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Article

Biochemical characterization of smoothened receptor antagonists by binding kinetics against drug-resistant mutant.

European journal of pharmacology - 5 Oct 2015

Shimizu Yuji, Ishii Tsuyoshi, Ogawa Kazumasa, Sasaki Satoshi, Matsui Hideki, Nakayama Masaharu

Abstract excerpt

Hedgehog (Hh) signaling critical for development, differentiation, and cell growth is involved in several cancers, including medulloblastoma and basal cell carcinoma. Although antagonism of the smoothened receptor (SMO), which mediates Hh signaling, is an attractive therapeutic target, a drug-resistant mutation in SMO (SMO-D473H) was identified in a clinical trial of the approved drug vismodegib. TAK-441 potently...

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Source

Identifiers

PMID: 26048307
DOI: 10.1016/j.ejphar.2015.05.062

Genes

SMO

Variants

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 6 Sept 2026. Manifest publication-graph-cohort-2026-09-06.1.

Source receipt: pubmed, retrieved 6 Sept 2026.

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