Preclinical and clinical pharmacology of Rosuvastatin, a new 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor F McTaggart, L Buckett, R Davidson, G Holdgate, A McCormick, ... The American journal of cardiology 87 (5), 28-32, 2001 | 589 | 2001 |
Epidermal growth factor receptor tyrosine kinase: investigation of catalytic mechanism, structure-based searching and discovery of a potent inhibitor WHJ Ward, PN Cook, AM Slater, DH Davies, GA Holdgate Biochemical pharmacology 48 (4), 659-666, 1994 | 341 | 1994 |
Measurements of binding thermodynamics in drug discovery GA Holdgate, WHJ Ward Drug discovery today 10 (22), 1543-1550, 2005 | 299 | 2005 |
The entropic penalty of ordered water accounts for weaker binding of the antibiotic novobiocin to a resistant mutant of DNA gyrase: a thermodynamic and crystallographic study GA Holdgate, A Tunnicliffe, WHJ Ward, SA Weston, G Rosenbrock, ... Biochemistry 36 (32), 9663-9673, 1997 | 279 | 1997 |
Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530 TP Green, M Fennell, R Whittaker, J Curwen, V Jacobs, J Allen, A Logie, ... Molecular oncology 3 (3), 248-261, 2009 | 256 | 2009 |
Kinetic and structural characteristics of the inhibition of enoyl (acyl carrier protein) reductase by triclosan WHJ Ward, GA Holdgate, S Rowsell, EG McLean, RA Pauptit, E Clayton, ... Biochemistry 38 (38), 12514-12525, 1999 | 235 | 1999 |
Biocalorimetry 2: applications of calorimetry in the biological sciences JE Ladbury, ML Doyle John Wiley & Sons, 2004 | 233 | 2004 |
Mechanistic enzymology in drug discovery: a fresh perspective GA Holdgate, TD Meek, RL Grimley Nature reviews Drug discovery 17 (2), 115-132, 2018 | 232 | 2018 |
Protein-ligand interactions: methods and applications MA Williams, T Daviter Humana Press, 2013 | 214* | 2013 |
7 Isothermal Titration Calorimetry in Drug Discovery WHJ Ward, GA Holdgate Progress in medicinal chemistry 38, 309-376, 2001 | 202 | 2001 |
Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation RA Ward, C Brassington, AL Breeze, A Caputo, S Critchlow, G Davies, ... Journal of medicinal chemistry 55 (7), 3285-3306, 2012 | 187 | 2012 |
Making cool drugs hot: isothermal titration calorimetry as a tool to study binding energetics. GA Holdgate Biotechniques 31 (1), 164-6, 168, 170 passim, 2001 | 182 | 2001 |
Potent and selective bivalent inhibitors of BET bromodomains MJ Waring, H Chen, AA Rabow, G Walker, R Bobby, S Boiko, ... Nature chemical biology 12 (12), 1097-1104, 2016 | 145 | 2016 |
Structure−Activity Studies of the Inhibition of FabI, the Enoyl Reductase from Escherichia coli, by Triclosan: Kinetic Analysis of Mutant FabIs S Sivaraman, J Zwahlen, AF Bell, L Hedstrom, PJ Tonge Biochemistry 42 (15), 4406-4413, 2003 | 145 | 2003 |
Molecular mechanism for inhibition of 3-hydroxy-3-methylglutaryl CoA (HMG-CoA) reductase by rosuvastatin GA Holdgate, WHJ Ward, F McTaggart Biochemical Society Transactions 31 (3), 528-531, 2003 | 129 | 2003 |
Methyl-thiazoles: a novel mode of inhibition with the potential to develop novel inhibitors targeting InhA in Mycobacterium tuberculosis PS Shirude, P Madhavapeddi, M Naik, K Murugan, V Shinde, ... Journal of Medicinal Chemistry 56 (21), 8533-8542, 2013 | 113 | 2013 |
Prevention of MKK6-dependent activation by binding to p38α MAP kinase JE Sullivan, GA Holdgate, D Campbell, D Timms, S Gerhardt, J Breed, ... Biochemistry 44 (50), 16475-16490, 2005 | 112 | 2005 |
Structural and dynamic insights into the energetics of activation loop rearrangement in FGFR1 kinase T Klein, N Vajpai, JJ Phillips, G Davies, GA Holdgate, C Phillips, ... Nature communications 6 (1), 7877, 2015 | 77 | 2015 |
Affinity-based, biophysical methods to detect and analyze ligand binding to recombinant proteins: matching high information content with high throughput GA Holdgate, M Anderson, F Edfeldt, S Geschwindner Journal of structural biology 172 (1), 142-157, 2010 | 72 | 2010 |
Structures of the human poly (ADP-ribose) glycohydrolase catalytic domain confirm catalytic mechanism and explain inhibition by ADP-HPD derivatives JA Tucker, N Bennett, C Brassington, ST Durant, G Hassall, G Holdgate, ... PloS one 7 (12), e50889, 2012 | 62 | 2012 |