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Updated: Dec 12, 2025

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
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Myeloid cell leukemin-1 inhibitors: a growing arsenal for cancer therapy

Peng-Ju Zhu1, Ze-Zhou Yu1, Qi-Dong You2

  • 1State Key Laboratory of Natural Medicines and Jiang Su Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.

Drug Discovery Today
|August 11, 2020
PubMed

Insights

Myeloid cell leukemia-1 (Mcl-1) is a key apoptosis regulator often overexpressed in cancers. Mcl-1 inhibitors are emerging as a promising therapeutic strategy for cancer treatment.

Area of Science:

  • Molecular Biology
  • Cancer Biology
  • Biochemistry

Background:

  • The B-cell lymphoma-2 (Bcl-2) protein family regulates apoptosis.
  • Myeloid cell leukemia-1 (Mcl-1) is an antiapoptotic protein frequently overexpressed in various cancers.
  • Mcl-1 overexpression is linked to oncogenesis and poor prognosis, hindering cancer therapy.

Purpose of the Study:

  • To review the role of Mcl-1 in apoptosis.
  • To highlight recent advancements in the development of Mcl-1-selective small-molecule inhibitors.

Main Methods:

  • Literature review of Mcl-1 function and inhibitor development.
  • Analysis of preclinical and clinical trial data for Mcl-1 inhibitors.

Main Results:

  • Mcl-1's role as a critical apoptosis inhibitor in cancer is confirmed.
  • Numerous Mcl-1-selective small-molecule inhibitors have shown promise in preclinical and clinical studies.

Conclusions:

  • Mcl-1 is a significant therapeutic target in oncology.
  • The development of Mcl-1 inhibitors represents a promising avenue for overcoming therapeutic resistance in cancer.

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