Diverse modes of binding in structures of Leishmania major N-myristoyltransferase with selective inhibitors.

ABSTRACT: The leishmaniases are a spectrum of global diseases of poverty associated with immune dysfunction and are the cause of high morbidity. Despite the long history of these diseases, no effective vaccine is available and the currently used drugs are variously compromised by moderate efficacy, complex side effects and the emergence of resistance. It is therefore widely accepted that new therapies are needed. N-Myristoyltransferase (NMT) has been validated pre-clinically as a target for the treatment of fungal and parasitic infections. In a previously reported high-throughput screening program, a number of hit compounds with activity against NMT from Leishmania donovani have been identified. Here, high-resolution crystal structures of representative compounds from four hit series in ternary comp

SUBMITTER: Brannigan JA 

PROVIDER: S-EPMC4107925 | biostudies-literature | 2014 Jul

REPOSITORIES: biostudies-literature