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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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Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase.pdf - Published Version Available under License Creative Commons Attribution. Download (1MB) | Preview |
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 |
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| 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: | 04 Sep 2021 10:23 |
| DOI or ID number: | 10.1039/c5md00241a |
| URI: | https://researchonline.ljmu.ac.uk/id/eprint/8862 |
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