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 | 169 | 2016 |
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 | 58 | 2022 |
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 | 46 | 2018 |
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 | 34 | 2017 |
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 | 26 | 2022 |
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 | 22 | 2021 |
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 | 22 | 2016 |
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 | 19 | 2017 |
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 | 11 | 2022 |
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 | 11 | 2016 |
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 | 9 | 2022 |
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 | 7 | 2019 |
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 | 7 | 2019 |
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 | 6 | 2022 |
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 | 3 | 2021 |
Targeting LRRK2 Mutations in Parkinson's Disease RK Leśniak, RJ Nichols, M Smith, TJ Montine Future Medicinal Chemistry 14 (16), 1167-1170, 2022 | 1 | 2022 |
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 | 1 | 2021 |
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 |