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Tumor pyruvate kinase M2 modulators: a comprehensive account of activators and inhibitors as anticancer agents

Bhagyashri Rathod1, Shivam Chak1, Sagarkumar Patel1

  • 1Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research Ahmedabad Opposite Air Force Station Gandhinagar Gujarat 382355 India amit@niperahm.ac.in.

RSC Medicinal Chemistry
|August 6, 2021
PubMed

Insights

Pyruvate kinase M2 (PKM2) is crucial for cancer cell metabolism and survival. This review details PKM2 modulators, assays, and strategies for developing new cancer therapies targeting this key enzyme.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Pyruvate kinase M2 (PKM2) is a key enzyme in glycolysis.
  • PKM2 is implicated in the metabolic reprogramming essential for cancer cell proliferation, survival, and apoptosis evasion.
  • Its prevalence in human tumors makes PKM2 a significant therapeutic target.

Purpose of the Study:

  • To provide a comprehensive review of PKM2 modulators.
  • To discuss assays used for evaluating PKM2 modulator potential.
  • To identify gaps in current modulator knowledge and propose strategies for PKM2-targeted anticancer drug development.

Main Methods:

  • Literature review of PKM2 modulators and associated assays.
  • Analysis of PKM2 enzyme states (tense (T) and relaxed (R)) in relation to modulator activity.
  • Synthesis of information on existing PKM2 modulators and therapeutic strategies.

Main Results:

  • Summarized known activators and inhibitors of PKM2.
  • Detailed various assays employed to assess PKM2 modulator efficacy.
  • Highlighted the importance of PKM2 conformational states (T and R) in modulator interactions.
  • Identified limitations in current PKM2 modulators.

Conclusions:

  • PKM2 is a promising target for anticancer drug development.
  • Further research into PKM2 modulators and their mechanisms is needed.
  • Developing effective PKM2-targeted therapies requires addressing current lacunae in modulator knowledge and application.

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