Document Detail

Non-peptidic small molecule inhibitors against Bcl-2 for cancer therapy.
MedLine Citation:
PMID:  18767026     Owner:  NLM     Status:  MEDLINE    
A critical regulator of the apoptotic machinery is the Bcl-2 family proteins whose over expression confers a protective effect on malignant cells against death signals of apoptosis. Cancer cells that are resistant to various anti-cancer drugs and treatment regimen are found to over express these Bcl-2 proteins such as Bcl-2, Bcl-X(L), Mcl-1, Bcl-w, and A1/Bfl1. In recent years there has been an exponential growth in the identification as well as synthesis of non-peptidic cell permeable small-molecule inhibitors (SMIs) of protein-protein interaction. The focus of this article is on inhibitors of anti-apoptotic protein Bcl-2. This review summarizes an up to date knowledge of the available SMIs, their mode of action as well as their current status in preclinical as well as clinical development.
Asfar S Azmi; Ramzi M Mohammad
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Review    
Journal Detail:
Title:  Journal of cellular physiology     Volume:  218     ISSN:  1097-4652     ISO Abbreviation:  J. Cell. Physiol.     Publication Date:  2009 Jan 
Date Detail:
Created Date:  2008-11-03     Completed Date:  2008-12-09     Revised Date:  2014-09-12    
Medline Journal Info:
Nlm Unique ID:  0050222     Medline TA:  J Cell Physiol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  13-21     Citation Subset:  IM    
Copyright Information:
(c) 2008 Wiley-Liss, Inc.
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MeSH Terms
Aniline Compounds / pharmacology
Apoptosis / drug effects,  physiology
Benzamides / pharmacology
Binding Sites
Biphenyl Compounds / pharmacology
Gossypol / analogs & derivatives,  pharmacology
Lymphoma / drug therapy
Models, Molecular
Neoplasms / drug therapy*,  pathology,  physiopathology
Nitrophenols / pharmacology
Piperazines / pharmacology
Protein Structure, Tertiary
Proto-Oncogene Proteins c-bcl-2 / antagonists & inhibitors*,  chemistry,  classification,  physiology
Pyrroles / pharmacology
Sulfonamides / pharmacology
Sulfones / pharmacology
Grant Support
CA109389/CA/NCI NIH HHS; R01 CA 109389/CA/NCI NIH HHS; R01 CA109389/CA/NCI NIH HHS; R01 CA109389-01A2/CA/NCI NIH HHS
Reg. No./Substance:
0/ABT-737; 0/Aniline Compounds; 0/Benzamides; 0/Biphenyl Compounds; 0/Nitrophenols; 0/Piperazines; 0/Proto-Oncogene Proteins c-bcl-2; 0/Pyrroles; 0/Sulfonamides; 0/Sulfones; 0/TW-37 compound; 0/obatoclax; KAV15B369O/Gossypol; XKJ5VVK2WD/navitoclax

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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