| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 5142754 | Chinese Chemical Letters | 2017 | 9 Pages |
Abstract
A series of peptides derived from Bim BH3 domain were synthesized and the in vitro binding affinity on anti-apoptotic Bcl-2 proteins and cell killing activity were evaluated. Of particular interest were the analogue SM-5 (KDÂ =Â 9.48Â nmol/L for Bcl-2) and SM-6 (KDÂ =Â 0.08Â nmol/L for Bcl-xL), which exhibited improved binding affinity compared with the lead Bim (KDÂ =Â 16.90Â nmol/L for Bcl-2 and 22.2Â nmol/L for Bcl-xL, respectively). Promising inhibitors of anti-apoptotic Bcl-2 proteins might be designed based on the active core.
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Authors
Chuan-Liang Zhang, Shan Liu, Xiao-Chun Liu, Jiang-Ming Gao, Shu-Lin Wang,