Structural bases of IMiD selectivity that emerges by 5-hydroxythalidomide

5-hydroxythalidomide is a primary thalidomide metabolite generated by the cytochrome P450 isozymes. The reported data, including crystal structure of the 5-hydroxythalidomide-mediated complex of CRBN with SALL4, elucidate how additional hydroxy group of the metabolite enhances the interaction of CRB...

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Auteurs principaux: Hirotake Furihata, Satoshi Yamanaka, Toshiaki Honda, Yumiko Miyauchi, Atsuko Asano, Norio Shibata, Masaru Tanokura, Tatsuya Sawasaki, Takuya Miyakawa
Format: article
Langue:EN
Publié: Nature Portfolio 2020
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Accès en ligne:https://doaj.org/article/e6839866ce1b4a9fbf178c9bea0007d2
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Résumé:5-hydroxythalidomide is a primary thalidomide metabolite generated by the cytochrome P450 isozymes. The reported data, including crystal structure of the 5-hydroxythalidomide-mediated complex of CRBN with SALL4, elucidate how additional hydroxy group of the metabolite enhances the interaction of CRBN with the neosubstrate SALL4.