Ikuti
Robert K Leśniak
Robert K Leśniak
Medicinal Chemist, Chemistry Team Lead, ARUK UCL DDI
Email yang diverifikasi di ucl.ac.uk
Judul
Dikutip oleh
Dikutip oleh
Tahun
Discovery and characterization of GSK2801, a selective chemical probe for the bromodomains BAZ2A and BAZ2B
P Chen, A Chaikuad, P Bamborough, M Bantscheff, C Bountra, C Chung, ...
Journal of medicinal chemistry 59 (4), 1410-1424, 2016
1692016
Imitation of β-lactam binding enables broad-spectrum metallo-β-lactamase inhibitors
J Brem, T Panduwawala, JU Hansen, J Hewitt, E Liepins, P Donets, ...
Nature Chemistry 14 (1), 15-24, 2022
582022
The Jumonji-C oxygenase JMJD7 catalyzes (3S)-lysyl hydroxylation of TRAFAC GTPases
S Markolovic, Q Zhuang, SE Wilkins, CD Eaton, MI Abboud, MJ Katz, ...
Nature chemical biology 14 (7), 688-695, 2018
462018
Crystallographic analyses of isoquinoline complexes reveal a new mode of metallo-β-lactamase inhibition
GB Li, J Brem, R Lesniak, MI Abboud, CT Lohans, IJ Clifton, SY Yang, ...
Chemical communications 53 (43), 5806-5809, 2017
342017
Discovery of G2019S-selective leucine rich repeat protein kinase 2 inhibitors with in vivo efficacy
RK Leśniak, RJ Nichols, M Schonemann, J Zhao, CR Gajera, WL Fitch, ...
European Journal of Medicinal Chemistry 229, 114080, 2022
262022
High-Throughput Crystallography Reveals Boron-Containing Inhibitors of a Penicillin-Binding Protein with Di- and Tricovalent Binding Modes
CGD Hector Newman, Alen Krajnc, Dom Bellini, Charles J. Eyermann*, Grant A ...
Journal of Medicinal Chemistry, 2021
222021
Cation–π Interactions Contribute to Substrate Recognition in γ‐Butyrobetaine Hydroxylase Catalysis
JJAG Kamps, A Khan, H Choi, RK Lesniak, J Brem, AM Rydzik, ...
Chemistry–A European Journal 22 (4), 1270-1276, 2016
222016
Human carnitine biosynthesis proceeds via (2 S, 3 S)-3-hydroxy-N ε-trimethyllysine
RK Leśniak, S Markolovic, K Tars, CJ Schofield
Chemical Communications 53 (2), 440-442, 2017
192017
Discovery of 1H-Pyrazole Biaryl Sulfonamides as Novel G2019S-LRRK2 Kinase Inhibitors
RK Leśniak, RJ Nichols, M Schonemann, J Zhao, CR Gajera, G Lam, ...
ACS medicinal chemistry letters 13 (6), 981-988, 2022
112022
Development and application of ligand-based NMR screening assays for γ-butyrobetaine hydroxylase
A Khan, RK Leśniak, J Brem, AM Rydzik, H Choi, IKH Leung, ...
MedChemComm 7 (5), 873-880, 2016
112016
Discovery of azaspirocyclic 1H-3, 4, 5-Trisubstitued pyrazoles as novel G2019S-LRRK2 selective kinase inhibitors
RK Leśniak, RJ Nichols, M Schonemann, J Zhao, CR Gajera, G Lam, ...
European Journal of Medicinal Chemistry 242 (15), 114693, 2022
92022
Small-molecules that covalently react with a human prolyl hydroxylase–towards activity modulation and substrate capture
JT Bush, RK Leśniak, TL Yeh, R Belle, H Kramer, A Tumber, ...
Chemical Communications 55 (8), 1020-1023, 2019
72019
19 F NMR studies on γ-butyrobetaine hydroxylase provide mechanistic insights and suggest a dual inhibition mode
RK Leśniak, AM Rydzik, JJAG Kamps, A Kahn, TDW Claridge, ...
Chemical Communications 55 (98), 14717-14720, 2019
72019
Development of mutation-selective LRRK2 kinase inhibitors as precision medicine for Parkinson's disease and other diseases for which carriers are at increased risk
RK Lesniak, RJ Nichols, TJ Montine
Frontiers in Neurology, 2022
62022
Enantiomers of 2-methylglutamate and 2-methylglutamine selectively impact mouse brain metabolism and behavior
AM Wawro, CR Gajera, SA Baker, RK Leśniak, CR Fischer, NL Saw, ...
Scientific Reports 11 (1), 8138, 2021
32021
Targeting LRRK2 Mutations in Parkinson's Disease
RK Leśniak, RJ Nichols, M Smith, TJ Montine
Future Medicinal Chemistry 14 (16), 1167-1170, 2022
12022
Enantiomers of 4-aminopentanoic acid act as false GABAergic neurotransmitters and impact mouse behavior
TJM Adam M. Wawro, Chandresh R. Gajera, Steven A. Baker, Robert K. Leśniak ...
Journal of Neurochemistry, 2021
12021
Selective pyrazole lrrk2 inhibitors and methods for use thereof
RLJMRJNM Smith
WO Patent WO2023004280A1, 2023
2023
Selective indazole lrrk2 inhibitors and methods for use thereof
RLJMRJNM Smith
WO Patent WO2022271840A1, 2022
2022
¹⁹F NMR studies on γ-butyrobetaine hydroxylase provide mechanistic insights and suggest a dual inhibition mode
RK Leśniak, AM Rydzik, JJAG Kamps, A Kahn, TDW Claridge, ...
ChemComm 55 (98), 14717-14720, 2019
2019
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