Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase

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Rackham, MD, Yu, Z, Brannigan, JA, Heal, WP, Paape, D, Barker, KV, Wilkinson, AJ, Smith, DF, Leatherbarrow, RJ and Tate, EW (2015) Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase. MedChemComm, 6 (10). pp. 1761-1766. ISSN 2040-2503

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Publisher URL: http://dx.doi.org/10.1039/c5md00241a

Abstract

N-Myristoyltransferase (NMT) is a potential drug target in Leishmania parasites. Scaffold-hopping from published inhibitors yielded the serendipitous discovery of a chemotype selective for Leishmania donovani NMT; development led to high affinity inhibitors with excellent ligand efficiency. The binding mode was characterised by crystallography and provides a structural rationale for selectivity.

Item Type:	Article
Uncontrolled Keywords:	0304 Medicinal And Biomolecular Chemistry, 0305 Organic Chemistry, 1115 Pharmacology And Pharmaceutical Sciences
Subjects:	Q Science > QD Chemistry Q Science > QR Microbiology R Medicine > RM Therapeutics. Pharmacology
Divisions:	Vice-Chancellor's Office
Publisher:	Royal Society of Chemistry
Related URLs:	http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000364153700004&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=7f77ca1697db64ccb27a8011c7ced90d
Date of acceptance:	4 August 2015
Date of first compliant Open Access:	20 June 2018
Date Deposited:	20 Jun 2018 09:05
Last Modified:	04 Sep 2021 10:23
DOI or ID number:	10.1039/c5md00241a
URI:	https://ljmu-9.eprints-hosting.org/id/eprint/8862

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