Design, synthesis and biological evaluation of a novel non-Gemini analog of UVB1 and crystal structure of its complex with the vitamin D receptor.

Fiche publication

Date publication

février 2025

Journal

Bioorganic chemistry

Auteurs

Membres identifiés du Cancéropôle Est :
Dr ROCHEL-GUIBERTEAU Natacha

Tous les auteurs :
Gómez-Bouzó U, Peluso-Iltis C, Santalla H, Verlinden L, Verstuyf A, Rochel N, Gómez G, Fall Y

Lien Pubmed

https://www.ncbi.nlm.nih.gov/pubmed/39938446

Résumé

We synthesized UG-650, a novel non-Gemini analog of UVB1 that combines structural features of UVB1 and MC 1288. The evaluation of the bioactivities indicates that UG-650 dose-dependently inhibited MCF-7 cell proliferation. In comparison to calcitriol, slightly lower concentrations of UG-650 were needed to achieve equivalent levels of proliferation inhibition. Structural analysis revealed that the analog forms additional interactions stabilizing VDR active form.