The oncometabolite 2‐hydroxyglutarate inhibits histone lysine demethylases R Chowdhury, KK Yeoh, YM Tian, L Hillringhaus, EA Bagg, NR Rose, ... EMBO reports 12 (5), 463-469, 2011 | 1111 | 2011 |
Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials TL Yeh, TM Leissing, MI Abboud, CC Thinnes, O Atasoylu, JP Holt-Martyn, ... Chemical science 8 (11), 7651-7668, 2017 | 202 | 2017 |
Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases NR Rose, ECY Woon, A Tumber, LJ Walport, R Chowdhury, XS Li, ... Journal of medicinal chemistry 55 (14), 6639-6643, 2012 | 159 | 2012 |
Structural basis for oxygen degradation domain selectivity of the HIF prolyl hydroxylases R Chowdhury, IKH Leung, YM Tian, MI Abboud, W Ge, C Domene, ... Nature communications 7 (1), 12673, 2016 | 128 | 2016 |
Structural and mechanistic studies on γ-butyrobetaine hydroxylase IKH Leung, TJ Krojer, GT Kochan, L Henry, F von Delft, TDW Claridge, ... Chemistry & biology 17 (12), 1316-1324, 2010 | 101 | 2010 |
Dynamic combinatorial chemistry employing boronic acids/boronate esters leads to potent oxygenase inhibitors M Demetriades, IKH Leung, R Chowdhury, MC Chan, MA McDonough, ... Angewandte Chemie International Edition 51 (27), 6672-6675, 2012 | 96 | 2012 |
Non-enzymatic chemistry enables 2-hydroxyglutarate-mediated activation of 2-oxoglutarate oxygenases H Tarhonskaya, AM Rydzik, IKH Leung, ND Loik, MC Chan, A Kawamura, ... Nature communications 5 (1), 3423, 2014 | 83 | 2014 |
Potent and selective triazole-based inhibitors of the hypoxia-inducible factor prolyl-hydroxylases with activity in the murine brain MC Chan, O Atasoylu, E Hodson, A Tumber, IKH Leung, R Chowdhury, ... PLoS One 10 (7), e0132004, 2015 | 68 | 2015 |
Human oxygen sensing may have origins in prokaryotic elongation factor Tu prolyl-hydroxylation JS Scotti, IKH Leung, W Ge, MA Bentley, J Paps, HB Kramer, J Lee, ... Proceedings of the National Academy of Sciences 111 (37), 13331-13336, 2014 | 68 | 2014 |
Reporter ligand NMR screening method for 2-oxoglutarate oxygenase inhibitors IKH Leung, M Demetriades, AP Hardy, C Lejeune, TJ Smart, ... Journal of medicinal chemistry 56 (2), 547-555, 2013 | 68 | 2013 |
Novel tyrosyl-DNA phosphodiesterase 1 inhibitors enhance the therapeutic impact of topoteсan on in vivo tumor models AL Zakharenko, OA Luzina, DN Sokolov, VI Kaledin, VP Nikolin, ... European Journal of Medicinal Chemistry 161, 581-593, 2019 | 67 | 2019 |
MCR-1: a promising target for structure-based design of inhibitors to tackle polymyxin resistance SJ Son, R Huang, CJ Squire, IKH Leung Drug Discovery Today 24 (1), 206-216, 2019 | 65 | 2019 |
A photoreactive small-molecule probe for 2-oxoglutarate oxygenases D Rotili, M Altun, A Kawamura, A Wolf, R Fischer, IKH Leung, ... Chemistry & biology 18 (5), 642-654, 2011 | 65 | 2011 |
Protein-directed dynamic combinatorial chemistry: a guide to protein ligand and inhibitor discovery R Huang, IKH Leung Molecules 21 (7), 910, 2016 | 55 | 2016 |
Protein-ligand binding affinity determination by the waterLOGSY method: an optimised approach considering ligand rebinding R Huang, A Bonnichon, TDW Claridge, IKH Leung Scientific Reports 7 (1), 43727, 2017 | 53 | 2017 |
Investigating the contribution of the active site environment to the slow reaction of hypoxia-inducible factor prolyl hydroxylase domain 2 with oxygen H Tarhonskaya, R Chowdhury, IKH Leung, ND Loik, JSO McCullagh, ... Biochemical Journal 463 (3), 363-372, 2014 | 53 | 2014 |
Studies on deacetoxycephalosporin C synthase support a consensus mechanism for 2-oxoglutarate dependent oxygenases H Tarhonskaya, A Szöllössi, IKH Leung, JT Bush, L Henry, ... Biochemistry 53 (15), 2483-2493, 2014 | 51 | 2014 |
Diphenylacetylene‐linked peptide strands induce bidirectional β‐sheet formation H Lingard, JT Han, AL Thompson, IKH Leung, RTW Scott, S Thompson, ... Angewandte Chemie International Edition 53 (14), 3650-3653, 2014 | 51 | 2014 |
Targeting isocitrate lyase for the treatment of latent tuberculosis RP Bhusal, G Bashiri, BXC Kwai, J Sperry, IKH Leung Drug discovery today 22 (7), 1008-1016, 2017 | 50 | 2017 |
An approach to enzyme inhibition employing reversible boronate ester formation IKH Leung, T Brown Jr, CJ Schofield, TDW Claridge MedChemComm 2 (5), 390-395, 2011 | 47 | 2011 |