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Covalent KRAS inhibition

Covalent KRAS inhibition

A drug strategy that forms a covalent bond with a mutant cysteine in KRAS G12C to inhibit selected KRAS states.

Overview

EXPLORE BY LEVEL

Some KRAS G12C medicines form a lasting chemical bond with the changed cysteine. This can hold the switch in a less active state and reduce signaling.

Quick Facts

AT A GLANCE
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Follow the Connections

See how Covalent KRAS inhibition links to other biological records.

Open network
VariantKRAS G12CtargetsProcessAcquired Drug resistancecan limit
All 2 Structured Connections
Covalent KRAS inhibition · ProcessTARGETS →KRAS G12C · Variant
Acquired Drug resistance · ProcessCAN LIMIT →Covalent KRAS inhibition · Process

Recommended Reading

Trusted references for learning more about Covalent KRAS inhibition.

reviewTargeting small GTPases: emerging grasps on previously untamable targets, pioneered by KRASPubMed · PMID 37221195 articleMEK inhibitor and anti-EGFR antibody overcome sotorasib resistance signals and enhance its antitumor effect in colorectal cancer cellsPubMed · PMID 37336286
Research Claims

Covalent engagement provides allele-selective chemistry but does not guarantee complete pathway suppression. Adaptive feedback, nucleotide-state exchange, secondary mutations, and tumor context influence response.