAC
CGCCTGACGGAGTCCCTGGATTTCACTGACTATGCCTCCCGGATCATTCACCCTATTGTT
CGAACACTGGACCAGAGCCCAGAACTGCGCTCCACAGCCATGGACACGCTGTCTTCACTT
GTTTTTCAGCTGGGGAAGAAGTACCAAATTTTCATTCCAATGGTGAATAAAGTTCTGGTG
CGACACCGAATCAATCATCAGCGCTATGATGTGCTCATCTGCAGAATTGTCAAGGGATAC
ACACTTGCTGATGAAGAGGAGGATCCTTTGATTTACCAGCATCGGATGCTTAGGAGTGGC
CAAGGGGATGCATTGGCTAGTGGACCAGTGGAAACAGGACCCATGAAGAAACTGCACGTC
AGCACCATCAACCTCCAAAAGGCCTGGGGCGCTGCCAGGAGGGTCTCCAAAGATGACTGG
CTGGAATGGCTGAGACGGCTGAGCCTGGAGCTGCTGAAGGACTCATCATCGCCCTCCCTG
CGCTCCTGCTGGGCCCTGGCACAGGCCTACAACCCGATGGCCAGGGATCTCTTCAATGCT
GCATTTGTGTCCTGCTGGTCTGAACTGAATGAAGATCAACAGGATGAGCTCATCAGAAGC
ATCGAGTTGGCCCTCACCTCACAAGACATCGCTGAAGTCACACAGACCCTCTTAAACTTG
GCTGAATTCATGGAACACAGTGACAAGGGCCCCCTGCCACTGAGAGATGACAATGGCATT
GTTCTGCTGGGTGAGAGAGCTGCCAAGTGCCGAGCATATGCCAAAGCACTACACTACAAA
GAACTGGAGTTCCAGAAAGGCCCCACCCCTGCCATTCTAGAATCTCTCATCAGCATTAAT
AATAAGCTACAGCAGCCGGAGGCAGCGGCCGGAGTGTTAGAATATGCCATGAAACACTTT
GGAGAGCTGGAGATCCAGGCTACCTGGTATGAGAAACTGCACGAGTGGGAGGATGCCCTT
GTGGCCTATGACAAGAAAATGGACACCAACAAGGACGACCCAGAGCTGATGCTGGGCCGC
ATGCGCTGCCTCGAGGCCTTGGGGGAATGGGGTCAACTCCACCAGCAGTGCTGTGAAAAG
TGGACCCTGGTTAATGATGAGACCCAAGCCAAGATGGCCCGGATGGCTGCTGCAGCTGCA
TGGGGTTTAGGTCAGTGGGACAGCATGGAAGAATACACCTGTATGATCCCTCGGGACACC
CATGATGGGGCATTTTATAGAGCTGTGCTGGCACTGCATCAGGACCTCTTCTCCTTGGCA
CAACAGTGCATTGACAAGGCCAGGGACCTGCTGGATGCTGAATTAACTGCAATGGCAGGA
GAGAGTTACAGTCGGGCATATGGGGCCATGGTTTCTTGCCACATGCTGTCCGAGCTGGAG
GAGGTTATCCAGTACAAACTTGTCCCCGAGCGACGAGAGATCATCCGCCAGATCTGGTGG
GAGAGACTGCAGGGCTGCCAGCGTATCGTAGAGGACTGGCAGAAAATCCTTATGGTGCGG
TCCCTTGTGGTCAGCCCTCATGAAGACATGAGAACCTGGCTCAAGTATGCAAGCCTGTGC
GGCAAGAGTGGCAGGCTGGCTCTTGCTCATAAAACTTTAGTGTTGCTCCTGGGAGTTGAT
CCGTCTCGGCAACTTGACCATCCTCTGCCAACAGTTCACCCTCAGGTGACCTATGCCTAC
ATGAAAAACATGTGGAAGAGTGCCCGCAAGATCGATGCCTTCCAGCACATGCAGCATTTT
GTCCAGACCATGCAGCAACAGGCCCAGCATGCCATCGCTACTGAGGACCAGCAGCATAAG
CAGGAACTGCACAAGCTCATGGCCCGATGCTTCCTGAAACTTGGAGAGTGGCAGCTGAAT
CTACAGGGCATCAATGAGAGCACAATCCCCAAAGTGCTGCAGTACTACAGCGCCGCCACA
GAGCACGACCGCAGCTGGTACAAGGCCTGGCATGCGTGGGCAGTGATGAACTTCGAAGCT
GTGCTACACTACAAACATCAGAACCAAGCCCGCGATGAGAAGAAGAAACTGCGTCATGCC
AGCGGGGCCAACATCACCAACGCCACCACTGCCGCCACCACGGCCGCCACTGCCACCACC
