Related Experiment Video

Updated: Sep 22, 2025

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

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Targeting the "undruggable" RAS - new strategies - new hope?

Britta Mörchen1,2, Oleksandr Shkura3, Raphael Stoll3,4

  • 1Skin Cancer Unit of the Dermatology Department, Medical Faculty, University Duisburg-Essen, West German Cancer Center, Essen 45147, Germany.

Cancer Drug Resistance (Alhambra, Calif.)
|May 18, 2022
PubMed

Insights

Targeting KRAS mutations in cancer is challenging due to protein structure. Recent advances show promise with small molecule antagonists and understanding KRAS-mutant signaling

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Development

Background:

  • KRAS is a frequently mutated oncogene in solid tumors, regulating cell signaling pathways.
  • Activating mutations in KRAS disrupt normal cell growth, leading to cancer.
  • The shallow surface of KRAS has historically hindered small molecule drug development.

Purpose of the Study:

  • To review recent progress in developing low molecular antagonists for KRAS.
  • To explore the interaction between mutant KRAS signaling and PD-L1 induced immunosuppression.

Main Methods:

  • Literature review of recent advancements in KRAS antagonist development.
  • Analysis of studies investigating the link between mutant KRAS and PD-L1.

Main Results:

  • Recent progress has been made in developing low molecular antagonists for KRAS.
  • A newly described interaction between mutant KRAS signaling and PD-L1 induced immunosuppression has been identified.

Conclusions:

  • New therapeutic strategies targeting KRAS mutations are emerging.
  • Understanding the interplay between KRAS mutations and the immune system offers new hope for cancer treatment.
Keywords:
K-RASPD-1PD-L1immune checkpointssmall molecules

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