A Rapid and Efficient Assay for the Characterization of Substrates and Inhibitors of Nicotinamide N-Methyltransferase MJ Van Haren, J Sastre Toraño, D Sartini, M Emanuelli, RB Parsons, ... Biochemistry 55 (37), 5307-5315, 2016 | 63 | 2016 |
Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT) with Enhanced Activity Y Gao, MJ Van Haren, EE Moret, JJM Rood, D Sartini, A Salvucci, ... Journal of medicinal chemistry 62 (14), 6597-6614, 2019 | 60 | 2019 |
Resin-Bound Sulfonyl Azides: Efficient Loading and Activation Strategy for the Preparation of the N-Acyl Sulfonamide Linker R Merkx, MJ van Haren, DTS Rijkers, RMJ Liskamp The Journal of Organic Chemistry 72 (12), 4574-4577, 2007 | 58 | 2007 |
Synthesis and evaluation of protein arginine N-methyltransferase inhibitors designed to simultaneously occupy both substrate binding sites M van Haren, LQ van Ufford, EE Moret, NI Martin Organic & biomolecular chemistry 13 (2), 549-560, 2015 | 55 | 2015 |
Inhibitors of nicotinamide N-methyltransferase designed to mimic the methylation reaction transition state MJ Van Haren, R Taig, J Kuppens, JS Toraño, EE Moret, RB Parsons, ... Organic & biomolecular chemistry 15 (31), 6656-6667, 2017 | 49 | 2017 |
Potent Inhibition of Nicotinamide N-Methyltransferase by Alkene-Linked Bisubstrate Mimics Bearing Electron Deficient Aromatics Y Gao, MJ Van Haren, N Buijs, P Innocenti, Y Zhang, D Sartini, ... Journal of Medicinal Chemistry 64 (17), 12938-12963, 2021 | 41 | 2021 |
Macrocyclic peptides as allosteric inhibitors of nicotinamide N-methyltransferase (NNMT) MJ Van Haren, Y Zhang, V Thijssen, N Buijs, Y Gao, L Mateuszuk, ... RSC Chemical Biology 2 (5), 1546-1555, 2021 | 36 | 2021 |
Structural studies of protein arginine methyltransferase 2 reveal its interactions with potential substrates and inhibitors V Cura, N Marechal, N Troffer‐Charlier, JM Strub, MJ van Haren, ... The FEBS journal 284 (1), 77-96, 2017 | 35 | 2017 |
Nicotinamide N-methyl transferase (NNMT): An emerging therapeutic target Y Gao, NI Martin, MJ van Haren Drug Discovery Today 26 (11), 2699-2706, 2021 | 32 | 2021 |
Transition state mimics are valuable mechanistic probes for structural studies with the arginine methyltransferase CARM1 MJ van Haren, N Marechal, N Troffer-Charlier, A Cianciulli, G Sbardella, ... Proceedings of the National Academy of Sciences 114 (14), 3625-3630, 2017 | 30 | 2017 |
Bioanalysis of ibrutinib, and its dihydrodiol-and glutathione cycle metabolites by liquid chromatography-tandem mass spectrometry JJM Rood, PJA Dormans, MJ Van Haren, JHM Schellens, JH Beijnen, ... Journal of Chromatography B 1090, 14-21, 2018 | 29 | 2018 |
Esterase-Sensitive Prodrugs of a Potent Bisubstrate Inhibitor of Nicotinamide N-Methyltransferase (NNMT) Display Cellular Activity MJ van Haren, Y Gao, N Buijs, R Campagna, D Sartini, M Emanuelli, ... Biomolecules 11 (9), 1357, 2021 | 27 | 2021 |
A concise preparation of the fluorescent amino acid l-(7-hydroxycoumarin-4-yl) ethylglycine and extension of its utility in solid phase peptide synthesis T Koopmans, M van Haren, LQ van Ufford, JM Beekman, NI Martin Bioorganic & medicinal chemistry 21 (2), 553-559, 2013 | 26 | 2013 |
Nicotinamide N-methyltransferase catalyses the N-methylation of the endogenous β-carboline norharman: evidence for a novel detoxification pathway MG Thomas, D Sartini, M Emanuelli, MJ van Haren, NI Martin, ... Biochemical Journal 473 (19), 3253-3267, 2016 | 23 | 2016 |
Aminocarboxylic acids related to aspergillomarasmine A (AMA) and ethylenediamine-N, N′-disuccinic acid (EDDS) are strong zinc-binders and inhibitors of the metallo-beta … KHME Tehrani, H Fu, NC Brüchle, V Mashayekhi, AP Luján, ... Chemical communications 56 (20), 3047-3049, 2020 | 22 | 2020 |
Novel cephalosporin conjugates display potent and selective inhibition of imipenemase-type metallo-β-lactamases KHME Tehrani, N Wade, V Mashayekhi, NC Brüchle, W Jespers, ... Journal of Medicinal Chemistry 64 (13), 9141-9151, 2021 | 20 | 2021 |
Cephalosporin Prodrug Inhibitors Overcome Metallo‐β‐Lactamase Driven Antibiotic Resistance MJ van Haren, KHME Tehrani, I Kotsogianni, N Wade, NC Brüchle, ... Chemistry–A European Journal 27 (11), 3806-3811, 2021 | 17 | 2021 |
Extrahepatic metabolism of ibrutinib JJM Rood, A Jamalpoor, S van Hoppe, MJ van Haren, RE Wasmann, ... Investigational New Drugs 39 (1), 1-14, 2021 | 17 | 2021 |
Small molecule carboxylates inhibit metallo-β-lactamases and resensitize carbapenem-resistant bacteria to meropenem KHME Tehrani, NC Brüchle, N Wade, V Mashayekhi, D Pesce, ... ACS Infectious Diseases 6 (6), 1366-1371, 2020 | 17 | 2020 |
Mechanistic Investigations of Metallo‐β‐lactamase Inhibitors: Strong Zinc Binding Is Not Required for Potent Enzyme Inhibition N Wade, KHME Tehrani, NC Brüchle, MJ van Haren, V Mashayekhi, ... ChemMedChem 16 (10), 1651-1659, 2021 | 15 | 2021 |