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Small molecule antagonists in distinct binding modes inhibit drug-resistant mutant of smoothened
Authors: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
Institution:Genomics Institute of the Novartis Research Foundation, San Diego, CA 92121, USA.
Abstract:
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  • Highlights? New small molecule antagonists of Smo with distinct binding modes discovered from high throughput screens ? ALLO-1 and ALLO-2 are potent against the drug-resistant mutant of Smo ? ALLO-1 is potent against oncogenic mutant of Smo (SmoM2)
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