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Article

Small molecule antagonists in distinct binding modes inhibit drug-resistant mutant of smoothened.

Chemistry & biology - 22 Apr 2011

Tao Haiyan, Jin Qihui, Koo Dong-In, Liao Xuebin, Englund Nathan P, Wang Yan, Ramamurthy Arun, Schultz Peter G, Dorsch Marion, Kelleher Joseph, Wu Xu

Abstract excerpt

Several small molecule antagonists for Smoothened (Smo) have been developed, and achieved promising preclinical efficacy in cancers that are dependent on Hedgehog (Hh) signaling. However, in a recent clinical study, a drug-resistant D473H SMO mutant was identified that is thought to be responsible for cancer relapse in a patient with medulloblastoma. Here, we report two Smo antagonists that bind to distinct...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Drug Resistance, Neoplasm

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Source

Identifiers

PMID: 21513879
DOI: 10.1016/j.chembiol.2011.01.018

Genes

SMO

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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