Myeloid cell leukemia 1 (MCL-1): Structural characteristics and application in cancer therapy

Int J Biol Macromol. 2021 Sep 30:187:999-1018. doi: 10.1016/j.ijbiomac.2021.07.166. Epub 2021 Jul 30.

Abstract

Apoptosis, a major hallmark of cancer cells, regulates cellular fate and homeostasis. BCL-2 (B-cell CLL/Lymphoma 2) protein family is popularly known to mediate the intrinsic mode of apoptosis, of which MCL-1 is a crucial member. Myeloid cell leukemia 1 (MCL-1) is an anti-apoptotic oncoprotein and one of the most investigated members of the BCL-2 family. It is commonly known to be genetically altered, aberrantly overexpressed, and primarily associated with drug resistance in various human cancers. Recent advancements in the development of selective MCL-1 inhibitors and evaluating their effectiveness in cancer treatment establish its popularity as a molecular target. The overall aim is the selective induction of apoptosis in cancer cells by using a single or combination of BCL-2 family inhibitors. Delineating the precise molecular mechanisms associated with MCL-1-mediated cancer progression will certainly improve the efficacy of clinical interventions aimed at MCL-1 and hence patient survival. This review is structured to highlight the structural characteristics of MCL-1, its specific interactions with NOXA, MCL-1-regulatory microRNAs, and at the same time focus on the emerging therapeutic strategies targeting our protein of interest (MCL-1), alone or in combination with other treatments.

Keywords: Apoptosis; BCL-2; BH3 groove; BH3 mimetics; Cancer; Inhibitors; MCL-1; microRNA.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / therapeutic use*
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Apoptosis / drug effects*
  • Drug Resistance, Neoplasm
  • Humans
  • MicroRNAs / genetics
  • MicroRNAs / metabolism
  • Molecular Targeted Therapy
  • Myeloid Cell Leukemia Sequence 1 Protein / antagonists & inhibitors*
  • Myeloid Cell Leukemia Sequence 1 Protein / genetics
  • Myeloid Cell Leukemia Sequence 1 Protein / metabolism
  • Neoplasms / drug therapy*
  • Neoplasms / genetics
  • Neoplasms / metabolism
  • Neoplasms / pathology
  • Proteolysis
  • Proto-Oncogene Proteins c-bcl-2 / metabolism
  • Signal Transduction

Substances

  • Antineoplastic Agents
  • MCL1 protein, human
  • MicroRNAs
  • Myeloid Cell Leukemia Sequence 1 Protein
  • PMAIP1 protein, human
  • Proto-Oncogene Proteins c-bcl-2