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Updated: Nov 5, 2025

Characterize Disease-related Mutants of RAF Family Kinases by Using a Set of Practical and Feasible Methods
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Characterize Disease-related Mutants of RAF Family Kinases by Using a Set of Practical and Feasible Methods

Published on: July 17, 2019

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A structural perspective on targeting the RTK/Ras/MAP kinase pathway in cancer

David E Heppner1,2, Michael J Eck3,4

  • 1Department of Chemistry, University at Buffalo, State University of New York, Buffalo, New York, USA.

Protein Science : a Publication of the Protein Society
|May 19, 2021
PubMed

Insights

Precision oncology targets cancer-driving proteins. Structural biology advances inhibitor discovery for key signaling pathways like EGFR and RAS, opening new avenues for targeted cancer therapies.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Precision oncology aims to inhibit proteins driving cancer growth.
  • The receptor tyrosine kinase-RAS-MAPK pathway is frequently mutated in cancers.
  • Key proteins like EGFR, SHP2, RAS, BRAF, and MEK are critical targets.

Purpose of the Study:

  • To review historical and recent efforts in developing inhibitors for cancer signaling pathways.
  • To emphasize the role of structural biology in inhibitor discovery and characterization.
  • To explore how structural insights reveal new vulnerabilities for drug development.

Main Methods:

  • Review of literature on targeted cancer therapies.
  • Analysis of structure-based drug design approaches.
  • Examination of structural biology findings on protein regulation and mutations.

Main Results:

  • Significant progress has been made in developing inhibitors for the RAS-MAPK pathway.
  • Structural biology has been crucial for understanding inhibitor mechanisms and optimizing drug design.
  • New therapeutic strategies are emerging based on allosteric regulation and oncogenic mutation effects.

Conclusions:

  • Understanding protein structure and regulation is vital for advancing precision oncology.
  • Structural biology provides critical insights for discovering and characterizing novel cancer drugs.
  • Targeting key signaling nodes offers promising avenues for effective cancer treatment.
Keywords:
cancer biologydrug discoverykinasestructural biology

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