Ontology highlight
ABSTRACT:
SUBMITTER: Ojo KK
PROVIDER: S-EPMC2896873 | biostudies-literature | 2010 May
REPOSITORIES: biostudies-literature
Nature structural & molecular biology 20100502 5
New drugs are needed to treat toxoplasmosis. Toxoplasma gondii calcium-dependent protein kinases (TgCDPKs) are attractive targets because they are absent in mammals. We show that TgCDPK1 is inhibited by low nanomolar levels of bumped kinase inhibitors (BKIs), compounds inactive against mammalian kinases. Cocrystal structures of TgCDPK1 with BKIs confirm that the structural basis for selectivity is due to the unique glycine gatekeeper residue in the ATP-binding site. We show that BKIs interfere w ...[more]