ACTGCCAGCACCGAGGGCAGCAACAGTGAGAGCGAGGCCGAGAGCACCGAGAACAGCCCC
ACCCCATCGCCGCTGCAGAAGAAGGTCACTGAGGATCTGTCCAAAACCCTCCTGATGTAC
ACGGTGCCTGCCGTCCAGGGCTTCTTCCGTTCCATCTCCTTGTCACGAGGCAACAACCTC
CAGGATACACTCAGAGTTCTCACCTTATGGTTTGATTATGGTCACTGGCCAGATGTCAAT
GAGGCCTTAGTGGAGGGGGTGAAAGCCATCCAGATTGATACCTGGCTACAGGTTATACCT
CAGCTCATTGCAAGAATTGATACGCCCAGACCCTTGGTGGGACGTCTCATTCACCAGCTT
CTCACAGACATTGGTCGGTACCACCCCCAGGCCCTCATCTACCCACTGACAGTGGCTTCT
AAGTCTACCACGACAGCCCGGCACAATGCAGCCAACAAGATTCTGAAGAACATGTGTGAG
CACAGCAACACCCTGGTCCAGCAGGCCATGATGGTGAGCGAGGAGCTGATCCGAGTGGCC
ATCCTCTGGCATGAGATGTGGCATGAAGGCCTGGAAGAGGCATCTCGTTTGTACTTTGGG
GAAAGGAACGTGAAAGGCATGTTTGAGGTGCTGGAGCCCTTGCATGCTATGATGGAACGG
GGCCCCCAGACTCTGAAGGAAACATCCTTTAATCAGGCCTATGGTCGAGATTTAATGGAG
GCCCAAGAGTGGTGCAGGAAGTACATGAAATCAGGGAATGTCAAGGACCTCACCCAAGCC
TGGGACCTCTATTATCATGTGTTCCGACGAATCTCAAAGCAGCTGCCTCAGCTCACATCC
TTAGAGCTGCAATATGTTTCCCCAAAACTTCTGATGTGCCGGGACCTTGAATTGGCTGTG
CCAGGAACATATGACCCCAACCAGCCAATCATTCGCATTCAGTCCATAGCACCGTCTTTG
CAAGTCATCACATCCAAGCAGAGGCCCCGGAAATTGACACTTATGGGCAGCAACGGACAT
GAGTTTGTTTTCCTTCTAAAAGGCCATGAAGATCTGCGCCAGGATGAGCGTGTGATGCAG
CTCTTCGGCCTGGTTAACACCCTTCTGGCCAATGACCCAACATCTCTTCGGAAAAACCTC
AGCATCCAGAGATACGCTGTCATCCCTTTATCGACCAACTCGGGCCTCATTGGCTGGGTT
CCCCACTGTGACACACTGCACGCCCTCATCCGGGACTACAGGGAGAAGAAGAAGATCCTT
CTCAACATCGAGCATCGCATCATGTTGCGGATGGCTCCGGACTATGACCACTTGACTCTG
ATGCAGAAGGTGGAGGTGTTTGAGCATGCCGTCAATAATACAGCTGGGGACGACCTGGCC
AAGCTGCTGTGGCTGAAAAGCCCCAGCTCCGAGGTGTGGTTTGACCGAAGAACCAATTAT
ACCCGTTCTTTAGCGGTCATGTCAATGGTTGGGTATATTTTAGGCCTGGGAGATAGACAC
CCATCCAACCTGATGCTGGACCGTCTGAGTGGGAAGATCCTGCACATTGACTTTGGGGAC
TGCTTTGAGGTTGCTATGACCCGAGAGAAGTTTCCAGAGAAGATTCCATTTAGACTAACA
AGAATGTTGACCAATGCTATGGAGGTTACAGGCCTGGATGGCAACTACAGAATCACATGC
CACACAGTGATGGAGGTGCTGCGAGAGCACAAGGACAGTGTCATGGCCGTGCTGGAAGCC
TTTGTCTATGACCCCTTGCTGAACTGGAGGCTGATGGACACAAATACCAAAGGCAACAAG
CGATCCCGAACGAGGACGGATTCCTACTCTGCTGGCCAGTCAGTCGAAATTTTGGACGGT
GTGGAACTTGGAGAGCCAGCCCATAAGAAAACGGGGACCACAGTGCCAGAATCTATTCAT
TCTTTCATTGGAGACGGTTTGGTGAAACCAGAGGCCCTAAATAAGAAAGCTATCCAGATT
ATTAACAGGGTTCGAGATAAGCTCACTGGTCGGGACTTCTCTCATGATGACACTTTGGAT
