Title : GTP-State-Selective Cyclic Peptide Ligands of K-Ras(G12D) Block Its Interaction with Raf.

Pub. Date : 2020 Oct 28

PMID : 33145412






2 Functional Relationships(s)
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1 These cyclic peptides show preferential binding to the GTP-bound state of K-Ras(G12D) over the GDP-bound state and block Ras-Raf interaction. Guanosine Diphosphate KRAS proto-oncogene, GTPase Homo sapiens
2 The union of G12D over wildtype selectivity and GTP state/GDP state selectivity is particularly desirable, considering that oncogenic K-Ras(G12D) exists predominantly in the GTP state in cancer cells, and wildtype K-Ras signaling is important for the maintenance of healthy cells. Guanosine Diphosphate KRAS proto-oncogene, GTPase Homo sapiens