Therapeutic Targets Database
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TTD Target ID: TTDS00350

Target Information
NameProto-oncogene tyrosine-protein kinase ABL1    
Type of targetSuccessful target    
SynonymsC-ABL    
P150    
DiseaseMyeloma disease
[ICD9: 203.0   ICD10: C90.0]
[1]
Drug(s)Adenosine triphosphateApprovedDietary shortage[2][3]
DasatinibLaunchedChronic myelogenous leukemia [4][5][6]
ImatinibLaunchedChronic myelogenous leukemia [4]
ImatinibPhase IIIIntestinal cancer & myeloid leukemia[4]
NilotinibPhase IIILeukemia[4]
AZD0530Phase IIOsteosarcoma; Hematological malignancies, solid tumours[4][7]
DasatinibPhase IISolid tumours, multiple myeloma[4][5][6]
ImatinibPhase IIGlioma, lung, prostate, solid tumours[4]
NilotinibPhase IIALL, CML, GIST[4]
BosutinibPhase I/IIAdvanced Breast Cancer[4]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.112
PathwayAxon guidance
Cell cycle
Chronic myeloid leukemia
ErbB signaling pathway
Pathogenic Escherichia coli infection
Pathogenic Escherichia coli infection
Pathways in cancer
UniProt IDP00519
P42684
PDB Structure2ECD; 2KK1; 2XYN; 3GVU; 3HMI; 3ULR; 4EIH.    
SequenceMGQQVGRVGEAPGLQQPQPRGIRGSSAARPSGRRRDPAGRTTETGFNIFTQHDHFASCVE DGFEGDKTGGSSPEALHRPYGCDVEPQALNEAIRWSSKENLLGATESDPNLFVALYDFVA SGDNTLSITKGEKLRVLGYNQNGEWSEVRSKNGQGWVPSNYITPVNSLEKHSWYHGPVSR SAAEYLLSSLINGSFLVRESESSPGQLSISLRYEGRVYHYRINTTADGKVYVTAESRFST LAELVHHHSTVADGLVTTLHYPAPKCNKPTVYGVSPIHDKWEMERTDITMKHKLGGGQYG EVYVGVWKKYSLTVAVKTLKEDTMEVEEFLKEAAVMKEIKHPNLVQLLGVCTLEPPFYIV TEYMPYGNLLDYLRECNREEVTAVVLLYMATQISSAMEYLEKKNFIHRDLAARNCLVGEN HVVKVADFGLSRLMTGDTYTAHAGAKFPIKWTAPESLAYNTFSIKSDVWAFGVLLWEIAT YGMSPYPGIDLSQVYDLLEKGYRMEQPEGCPPKVYELMRACWKWSPADRPSFAETHQAFE TMFHDSSISEEVAEELGRAASSSSVVPYLPRLPILPSKTRTLKKQVENKENIEGAQDATE NSASSLAPGFIRGAQASSGSPALPRKQRDKSPSSLLEDAKETCFTRDRKGGFFSSFMKKR NAPTPPKRSSSFREMENQPHKKYELTGNFSSVASLQHADGFSFTPAQQEANLVPPKCYGG SFAQRNLCNDDGGGGGGSGTAGGGWSGITGFFTPRLIKKTLGLRAGKPTASDDTSKPFPR SNSTSSMSSGLPEQDRMAMTLPRNCQRSKLQLERTVSTSSQPEENVDRANDMLPKKSEES AAPSRERPKAKLLPRGATALPLRTPSGDLAITEKDPPGVGVAGVAAAPKGKEKNGGARLG MAGVPEDGEQPGWPSPAKAAPVLPTTHNHKVPVLISPTLKHTPADVQLIGTDSQGNKFKL LSEHQVTSSGDKDRPRRVKPKCAPPPPPVMRLLQHPSICSDPTEEPTALTAGQSTSETQE GGKKAALGAVPISGKAGRPVMPPPQVPLPTSSISPAKMANGTAGTKVALRKTKQAAEKIS ADKISKEALLECADLLSSALTEPVPNSQLVDTGHQLLDYCSGYVDCIPQTRNKFAFREAV SKLELSLQELQVSSAAAGVPGTNPVLNNLLSCVQEISDVVQR
Target ValidationClick to Find Target Validation Information.    
Inhibitor (E)-4-[8]
3'',5''-dimethoxy-[1,1',   2',1'']-terphenyl-4-ol[8]
3'',5''-dimethoxy-[1,1',   3',1'']-terphenyl-4-ol[8]
4,3'',5''-trimethoxy-[1,1',   2',1'']-terphenyl[8]
4,3'',5''-trimethoxy-[1,1',   3',1'']-terphenyl[8]
4-[ (3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol[9]
AG-1879[10]
AP-24163[11]
AP-24226[11]
AZD0530[4][7]
Adenosine triphosphate[2][3]
BAS-00387275[12]
BAS-00387328[12]
BAS-00387347[12]
BAS-00672722[12]
BAS-01373578[12]
BAS-0338872[13]
BAS-0338876[13]
BAS-09534324[12]
Bis- (5-hydroxy-1H-indol-2-yl)-methanone[14]
Bosutinib[4]
Dasatinib[4][5][6]
Imatinib[4]
JNJ-10198409[15]
MYRISTIC ACID[16]
Nilotinib[4]
PD-0166326,   PD-166326[17]