GTTCCAACGCAAGTTGAGCTGCTCATCAAACAAGCGACATCCCATGAAAACCTCTGCCAG
TGCTATATTGGCTGGTGCCCTTTCTGGTAA
Target 1 GenBank Gene ID
Target 1 GeneCard ID FRAP1 Link Image
Target 1 GenAtlas ID FRAP1 Link Image
Target 1 HGNC ID HGNC:3942 Link Image
Target 1 Chromosome Location 1
Target 1 Locus 1p36.2
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Liang J, Choi J, Clardy J: Refined structure of the FKBP12-rapamycin-FRB ternary complex at 2.2 A resolution. Acta Crystallogr D Biol Crystallogr. 1999 Apr;55(Pt 4):736-44. [PubMed Link Image]
  2. Stover C, Endo Y, Takahashi M, Lynch NJ, Constantinescu C, Vorup-Jensen T, Thiel S, Friedl H, Hankeln T, Hall R, Gregory S, Fujita T, Schwaeble W: The human gene for mannan-binding lectin-associated serine protease-2 (MASP-2), the effector component of the lectin route of complement activation, is part of a tightly linked gene cluster on chromosome 1p36.2-3. Genes Immun. 2001 May;2(3):119-27. [PubMed Link Image]
  3. Chiu MI, Katz H, Berlin V: RAPT1, a mammalian homolog of yeast Tor, interacts with the FKBP12/rapamycin complex. Proc Natl Acad Sci U S A. 1994 Dec 20;91(26):12574-8. [PubMed Link Image]
  4. Brown EJ, Albers MW, Shin TB, Ichikawa K, Keith CT, Lane WS, Schreiber SL: A mammalian protein targeted by G1-arresting rapamycin-receptor complex. Nature. 1994 Jun 30;369(6483):756-8. [PubMed Link Image]
  5. Choi J, Chen J, Schreiber SL, Clardy J: Structure of the FKBP12-rapamycin complex interacting with the binding domain of human FRAP. Science. 1996 Jul 12;273(5272):239-42. [PubMed Link Image]
  6. Onyango P, Lubyova B, Gardellin P, Kurzbauer R, Weith A: Molecular cloning and expression analysis of five novel genes in chromosome 1p36. Genomics. 1998 Jun 1;50(2):187-98. [PubMed Link Image]
Target 1 Drug References
  1. Radulovic S, Bjelogrlic SK: Sunitinib, sorafenib and mTOR inhibitors in renal cancer. J BUON. 2007 Sep;12 Suppl 1:S151-62. [PubMed Link Image]
  2. Patard JJ, Pouessel D, Bensalah K, Culine S: Targeted therapy in renal cell carcinoma. World J Urol. 2008 Apr;26(2):135-40. Epub 2008 Feb 12. [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.