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Article

Investigation of the structural requirements of K-Ras(G12D) selective inhibitory peptide KRpep-2d using alanine scans and cysteine bridging.

Bioorganic & medicinal chemistry letters - 15 Jun 2017

Niida Ayumu, Sasaki Shigekazu, Yonemori Kazuko, Sameshima Tomoya, Yaguchi Masahiro, Asami Taiji, Sakamoto Kotaro, Kamaura Masahiro

Abstract excerpt

A structure-activity relationship study of a K-Ras(G12D) selective inhibitory cyclic peptide, KRpep-2d was performed. Alanine scanning of KRpep-2d focusing on the cyclic moiety showed that Leu7, Ile9, and Asp12 are the key elements for K-Ras(G12D) selective inhibition of KRpep-2d. The cysteine bridging was also examined to identify the stable analog of KRpep-2d under reductive conditions. As a result, the...

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Identifiers

PMID: 28457754
DOI: 10.1016/j.bmcl.2017.04.063

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 5 Sept 2026. Manifest publication-graph-cohort-2026-09-05.1.

Source receipt: pubmed, retrieved 5 Sept 2026.

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