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Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase

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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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:
Date Deposited: 20 Jun 2018 09:05
Last Modified: 20 Jun 2018 09:05
DOI or Identification number: 10.1039/c5md00241a
URI: http://researchonline.ljmu.ac.uk/id/eprint/8862

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