Literature DB >> 35033817

Recent advances in B-RAF inhibitors as anticancer agents.

Pathan Shahebaaz Khan1, Patil Rajesh2, Patil Rajendra3, Manohar G Chaskar4, Arote Rohidas5, Sangshetti Jaiprakash6.   

Abstract

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.

Entities:  

Keywords:  Cancer; ERK; MAPK; MEK; RAF

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Year:  2022        PMID: 35033817     DOI: 10.1016/j.bioorg.2022.105597

Source DB:  PubMed          Journal:  Bioorg Chem        ISSN: 0045-2068            Impact factor:   5.275


  1 in total

1.  Kinome profiling of cholangiocarcinoma organoids reveals potential druggable targets that hold promise for treatment stratification.

Authors:  Ruby Lieshout; Alessandra V S Faria; Monique M A Verstegen; Gwenny M Fuhler; Maikel P Peppelenbosch; Luc J W van der Laan
Journal:  Mol Med       Date:  2022-06-28       Impact factor: 6.376

  1 in total

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