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Pyruvate kinase activators as a therapy target: a patent review 2011-2017

Sevki Adem1, Veysel Comakli2, Naim Uzun3

  • 1a Faculty of Science, Chemistry Department , Cankiri Karatekin University , Cankiri , Turkey.

Expert Opinion on Therapeutic Patents
|October 11, 2017
PubMed
Abstract

Insights

Cancer cells alter metabolism, utilizing pyruvate kinase isoenzyme M2 (PKM2) for growth. PKM2 activators inhibit cancer cell proliferation, offering a promising therapeutic strategy for cancer treatment.

Area of Science:

  • Biochemistry
  • Oncology
  • Medicinal Chemistry

Background:

  • Cancer cells exhibit altered metabolism to support rapid growth and proliferation.
  • Pyruvate kinase isoenzyme M2 (PKM2) plays a crucial role in regulating glucose metabolism for biosynthesis in cancer cells.
  • The dimeric form of PKM2 facilitates the production of precursors for macromolecule synthesis, fueling cancer cell growth.

Purpose of the Study:

  • To review and classify pyruvate kinase isoenzyme M2 (PKM2) activators based on their synthesis and biological activities.
  • To explore the potential of PKM2 activators as anti-cancer agents.
  • To highlight the need for developing novel, potent, and selective PKM2-activating compounds.

Main Methods:

  • Literature review of publications on PKM2 activators from 2011-2017.
  • Classification of PKM2 activators based on chemical structure.
  • Analysis of synthesis routes and biological activities of identified compounds.

Main Results:

  • PKM2 activators were categorized into four main classes: sulfonamide, phenolic, carboxamide, and pyridopyrimidinone derivatives.
  • PKM2 activation was shown to inhibit cancer cell growth and proliferation.
  • The mechanism involves the reduction of essential biomolecules required for cell building.

Conclusions:

  • PKM2 activators represent a promising therapeutic strategy for various cancer types.
  • Targeting PKM2 offers a potential pathway for developing novel anti-cancer drugs.
  • Further research is essential to discover and optimize new compounds with enhanced activity and selectivity for PKM2 activation.
Keywords:
Pyruvate kinases isoenzyme M2activatorcancercarboxamidephenolic compoundsulfonamide

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