Trends in targeting Bcl-2 anti-apoptotic proteins for cancer treatment

Eur J Med Chem. 2022 Mar 15:232:114184. doi: 10.1016/j.ejmech.2022.114184.

Zhenwei Zhang ¹, Lijun Bai ¹, Linghui Hou ¹, Hongguang Deng ¹, Shenglin Luan ², Dan Liu ¹, Min Huang ³, Linxiang Zhao ⁴

Affiliations

1 Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China.
2 China Resources Sanjiu Medical & Pharmaceutical Co. Ltd, Shenzhen, China.
3 Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China. Electronic address: huangcrazye@sina.com.
4 Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China. Electronic address: linxiang.zhao@vip.sina.com.

PMID: 35182816 DOI: 10.1016/j.ejmech.2022.114184

Abstract

Apoptosis is the major mode of programmed cell death, which conduces to maintain tissue homeostasis, clearance of abnormal cells and development of organisms. Over the past two decades, great progress and significant clinical benefits in Cancer treatment have been made by targeting Bcl-2 anti-apoptotic proteins. However, with the deep research of clinic, the therapeutic value of single target inhibitors is restricted due to the limited monotherapy activity, potential and complex drug resistance as well as monotherapy safety. This review focuses on recent advance in discovery of novel Apoptosis inducers targeting Bcl-2 anti-apoptotic proteins aiming to overcome existing therapeutic limitations, and introduce the strategies and advanced technologies in the drug design and optimization.

Keywords

Antibody-drug conjugates; Bcl-2 anti-apoptotic proteins; Cancer treatment; Degraders; Dual targeting BH3 mimetics.

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