Holdgate GA
Holdgate GA
Senior Principal Scientist, AstraZeneca
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Cited by
Cited by
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
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
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
Measurements of binding thermodynamics in drug discovery
GA Holdgate, WHJ Ward
Drug discovery today 10 (22), 1543-1550, 2005
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
Biocalorimetry 2: applications of calorimetry in the biological sciences
JE Ladbury, ML Doyle
John Wiley & Sons, 2004
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
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
7 Isothermal Titration Calorimetry in Drug Discovery
WHJ Ward, GA Holdgate
Progress in medicinal chemistry 38, 309-376, 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
Protein-ligand interactions
M Williams, T Daviter
Springer, 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
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
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
Mechanistic enzymology in drug discovery: a fresh perspective
GA Holdgate, TD Meek, RL Grimley
Nature reviews Drug discovery 17 (2), 115-132, 2018
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
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
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
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
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), 1-12, 2015
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