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Related Concept Videos

The Ras Gene02:38

The Ras Gene

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The Ras-gene-encoded proteins are regulators of signaling pathways controlling cell proliferation, differentiation, or cell survival. The Ras-gene family in humans constitutes three primary members—the HRas, NRas, and KRas. These genes code for four functionally distinct yet closely related proteins—the HRas, NRas, KRas4A, and KRas4B. The involvement of mutant Ras genes in human cancer was first discovered in 1982 and is among the most common causes of human tumorigenesis.
Ras is a...
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Spatiotemporally Controlled Nuclear Translocation of Guests in Living Cells Using Caged Molecular Glues as Photoactivatable Tags10:10

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This protocol describes light-triggered nuclear translocation of guests in living cells using caged molecular glue tags. This method is promising for site-selective nuclear-targeting drug...
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Small GTPases - Ras and Rho01:24

Small GTPases - Ras and Rho

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Ras and Rho are small monomeric GTPases that act downstream of receptor tyrosine kinase (RTK) and regulate various cellular processes. These GTPases switch between active and inactive states by binding to guanine nucleotides.
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Modeling an Enzyme Active Site using Molecular Visualization Freeware

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A key skill in biomolecular modeling is displaying and annotating active sites in proteins. This technique is demonstrated using four popular free programs for macromolecular visualization: iCn3D, Jmol, PyMOL, and UCSF...
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Related Experiment Video

Updated: Jan 20, 2026

Spatiotemporally Controlled Nuclear Translocation of Guests in Living Cells Using Caged Molecular Glues as Photoactivatable Tags
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Spatiotemporally Controlled Nuclear Translocation of Guests in Living Cells Using Caged Molecular Glues as Photoactivatable Tags

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Targeting active RAS with molecular glue.

Wenjing Su1, Xuben Hou2

  • 1The Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, Zhejiang, 310058, China.

Pharmaceutical Science Advances
|January 19, 2026
PubMed
Summary
This summary is machine-generated.

New tri-complex inhibitors targeting KRASG12C mutations show superior preclinical efficacy compared to existing therapies. These advancements offer a promising paradigm shift in RAS-targeted cancer treatment, potentially leading to more durable patient benefits.

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Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Activating RAS gene mutations, particularly KRASG12C, are common in many cancers and historically difficult to target therapeutically.
  • The development of KRASG12C allosteric inhibitors (sotorasib, adagrasib) represented a significant advance, but limitations in response depth and duration necessitate further innovation.

Purpose of the Study:

  • To explore novel therapeutic strategies for cancers driven by RAS mutations.
  • To evaluate the preclinical efficacy of new tri-complex inhibitors targeting activated RAS variants.

Main Methods:

  • Preclinical evaluation of novel tri-complex inhibitors (RMC-7977, RMC-6236).
  • Comparative efficacy studies against existing KRASG12C inhibitors like adagrasib.

Main Results:

  • The novel tri-complex inhibitors demonstrated promising preclinical efficacy.
  • These new agents showed superior performance compared to adagrasib in preclinical models.

Conclusions:

  • Tri-complex inhibitors represent a significant advancement in RAS-targeted cancer therapy.
  • These findings suggest a potential paradigm shift in RAS oncology, offering improved therapeutic benefits.
  • Further clinical investigation of these novel inhibitors is warranted.