Recent advances in B-RAF inhibitors as anticancer agents.

Pathan Shahebaaz Khan, Patil Rajesh, Patil Rajendra, Manohar G Chaskar, Arote Rohidas, Sangshetti Jaiprakash

Bioorganic chemistry 2022 Mar

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The significance of B-RAF in the promotion of cell proliferation and motility was explored by the researchers in the past. However, in 2002, several researchers found that mutation in B-RAF leads to cancer. Extensive research on B-RAF mutations suggested B-RAF V600E mutation as a critical predictive, prognostic and diagnostic biomarker in numerous cancers such as melanoma, thyroid, and colorectal cancers. Based on the significance of B-RAF kinase and associated mutation, the present review will give a brief overview about structure and functions of B-RAF enzyme, its role in different types of cancer, available drugs in the market for B-RAF inhibition, chemical classification and SAR studies of reported investigational B-RAF inhibitors in patented and non-patented literature during last decade. The SAR provided for all the reported inhibitors will help researchers to gain knowledge about the possible structural features required for selective B-RAF inhibition. This insightful analysis of B-RAF will certainly help researchers to develop novel anticancer agents in the future. Copyright © 2022 Elsevier Inc. All rights reserved.

Citation

Pathan Shahebaaz Khan, Patil Rajesh, Patil Rajendra, Manohar G Chaskar, Arote Rohidas, Sangshetti Jaiprakash. Recent advances in B-RAF inhibitors as anticancer agents. Bioorganic chemistry. 2022 Mar;120:105597