ArticleBioorganic & medicinal chemistry2007
Development of selective inhibitors for anti-apoptotic Bcl-2 proteins from BHI-1.
Article in Bioorganic & medicinal chemistry, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- Modifying inhibitor specificity for homologous enzymes by machine learning.The FEBS journal · 2026Article
- Anticancer Profile of Rhodanines: Structure-Activity Relationship (SAR) and Molecular Targets-A Review.Molecules (Basel, Switzerland) · 2022Review
- 5-Ene-4-thiazolidinones - An efficient tool in medicinal chemistry.European journal of medicinal chemistry · 2017Review
- Synthesis and anticancer activity of novel quinazolinone-based rhodanines.Chemistry Central journal · 2017Article
- Design and synthesis of L- and D-phenylalanine derived rhodanines with novel C5-arylidenes as inhibitors of HCV NS5B polymerase.Bioorganic & medicinal chemistry · 2013Article
- Non-peptidic small molecule inhibitors against Bcl-2 for cancer therapy.Journal of cellular physiology · 2009Review
- WL-276, an antagonist against Bcl-2 proteins, overcomes drug resistance and suppresses prostate tumor growth.Cancer research · 2008Article
- Development of dimeric modulators for anti-apoptotic Bcl-2 proteins.Bioorganic & medicinal chemistry letters · 2008Article
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Authors and funding
4 authors.
Funding
Abstract
A series of inhibitors for anti-apoptotic Bcl-2 proteins based on BHI-1 were synthesized and their binding interactions with Bcl-2, Bcl-X(L), and Bcl-w were evaluated. It was found that modification of BHI-1 resulted in varied binding profiles among Bcl-2, Bcl-X(L), and Bcl-w, and a set of inhibitors with varied selectivity to Bcl-2, Bcl-X(L), and Bcl-w proteins have been identified. Molecular modeling of the interaction of the BHI-1 based analogues with the anti-apoptotic Bcl-2 proteins suggested that the binding site for the BHI-1 based inhibitor was the least conserved section among Bcl-2, Bcl-X(L), and Bcl-w: targeting the non-conserved section may account for the observed selectivity of the BHI-1 based inhibitors among the anti-apoptotic Bcl-2 proteins. The validity of the model was supported by a strong correlation between the model-calculated binding energy and the experimental binding affinity. In summary, our studies suggest that most of the reported inhibitors for anti-apoptotic Bcl-2 proteins are nonselective and BHI-1 is a promising template to distinguish among Bcl-2, Bcl-X(L), and Bcl-w by targeting the non-conserved domain among the anti-apoptotic Bcl-2 proteins. Molecular-modeling-aided rational development of BHI-1 based selective inhibitor for anti-apoptotic Bcl-2 proteins is underway.
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