Rackham, M. D., Yu, Z., Brannigan, J. A., Heal, W. P., Paape, D. , Barker, K. V., Wilkinson, A. J., Smith, D. F., Leatherbarrow, R. J. and Tate, E. W. (2015) Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase. MedChemComm, 6(10), pp. 1761-1766. (doi: 10.1039/C5MD00241A)
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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: | Articles |
|---|---|
| Status: | Published |
| Refereed: | Yes |
| Glasgow Author(s) Enlighten ID: | Paape, Dr Daniel |
| Authors: | Rackham, M. D., Yu, Z., Brannigan, J. A., Heal, W. P., Paape, D., Barker, K. V., Wilkinson, A. J., Smith, D. F., Leatherbarrow, R. J., and Tate, E. W. |
| College/School: | College of Medical Veterinary and Life Sciences > School of Infection & Immunity |
| Journal Name: | MedChemComm |
| Publisher: | Royal Society of Chemistry |
| ISSN: | 2040-2503 |
| ISSN (Online): | 2040-2511 |
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