Professor Ian Gilbert FRSC
I am a medicinal chemist and my research interests are in the design and synthesis of potential drugs. The mainstay of my work is synthetic medicinal chemistry as part of the Drug Discovery Unit (DDU). Where possible we make extensive use of molecular modeling to guide our synthetic efforts. I have a particular interests in the following aspects of drug discovery:
Neglected diseases such as human African trypanosomiasis, leishmaniasis and malaria.
Chemical validation of drug targets, including novel targets for which there is little or no precedence for drug discovery.
Novel approaches to and paradigms for drug discovery.
Mode of action studies and target identification.
I am Head of Chemistry in the DDU. Our main focuses are on neglected diseases and novel drug targets. The neglected diseases we are tackling are malaria, tuberculosis and the kinetoplastid diseases. We use both target-based approaches and phenotypic approaches (whole parasite screening). We have had particular success in validating the enzyme N-myristoyltransferase as a drug target in human African trypanosomiasis, and in identifying and optimising phenotypic hits. In our novel targets area, we aim to validate novel areas of biology as potential drug targets.
- From on-target to off-target activity: identification and optimisation of Trypanosoma brucei GSK3 inhibitors and their characterisation as anti-Trypanosoma brucei drug discovery lead molecules. Woodland, A.; Grimaldi, R.; Luksch, T.; Cleghorn, L. A.; Ojo, K. K.; Van Voorhis, W. C.; Brenk, R. Frearson, J. A.; Gilbert, I. H.; Wyatt, P. G. ChemMedChem, 2013, 8, 1127-1137.
- Discovery and structure-activity relationships of pyrrolone antimalarials. Murugesan, D.; Mital, A.; Kaiser, M.; Shackleford, D. M.; Morizzi, J.; Katneni, K.; Campbell, M.; Hudson, A.; Charman, S. A.; Yeates, C.; Gilbert, I. H. J. Med. Chem., 2013, 56, 2975-2990.
- Synthesis and Evaluation of α-Thymidine Analogues as Novel Antimalarials. Cui, H.; Carrero-Lérida, J.; Silva, A. P.; Whittingham, J. L.; Brannigan, J. A.; Ruiz-Pérez, L. M.; Read, K. D.; Wilson, K. S.; González-Pacanowska, D.; Gilbert, I. H. J. Med. Chem., 2012, 55, 10948-10957.
- Automated design of ligands to polypharmacological profiles. Besnard, J.; Ruda, G. F.; Setola, V.; Abecassis, K.; Rodriguiz, R. M.; Huang, X. P.; Norval, S.; Sassano, M. F.; Shin, A. I.; Webster, L. A.; Simeons, F. R.; Stojanovski, L.; Prat, A.; Seidah, N. G.; Constam, D. B.; Bickerton, G. R.; Read, K. D.; Wetsel, W. C.; Gilbert, I. H.; Roth, B. L.; Hopkins, A. L. Nature, 2012, 492, 215-220.
- Design, Synthesis and Biological Evaluation of Trypanosoma brucei Trypanothione Synthetase Inhibitors. Spinks, D.; Torrie, L. S.; Thompson, S.; Harrison, J. R.; Frearson, J. A.; Read, K. D.; Fairlamb, A. H.; Wyatt, P. G.; Gilbert, I. H. ChemMedChem, 2012, 7, 95-106.
- Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors. Brand, S.; Cleghorn, L. A. T.; McElroy, S. P.; Robinson, D. A.; Smith, V. C.; Hallyburton, I.; Harrison, J. R.; Norcross, N. R.; Norval, S.; Spinks, S.; Stojanovski, L.; Torrie, L. S.; Frearson, J. A.; Brenk, R.; Fairlamb, A. H.; Ferguson, M. A. J.; Read, K. D.; Wyatt, P. G.; Gilbert, I. H. J. Med. Chem. 2012, 55, 140-152.