Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00319

Target Information
NameApoptosis regulator Bcl-2    
Type of targetClinical trial target    
SynonymsBcl-2    
DiseaseChronic lymphocytic leukemia
[ICD9: 204.1   ICD10: C91.1]
[1]
Prostate cancer (hormone refractory)
[ICD9: 140-229, 185   ICD10: C00-C96, C61]
[2]
Waldenstrom's macroglobulinemia
[ICD9: 273.3   ICD10: C88.0]
[3]
Drug(s)MCI-186Phase III completedAmyotrophic Lateral Sclerosis (ALS), Stroke[4]
OblimersenPhase IIIAdvanced Melanoma and Normal or Impaired Hepatic Function, Multiple myeloma[5]
ABT-263Phase IIAdvanced small cell lung cancer; Relapsed or refractory chronic lymphocytic leukemia; Relapsed or refractory lymphoid malignancies[6][7][8]
AT-101Phase IILymphoid Leukemia, Non-Hodgkin's Lymphoma, Prostate Cancer[9]
PNT2258Phase IIB-cell lymphoma
ABT-199/GDC-0199Phase ICLL
ABT-199/GDC-0199/RG7601Phase IMyeloma (see also leukemia, lymphoma)
ABT-199/GDC-0199/RG7601Phase INon-Hodgkin lymphoma (see also leukemia, myeloma)
ABT-199/GDC-0199/RG7601Phase IRelapsed/refractory chronic lymphocytic leukemia (CLL) (see also lymphoma, myeloma)
GDC-0199Phase IChronic lymphocytic leukemia and non-Hodgkin's lymphoma
PNT2258Phase ISolid Tumors
RG7601Phase IRelapsed or refractory chronic lymphocytic leukaemia
BioChemical ClassTransmembrane protein    
PathwayAmyotrophic lateral sclerosis (ALS)
Apoptosis
Colorectal cancer
Focal adhesion
Pathways in cancer
Prostate cancer
Small cell lung cancer
UniProt IDP10415
PDB Structure1G5M; 1GJH; 1YSW; 2O21; 2O22; 2O2F; 2W3L.    
FunctionSuppresses apoptosis in a variety of cell systems including factor-dependent lymphohematopoietic and neural cells. Regulates cell death by controlling the mitochondrial membrane permeability. appears to function in a feedback loop system with caspases.    
SequenceMAHAGRTGYDNREIVMKYIHYKLSQRGYEWDAGDVGAAPPGAAPAPGIFSSQPGHTPHPA ASRDPVARTSPLQTPAAPGAAAGPALSPVPPVVHLTLRQAGDDFSRRYRRDFAEMSSQLH LTPFTARGRFATVVEELFRDGVNWGRIVAFFEFGGVMCVESVNREMSPLVDNIALWMTEY LNRHLHTWIQDNGGWDAFVELYGPSMRPLFDFSWLSLKTLLSLALVGACITLGAYLGHK
Target ValidationClick to Find Target Validation Information.    
Inhibitor2,3,4-trihydroxy-5-isopropyl-N-phenyl-benzamide[10]
4,5-dibenzylbenzene-1,2-diol[11]
5,10-Dioxy-2-phenyl-benzo[g]pteridin-4-ylamine[12]
ABT-263[6][7][8]
ABT-737[13]
AT-101[9]
N-phenyl-2,3,4-trihydroxy-5-benzyl-benzamide[10]
Oblimersen[5]
QEDIIRNIARHLAQVGDSMDR[10]
TW-37[10]
RegulatorGossypol[14]
UpRegulatorMCI-186[4]
MultitargetABT-263[6][7][8]
AT-101[9]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Bcl-2 and apoptosis in chronic lymphocytic leukemia. Curr Treat Options Oncol. 2003 Jun;4(3):211-8. To Reference
Ref 2Fas-mediated killing of primary prostate cancer cells is increased by mitoxantrone and docetaxel. Mol Cancer Ther. 2008 Sep;7(9):3018-28. To Reference
Ref 3Modulation of the activity of Bcl-2 in Waldenstrom's macroglobulinemia using antisense oligonucleotides. Semin Oncol. 2003 Apr;30(2):297-9. To Reference
Ref 4Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52. To Reference
Ref 5Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127. To Reference
Ref 6Roche. Product Development Pipeline. July 29 2009. To Reference
Ref 7ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo. Mol Cancer Ther. 2008 Oct;7(10):3265-74. To Reference
Ref 8Cancer Res. 2008 May 1;68(9):3421-8.ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor. To Reference
Ref 9Mcl1 downregulation sensitizes neuroblastoma to cytotoxic chemotherapy and small molecule Bcl2-family antagonists. Cancer Biol Ther. 2009 Aug 8;8(16). [Epub ahead of print] To Reference
Ref 10J Med Chem. 2006 Oct 19;49(21):6139-42.Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins. To Reference
Ref 11J Med Chem. 2010 May 27;53(10):3899-906.Vaccinia virus virulence factor N1L is a novel promising target for antiviral therapeutic intervention. To Reference
Ref 12J Med Chem. 2001 Dec 6;44(25):4313-24.Discovery of small-molecule inhibitors of Bcl-2 through structure-based computer screening. To Reference
Ref 13J Med Chem. 2007 Feb 22;50(4):641-62. Epub 2007 Jan 26.Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. To Reference
Ref 14Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40. To Reference



 

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