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MCL-1 inhibition in cancer treatment

Weiguo Xiang1, Chao-Yie Yang1,2, Longchuan Bai1,2

  • 1Department of Internal Medicine, University of Michigan Medical School, lbai@umich.edu.

Oncotargets and Therapy
|November 15, 2018
PubMed

Insights

Small-molecule inhibitors targeting myeloid cell leukemia-1 (MCL-1), an antiapoptotic protein, show promise for cancer therapy. Recent advancements have led to selective MCL-1 inhibitors entering clinical trials for treating various cancers.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Myeloid cell leukemia-1 (MCL-1) is an antiapoptotic protein crucial for mitochondrial homeostasis.
  • Overexpression of MCL-1 is common in human cancers, including drug-resistant types, making it a key therapeutic target.

Purpose of the Study:

  • To review recent advancements in the development of small-molecule inhibitors targeting MCL-1.
  • To highlight the therapeutic potential of MCL-1 inhibition in cancer treatment.

Main Methods:

  • Literature review of recent studies on small-molecule MCL-1 inhibitors.
  • Analysis of progress in preclinical and clinical development of these inhibitors.

Main Results:

  • Significant progress has been made in developing selective small-molecule MCL-1 inhibitors.
  • Three MCL-1 selective inhibitors have advanced to clinical trials, indicating therapeutic promise.

Conclusions:

  • Small-molecule MCL-1 inhibitors represent a promising strategy for cancer therapy.
  • Targeting MCL-1 offers a potential approach to overcome drug resistance in cancer treatment.
Keywords:
BAKBAXBCL-2BH3 mimeticsapoptosis

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