Projects per year
Abstract
Visceral leishmaniasis causes considerable mortality and morbidity in many parts of the world. There is an urgent need for the development of new, effective treatments for this disease. Here we describe the development of an anti-leishmanial drug-like chemical series based on a pyrazolopyrimidine scaffold. The leading compound from this series (7, DDD853651/GSK3186899) is efficacious in a mouse model of visceral leishmaniasis, has suitable physicochemical, pharmacokinetic and toxicological properties for further development, and has been declared a preclinical candidate. Detailed mode-of-action studies indicate that compounds from this series act principally by inhibiting the parasite cdc-2-related kinase 12 (CRK12), thus defining a druggable target for visceral leishmaniasis.
Original language | English |
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Pages (from-to) | 192-197 |
Number of pages | 6 |
Journal | Nature |
Volume | 560 |
Issue number | 7717 |
Early online date | 25 Jul 2018 |
DOIs | |
Publication status | Published - 9 Aug 2018 |
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Dive into the research topics of 'Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis'. Together they form a unique fingerprint.-
Protein Glycosylation in Trypanosomes: Defining and Exploiting a Biological System (Senior Investigator Award)
1/10/13 → 30/06/23
Project: Research
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Chemical Biology: Leveraging Phenotypic Hits Against Kinetoplastids (Strategic Grant)
Fairlamb, A., Field, M., Gilbert, I., Gray, D., Horn, D. & Wyatt, P.
1/01/15 → 31/12/20
Project: Research
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A Translational Engine for Biomedical Discoveries (Strategic Grant)
1/01/13 → 30/09/15
Project: Research
Profiles
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Fairlamb, Alan
- Biological Chemistry and Drug Discovery - Associate Staff & Biochemistry (Consulting)
Person: Associate Staff