X-ray and cryo-EM structures of inhibitor-bound cytochrome bc₁ complexes for structure-based drug discovery.

ABSTRACT: Cytochrome bc₁, a dimeric multi-subunit electron-transport protein embedded in the inner mitochondrial membrane, is a major drug target for the treatment and prevention of malaria and toxoplasmosis. Structural studies of cytochrome bc₁ from mammalian homologues co-crystallized with lead compounds have underpinned structure-based drug design to develop compounds with higher potency and selectivity. However, owing to the limited amount of cytochrome bc₁ that may be available from parasites, all efforts have been focused on homologous cytochrome bc₁ complexes from mammalian species, which has resulted in the failure of some drug candidates owing to toxicity in the host. Crystallographic studies of the native parasite prot

SUBMITTER: Amporndanai K 

PROVIDER: S-EPMC5947725 | biostudies-literature | 2018 Mar

REPOSITORIES: biostudies-literature