Pyruvate kinase modulators as a therapy target: an updated patent review 2018-2023

Area of Science:

• Biochemistry
• Molecular Biology
• Oncology

Background:

• Cancer cells exhibit altered metabolism, favoring glycolysis for energy.
• Pyruvate kinase M2 (PKM2) is a key regulator in cancer metabolic reprogramming and is overexpressed in various cancers.
• PKM2 dimerization generates precursors essential for cancer cell growth and proliferation.

Purpose of the Study:

• To review recent patents (2018-2023) on PKM2 activators and inhibitors.
• To analyze the biological and synthesis properties of these compounds.
• To identify novel therapeutic strategies targeting PKM2 in cancer.

Main Methods:

• Advanced search of the European Patent Office (EPO) database.
• Literature search using PubMed, Google Scholar, and Elsevier.
• Classification of PKM2 modulators based on chemical structures.

Main Results:

• PKM2 activators and inhibitors are diverse, including pyrazole, phenol, and benzoxazine derivatives.
• These compounds demonstrate potential in treating various cancer types.
• Activating PKM2 can reduce cell proliferation by limiting essential biomolecules for cell formation.

Conclusions:

• PKM2 plays a critical role in cancer metabolism and proliferation.
• Developing potent and selective PKM2 activators and inhibitors is crucial for effective cancer therapy.
• Recent patents reveal promising chemical scaffolds for PKM2-targeted drug discovery.