PD-0173955,   PD-17395[18]
PD-0173956[17]
SKI-758[19]
TG-100435[20]
TRISMETHOXYRESVERATROL[8]
[1,1',   2',1'']-terphenyl-4,3'',5''-triol[8]
MultitargetAZD0530[4][7]
Bosutinib[4]
Dasatinib[4][5][6]
Imatinib[4]
Nilotinib[4]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Comparison of gene expression profiling between malignant and normal plasma cells with oligonucleotide arrays. Oncogene. 2002 Oct 3;21(44):6848-57. To Reference
Ref 2Targeted chronic myeloid leukemia therapy: Seeking a cure. Am J Health Syst Pharm. 2007 Dec 15;64(24 Suppl 15):S9-15. To Reference
Ref 3High frequency of point mutations clustered within the adenosine triphosphate-binding region of BCR/ABL in patients with chronic myeloid leukemia or Ph-positive acute lymphoblastic leukemia who develop imatinib (STI571) resistance. Blood. 2002 May 1;99(9):3472-5. To Reference
Ref 4A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. To Reference
Ref 5In vitro and clinical investigation of the relationship between CCR5 receptor occupancy and anti-HIV activity of Aplaviroc. J Clin Pharmacol. 2008 Oct;48(10):1179-88. Epub 2008 Aug 1. To Reference
Ref 6Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42. Epub 2006 Nov 28. To Reference
Ref 7AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 8J Med Chem. 2006 May 18;49(10):3012-8.Identification of a terphenyl derivative that blocks the cell cycle in the G0-G1 phase and induces differentiation in leukemia cells. To Reference
Ref 9J Med Chem. 2006 Nov 2;49(22):6500-9.4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. To Reference
Ref 10J Med Chem. 2008 Mar 13;51(5):1252-9. Epub 2008 Feb 8.Structure-based optimization of pyrazolo[3,4-d]pyrimidines as Abl inhibitors and antiproliferative agents toward human leukemia cell lines. To Reference
Ref 11J Med Chem. 2010 Jun 24;53(12):4701-19.Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant. To Reference
Ref 12J Med Chem. 2006 Jun 1;49(11):3278-86.A combination of docking/dynamics simulations and pharmacophoric modeling to discover new dual c-Src/Abl kinase inhibitors. To Reference
Ref 13Bioorg Med Chem Lett. 2008 Feb 1;18(3):1207-11. Epub 2007 Dec 4.Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents. To Reference
Ref 14J Med Chem. 2006 Jun 1;49(11):3101-15.Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase. To Reference
Ref 15J Med Chem. 2005 Dec 29;48(26):8163-73.(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells. To Reference
Ref 16Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 17Bioorg Med Chem Lett. 2009 Dec 15;19(24):6872-6. Epub 2009 Oct 23.Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors. To Reference
Ref 18J Med Chem. 2006 Sep 21;49(19):5759-68.Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling. To Reference
Ref 19J Med Chem. 2006 Dec 28;49(26):7868-76.Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. To Reference
Ref 20Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. Epub 2006 Nov 7.Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays. To Reference



 

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