Recent advances in B-RAF inhibitors as anticancer agents

• Published in: Bioorganic chemistry Vol. 120; p. 105597
• Main Authors: Khan, Pathan Shahebaaz, Rajesh, Patil, Rajendra, Patil, Chaskar, Manohar G., Rohidas, Arote, Jaiprakash, Sangshetti
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01-03-2022
• Subjects: Cancer; ERK; MAPK; MEK; RAF; MEK; MAPK; RAF; ERK; Cancer
• ISSN: 0045-2068; 1090-2120
• DOI: 10.1016/j.bioorg.2022.105597

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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.