Publications by authors named "Geoffrey A Holdgate"

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Validation of ion mobility spectrometry - mass spectrometry as a screening tool to identify type II kinase inhibitors of FGFR1 kinase.
Helen S Beeston, Tobias Klein, Richard A Norman, Julie A Tucker, Malcolm Anderson, Geoffrey A Holdgate

Rapid Commun Mass Spectrom· May 2025

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High throughput application of the NanoBiT Biochemical Assay for the discovery of selective inhibitors of the interaction of PI3K-p110α with KRAS.
Mohamed Ismail, Gareth Davies, Graham Sproat, Tiziana Monteverde, Jonathan Tart, Geoffrey A Holdgate

SLAS Discov· December 2024

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Hit me with your best shot: Integrated hit discovery for the next generation of drug targets.
S Neha Ashraf, J Henry Blackwell, Geoffrey A Holdgate, Simon C C Lucas, Alisa Solovyeva

Drug Discov Today· October 2024

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Characterisation of high throughput screening outputs for small molecule degrader discovery.
Lillie E Bell, Catherine Bardelle, Martin J Packer, Johanna Kastl, Geoffrey A Holdgate

SLAS Discov· July 2024

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POLARISED views and FRETting about probe modulation assays: Learning from High Throughput Screening.
Alice Lanne, Catherine Bardelle, Gareth Davies, Antonia Turberville, Hannah Semple, Geoffrey A Holdgate

SLAS Discov· June 2024

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Screening for molecular glues - Challenges and opportunities.
Geoffrey A Holdgate, Catherine Bardelle, Sophia K Berry, Alice Lanne, Maria Emanuela Cuomo

SLAS Discov· March 2024

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A perspective on the changing landscape of HTS.
Alice Lanne, Laura E J Usselmann, Poppy Llowarch, Iacovos N Michaelides, Martin Fillmore, Geoffrey A Holdgate

Drug Discov Today· August 2023

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Thermal unfolding methods in drug discovery.
Poppy Llowarch, Laura Usselmann, Delyan Ivanov, Geoffrey A Holdgate

Biophys Rev (Melville)· June 2023

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High throughput screening of 0.5 million compounds against CRAF using Alpha CETSA.
Hannah Rowlands, Kirsten Tschapalda, Carolyn Blackett, Delyan Ivanov, Darren Plant, Geoffrey A Holdgate

SLAS Discov· April 2023

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A perspective on the discovery of enzyme activators.
Antonia Turberville, Hannah Semple, Gareth Davies, Delyan Ivanov, Geoffrey A Holdgate

SLAS Discov· December 2022

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Bromodomain Interactions with Acetylated Histone 4 Peptides in the BRD4 Tandem Domain: Effects on Domain Dynamics and Internal Flexibility.
Sven Wernersson, Romel Bobby, Liz Flavell, Alexander G Milbradt, Geoffrey A Holdgate

Biochemistry· November 2022

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Utilising acoustic mist ionisation mass spectrometry to identify redox cycling compounds in high throughput screening outputs.
Rachel Moore, Corinne Molyneux, Ian Sinclair, Geoffrey A Holdgate, Jarrod Walsh

SLAS Discov· September 2022

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Advancing automation in high-throughput screening: Modular unguarded systems enable adaptable drug discovery.
Catherine S Hansel, Darren L Plant, Geoffrey A Holdgate, Matthew J Collier, Helen Plant

Drug Discov Today· August 2022

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High-throughput detection of metal contamination in HTS outputs.
Corinne Molyneux, Ian Sinclair, Helen L Lightfoot, Jarrod Walsh, Geoffrey A Holdgate

SLAS Discov· July 2022

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Drug discovery for epigenetics targets.
Geoffrey A Holdgate, Catherine Bardelle, Alice Lanne, Jon Read, Daniel H O'Donovan

Drug Discov Today· April 2022

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Applications of Biophysics in Early Drug Discovery.
Geoffrey A Holdgate, Christian Bergsdorf

SLAS Discov· September 2021

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The Use of Acoustic Mist Ionization Mass Spectrometry for High-Throughput Screening.
Helen Plant, David Murray, Hannah Semple, Gareth Davies, Ian Sinclair, Geoffrey A Holdgate

Methods Mol Biol· June 2021

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Ligand Discovery: High-Throughput Binding: Fluorescence Polarization (Anisotropy).
Geoffrey A Holdgate, Paul E Hemsley

Methods Mol Biol· June 2021

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Small-Molecule Degraders beyond PROTACs-Challenges and Opportunities.
Johanna M Kastl, Gareth Davies, Eleanor Godsman, Geoffrey A Holdgate

SLAS Discov· April 2021

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High-Throughput Mechanism of Inhibition.
Gareth Davies, Hannah Semple, Megan McCandless, Jonathan Cairns, Geoffrey A Holdgate

SLAS Discov· February 2021

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Myc phosphorylation in its basic helix-loop-helix region destabilizes transient α-helical structures, disrupting Max and DNA binding.
Pavel Macek, Matthew J Cliff, Kevin J Embrey, Geoffrey A Holdgate, J Willem M Nissink

J Biol Chem· June 2018

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Mechanistic enzymology in drug discovery: a fresh perspective.
Geoffrey A Holdgate, Thomas D Meek, Rachel L Grimley

Nat Rev Drug Discov· February 2018

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Mechanistic enzymology in drug discovery: a fresh perspective.
Geoffrey A Holdgate, Thomas D Meek, Rachel L Grimley

Nat Rev Drug Discov· January 2018

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Structural and dynamic insights into the energetics of activation loop rearrangement in FGFR1 kinase.
Tobias Klein, Navratna Vajpai, Jonathan J Phillips, Gareth Davies, Geoffrey A Holdgate

Nat Commun· July 2015

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Discovery and characterization of MAPK-activated protein kinase-2 prevention of activation inhibitors.
John G Cumming, Judit É Debreczeni, Fredrik Edfeldt, Emma Evertsson, Martin Harrison, Geoffrey A Holdgate

J Med Chem· January 2015

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