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Updated: Sep 28, 2025

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
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Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries

Published on: January 22, 2019

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Topical advances in PIM kinases and their inhibitors: Medicinal chemistry perspectives

Vinayak Walhekar1, Chandrakant Bagul1, Dileep Kumar1

  • 1Department of Pharmaceutical Chemistry, BVDU'S Poona College of Pharmacy, Erandwane, Pune 411038, Maharashtra, India.

Biochimica Et Biophysica Acta. Reviews on Cancer
|April 3, 2022
PubMed

Insights

PIM kinases are crucial for cancer development and are promising anticancer targets. This review covers PIM kinase biology, structure, and inhibitors, highlighting their potential despite clinical trial challenges.

Area of Science:

  • Biochemistry and Molecular Biology
  • Medicinal Chemistry
  • Oncology

Background:

  • Cytosolic PIM kinases, a serine/threonine kinase family, are implicated in cancer progression.
  • Overexpression of PIM kinases is prevalent in various cancers, including prostate, hematological, and breast carcinoma.
  • PIM kinases represent a significant therapeutic target due to the lack of approved drugs.

Purpose of the Study:

  • To provide a comprehensive review of PIM kinases.
  • To cover the biological and structural aspects of PIM kinases.
  • To discuss the medicinal chemistry of recently developed PIM inhibitors.

Main Methods:

  • Literature review of biological and structural data on PIM kinases.
  • Analysis of medicinal chemistry efforts in developing PIM kinase inhibitors.
  • Examination of clinical trial data for PIM kinase inhibitors.

Main Results:

  • PIM kinases play a vital role in cancer cell proliferation and survival.
  • Numerous PIM kinase inhibitors have been synthesized and evaluated.
  • Despite promising preclinical data, many PIM inhibitors have failed to advance through clinical trials.

Conclusions:

  • PIM kinases remain attractive targets for novel anticancer drug discovery.
  • Understanding PIM kinase biology and structure is key to designing effective inhibitors.
  • Further medicinal chemistry optimization is needed to overcome clinical trial attrition.
Keywords:
ATP competitiveApoptosisMutationPIM kinaseProstate cancerSerine-threonine kinase

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