Therapeutic Targets Database
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TTD Target ID: TTDS00265

Target Information
NameSerine/threonine-protein kinase mTOR    
Type of targetSuccessful target    
SynonymsFK506-binding protein 12-rapamycin complex-associated protein 1    
FKBP-rapamycin associated protein    
FKBP12-rapamycin complex-associated protein    
FRAP    
FRAP1    
Mammalian target of rapamycin    
RAPT1    
Rapamycin target protein    
TOR kinase    
Target of rapamycin    
mTOR    
DiseaseCancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[1]
Immunosuppression[2]
Drug(s)EverolimusApprovedRenal cell carcinoma[3][4]
SirolimusApprovedOrgan rejection[5]
TemsirolimusApprovedRenal cell carcinoma[6]
Zotarolimus; Abt-578ApprovedOncological disease[7]
AP23573Phase IIIMetastatic Soft-Tissue Sarcomas; Metastatic Bone Sarcomas[8]
EverolimusPhase IIIAdvanced kidney cancer[3]
RidaforolimusPhase IIICancer; Sarcoma[9][10]
TemsirolimusPhase IIIRenal cell carcinoma[6]
KD032Phase II completedNSCLC (see also pancreatic)
KD032Phase I/II completedPancreatic Cancer
DeforolimusPhase IIMultiple myeloma[11]
GDC-0980/RG7422Phase IINon-Hodgkin lymphoma
PF-04691502Phase IIEndometrial cancer
PF-05212384Phase IIEndometrial cancer
RG7422Phase IISolid tumors, non-Hodgkin's lymphoma
AZD8055Phase I/IIAdvanced solid tumours; endometrial carcinoma; lymphoma[12]
BEZ235Phase I/IIAdvanced solid tumours; Advanced breast cancer[8]
BGT226Phase I/IISolid tumours; Advanced breast cancer; CowdenĄŻs syndrome[8]
SirolimusPhase I/IIDutch Elm disease[5]
XL765Phase I/IISolid tumours; non-small-cell lung cancer; malignant gliomas[13]
AZD2014Phase ISolid Tumors
AZD2014Phase ISolid tumours
CC-223Phase IMultiple Myeloma
CC-223Phase INSCLC (see also lymphoma, multiple myeloma)
CC-223Phase INon-Hodgkin's lymphoma
DS-3078Phase ISolid cancer, lymphoma
DS-7423Phase ISolid cancer
GDC-0980Phase IAdvanced solid tumours, non-Hodgkin's lymphoma[14]
GSK2126458Phase ILymphoma
GSK2126458Phase ISolid Tumors
INK128Phase IMultiple Myeloma[15]
OSI-027Phase ISolid tumours; Lymphoma[8]
PF-04691502Phase ISolid Tumors
PF-05212384Phase ISolid Tumors
PI3 Kinase/mTOR InhibitorPhase ICancer
PWT33597Phase ISolid Tumors
SAR245409/MSC1936369B combination therapyPhase ISolid Tumors
PathwayAcute myeloid leukemia
Adipocytokine signaling pathway
ErbB signaling pathway
Glioma
Insulin signaling pathway
Pathways in cancer
Prostate cancer
Type II diabetes mellitus
mTOR signaling pathway
UniProt IDP42345
PDB Structure1AUE; 1FAP; 1NSG; 2FAP; 2GAQ; 2NPU; 2RSE; 3FAP; 4DRH; 4DRI; 4DRJ; 4FAP; 4JSN; 4JSP; 4JSV; 4JSX; 4JT5; 4JT6.    
FunctionActs as the target for the cell-cycle arrest and immunosuppressive effects of the fkbp12-rapamycin complex.    
SequenceMLGTGPAAATTAATTSSNVSVLQQFASGLKSRNEETRAKAAKELQHYVTMELREMSQEES 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 ValidationClick to Find Target Validation Information.    
Inhibitor (4-[16]
2- (2-Methyl-morpholin-4-yl)-benzo[h]chromen-4-one[17]
2- (6-morpholino-9H-purin-2-yl)phenol[16]
2-Morpholin-4-yl-pyrimido[2,1-a]isoquinolin-4-one[17]
2-chloro-N- (6-cyanopyridin-3-yl)propanamide[18]
3- (6-morpholino-9H-purin-2-yl)phenol[16]
4- (2-[16]
4- (2-[16]
4- (2-[16]
4- (6-morpholino-9H-purin-2-yl)phenol[16]
AP-21967[19]
AP23573[8]
AZD8055[12]
BEZ235[8]
BGT226[8]
C-16- (S)-3-methylindolerapamycin[19]
Deforolimus[11]
Everolimus[3][4]
Everolimus[3]
GDC-0980[14]
INK128[15]
LY-293646[17]
LY-294002[17]
Macrolide derivative[20]
Macrolide derivative[20]
OSI-027[8]
Rapamycin[11]
Rapamycin complexed with immunophilin FKBP12[1]
Ridaforolimus[9][10]
Sirolimus[5]
Temsirolimus[6]
XL765[13]
MultitargetBEZ235[8]
BGT226[8]
GDC-0980[14]
XL765[13]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Selected novel anticancer treatments targeting cell signaling proteins. Oncologist. 2001;6(6):517-37. To Reference
Ref 2Vaccination with CD20 peptides induces a biologically active, specific immune response in mice. Blood. 2002 May 15;99(10):3748-55. To Reference
Ref 3Mammalian target of rapamycin, its mode of action and clinical response in metastatic clear cell carcinoma. Gan To Kagaku Ryoho. 2009 Jul;36(7):1076-9. To Reference
Ref 4Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92. To Reference
Ref 5Nat Rev Drug Discov. 2003 Jan;2(1):38-51.Knockouts model the 100 best-selling drugs--will they model the next 100? To Reference
Ref 6Targeted therapies and their indications in solid neoplasias. Rev Med Interne. 2009 May;30(5):416-24. Epub 2009 Mar 18. To Reference
Ref 718497896 To Reference
Ref 8Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44. To Reference
Ref 9Merck. Product Development Pipeline. July 15 2009. To Reference
Ref 10Merck. Report of Merck. January 20 2008. To Reference
Ref 11Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127. To Reference
Ref 12AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 13Pipeline of EXELIXIS. EXELIXIS. 2009 To Reference
Ref 142011 Pipeline of Genentech. To Reference
Ref 152011 Pipeline of Intellikine. To Reference
Ref 16Bioorg Med Chem Lett. 2010 Jan 15;20(2):636-9. Epub 2009 Dec 5.Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies. To Reference
Ref 17J Med Chem. 2005 Jan 27;48(2):569-85.Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro. To Reference
Ref 18Bioorg Med Chem Lett. 2009 Jun 1;19(11):2949-52. Epub 2009 Apr 18.Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors. To Reference
Ref 19J Biol Chem. 2007 May 4;282(18):13395-401. Epub 2007 Mar 9.The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain. To Reference
Ref 20J Med Chem. 2004 Sep 23;47(20):4950-7.A locally active antiinflammatory macrolide (MLD987) for inhalation therapy of asthma. To Reference



 

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Professor in Department of Pharmacy
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