2. Academic Validation
  3. Comprehensive Insights that Targeting PIM for Cancer Therapy: Prospects and Obstacles

Comprehensive Insights that Targeting PIM for Cancer Therapy: Prospects and Obstacles

  • J Med Chem. 2024 Jan 11;67(1):38-64. doi: 10.1021/acs.jmedchem.3c01802.
Li Chen 1 2 3,  Wuyu Mao 1,  Changyu Ren 4,  Jinqi Li 2 3,  Jifa Zhang 1
Affiliations

Affiliations

  • 1 Department of Neurology, Joint Research Institution of Altitude Health and Institute of Respiratory Health and National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China.
  • 2 Department of Pharmacy, Sichuan Academy of Medical Sciences & Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu 610072, Sichuan, China.
  • 3 Personalized Drug Therapy Key Laboratory of Sichuan Province, School of Medicine, University of Electronic Science and Technology of China, Chengdu 610072, Sichuan, China.
  • 4 Department of Pharmacy, Chengdu Fifth People's Hospital, Chengdu 611130, Sichuan, China.
PMID: 38164076 DOI: 10.1021/acs.jmedchem.3c01802
Abstract

Proviral integration sitea for Moloney-murine leukemia virus (Pim) kinases are a family of highly conserved serine/tyrosine kinases consisting of three members, PIM-1, PIM-2, and PIM-3. These kinases regulate a wide range of substrates through phosphorylation and affect key cellular processes such as transcription, translation, proliferation, Apoptosis, and energy metabolism. Several Pim inhibitors are currently undergoing clinical trials, such as a phase I clinical trial of Uzanserti (5) for the treatment of relapsed diffuse large B-cell lymphoma that has been completed. The current focus encompasses the structural and biological characterization of Pim, ongoing research progress on small-molecule inhibitors undergoing clinical trials, and evaluation analysis of persisting challenges in this field. Additionally, the design and discovery of small-molecule inhibitors targeting Pim in recent years have been explored, with a particular emphasis on medicinal chemistry, aiming to provide valuable insights for the future development of Pim inhibitors.

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