Ontology highlight
ABSTRACT:
SUBMITTER: Prota AE
PROVIDER: S-EPMC5559732 | biostudies-literature | 2017 May
REPOSITORIES: biostudies-literature
Prota Andrea E AE Bargsten Katja K Redondo-Horcajo Mariano M Smith Amos B AB Yang Chia-Ping H CH McDaid Hayley M HM Paterson Ian I Horwitz Susan B SB Fernando Díaz José J Steinmetz Michel O MO
Chembiochem : a European journal of chemical biology 20170327 10
Microtubule-stabilizing agents (MSAs) are widely used in chemotherapy. Using X-ray crystallography we elucidated the detailed binding modes of two potent MSAs, (+)-discodermolide (DDM) and the DDM-paclitaxel hybrid KS-1-199-32, in the taxane pocket of β-tubulin. The two compounds bind in a very similar hairpin conformation, as previously observed in solution. However, they stabilize the M-loop of β-tubulin differently: KS-1-199-32 induces an M-loop helical conformation that is not observed for D ...[more]