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September 5, 2025Mini-Reviews in Organic Chemistry

KRASG12D in Cancer: Structural Insights, Signaling Pathways, and Progress in Targeted Inhibitor Design

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Authors

JZJian ZhouFZFang ZhouWZWen Zhang

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Overview

Review highlights KRASG12D's role in pancreatic, colorectal, and lung cancers, indicating advances in targeted inhibitors.

Key Points

  • Targeting KRASG12D has gained traction due to potential breakthroughs in effective inhibitors.
  • The non-covalent inhibitor MRTX1133 demonstrated significant anti-tumor activity via the Switch II pocket.
  • Innovative therapeutic approaches such as PROTAC-based degraders are explored to counteract drug resistance.
  • Challenges like selectivity and adaptive resistance continue to impede the development of KRASG12D-targeted therapies.

Cite This Study

Zhou et al. (2025) studied this question.

synapsesocial.com/papers/68c23922b210217d6477a7cehttps://doi.org/10.2174/0118756298391640250731025705
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1KRAS G12C Inhibition in Solid Tumors: Biological Breakthroughs, Clinical Evidence, and Open Challenges2025 · 5 citations
  2. 2Unveiling KRAS G12D inhibition: from molecular dynamics to therapeutic strategies2025
  3. 3Identification of KRAS mutants (G12C, G12D, and G12V) inhibitors2025
  4. 4MRTX1133 is a potent non-covalent KRAS (G12C) inhibitor with tissue-specific activity2025 · 2 citations
  5. 5Optimizing KRAS Therapeutics for Non–Small Cell Lung Cancer2025 · 3 citations