Nature Communications (Sep 2020)

Structural bases of IMiD selectivity that emerges by 5-hydroxythalidomide

  • Hirotake Furihata,
  • Satoshi Yamanaka,
  • Toshiaki Honda,
  • Yumiko Miyauchi,
  • Atsuko Asano,
  • Norio Shibata,
  • Masaru Tanokura,
  • Tatsuya Sawasaki,
  • Takuya Miyakawa

DOI
https://doi.org/10.1038/s41467-020-18488-4
Journal volume & issue
Vol. 11, no. 1
pp. 1 – 11

Abstract

Read online

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.