MCL-1 as a potent target for cancer: Recent advancements, structural insights and SAR studies.

in Bioorganic chemistry by Vishakha Sharma, Ankush Kumar

TLDR

  • The review provides an overview of the recent advancements in designing Mcl-1 inhibitors, highlighting their potential in cancer treatment and the need for further research.

Abstract

The myeloid cell leukemia-1 (Mcl-1) differentiation protein belongs to the B-cell lymphoma 2 (Bcl-2) family of proteins which regulates the apoptosis or cell death. Mcl-1 is known for its pro-survival in response to various stressors. Therefore, it acts as a prominent target in cancer treatment. Mcl-1 has emerged as one of the validated drug targets for anticancer drug discovery as their expression has been implicated in the pathogenesis of cancers. In this review, we have included the various inhibitors based on many heterocyclic rings such as pyrrole, pyrazole, coumarin, quinoline and indole. This manuscript incorporates the anticancer activity, structure activity relationship (SAR) and molecular modelling of recently synthesized Mcl-1 inhibitors. The clinical trial status of Mcl-1 inhibitors is also described. But till now, no Mcl-1 inhibitor has been approved by any drug authority. This review is based on extensive research in the field of designing Mcl-1 inhibitors from 2020 to till now. It will provide extensive information to researchers and scientists for designing of novel Mcl-1 inhibitors.

Overview

  • The study aims to provide an overview of the recent advancements in designing Mcl-1 inhibitors and their potential in cancer treatment.

Comparative Analysis & Findings

  • Despite these advancements, no Mcl-1 inhibitor has been approved by any drug authority, highlighting the need for further research in this area.

Implications and Future Directions

  • Translation of these inhibitors into clinical trials will be crucial in evaluating their potential as anticancer agents.