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Targeting protein-protein interactions in drug discovery: Modulators approved or in clinical trials for cancer

Cristina Camps-Fajol1, Debora Cavero2, Jordi Minguillón3

  • 1Unitat Mixta de Recerca en Medicina Genòmica, Universitat Autònoma de Barcelona (UAB)-IR SANT PAU, Barcelona, Spain; Institut de Bioenginyeria de Catalunya (IBEC), Barcelona, Spain; Centro de Investigación Biomédica en Red de Enfermedades Raras, Instituto de Salud Carlos III (CIBERER, ISCIII), Madrid, Spain.

Pharmacological Research
|December 12, 2024
PubMed

Insights

Targeting protein-protein interactions (PPIs) offers new cancer drug discovery avenues. Several PPI modulators are in clinical trials, with venetoclax approved for leukemia, showing promise for complex diseases.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Protein-protein interactions (PPIs) are crucial for cellular functions like signal transduction and DNA repair.
  • Dysregulation of PPIs is linked to numerous human diseases, particularly cancer.
  • Targeting PPIs presents a significant opportunity for developing novel, highly specific therapeutics.

Purpose of the Study:

  • To review the clinical development status of drugs targeting various protein-protein interactions in cancer therapy.
  • To highlight the progress and challenges in developing PPI modulators for oncological applications.

Main Methods:

  • Review of clinical trial data for PPI-targeting anticancer drugs.
  • Analysis of advancements in genetic, proteomic, and computational approaches for PPI modulator discovery.
  • Case study of approved drugs like venetoclax.

Main Results:

  • Several PPI modulators targeting interactions such as MDM2-p53, Hsp90-CDC37, and KRAS-SOS1 have advanced into clinical trials.
  • Venetoclax, a Bcl-2 family inhibitor, is approved for treating certain leukemias.
  • Progress in discovery and optimization techniques has accelerated the development of PPI-based cancer therapies.

Conclusions:

  • Modulating protein-protein interactions is a viable and advancing strategy in cancer drug discovery.
  • The clinical success of drugs like venetoclax validates the therapeutic potential of targeting PPIs.
  • Continued research and technological advancements are expected to yield more targeted therapies for complex diseases.
Keywords:
ApprovedCancer treatmentClinical trialsModulatorsPPIProtein-protein interaction

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