Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis B Baragaña, B Forte, R Choi, S Nakazawa Hewitt, JA Bueren-Calabuig, ... Proceedings of the National Academy of Sciences 116 (14), 7015-7020, 2019 | 114 | 2019 |
Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1 KM Orrling, C Jansen, XL Vu, V Balmer, P Bregy, A Shanmugham, ... Journal of medicinal chemistry 55 (20), 8745-8756, 2012 | 68 | 2012 |
Molecular basis of RNA guanine-7 methyltransferase (RNMT) activation by RAM D Varshney, AP Petit, JA Bueren-Calabuig, C Jansen, DA Fletcher, ... Nucleic acids research 44 (21), 10423-10436, 2016 | 66 | 2016 |
Discovery of Novel Trypanosoma brucei Phosphodiesterase B1 Inhibitors by Virtual Screening against the Unliganded TbrPDEB1 Crystal Structure C Jansen, H Wang, AJ Kooistra, C de Graaf, KM Orrling, H Tenor, ... Journal of medicinal chemistry 56 (5), 2087-2096, 2013 | 65 | 2013 |
PDEStrIAn: a phosphodiesterase structure and ligand interaction annotated database as a tool for structure-based drug design C Jansen, AJ Kooistra, GK Kanev, R Leurs, IJP de Esch, C de Graaf Journal of medicinal chemistry 59 (15), 7029-7065, 2016 | 64 | 2016 |
Biochemical and Structural Characterization of Selective Allosteric Inhibitors of the Plasmodium falciparum Drug Target, Prolyl-tRNA-synthetase SN Hewitt, DM Dranow, BG Horst, JA Abendroth, B Forte, I Hallyburton, ... ACS infectious diseases 3 (1), 34-44, 2017 | 57 | 2017 |
Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi S Brand, EJ Ko, E Viayna, S Thompson, D Spinks, M Thomas, L Sandberg, ... Journal of medicinal chemistry 60 (17), 7284-7299, 2017 | 48 | 2017 |
Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals J Veerman, T van den Bergh, KM Orrling, C Jansen, P Cos, L Maes, ... Bioorganic & medicinal chemistry 24 (7), 1573-1581, 2016 | 41 | 2016 |
Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal … AR Blaazer, AK Singh, E De Heuvel, E Edink, KM Orrling, JJN Veerman, ... Journal of medicinal chemistry 61 (9), 3870-3888, 2018 | 40 | 2018 |
The heat is on: thermodynamic analysis in fragment-based drug discovery E Edink, C Jansen, R Leurs, IJP de Esch Drug Discovery Today: Technologies 7 (3), e189-e201, 2010 | 34 | 2010 |
Fragment-based screening in tandem with phenotypic screening provides novel antiparasitic hits AR Blaazer, KM Orrling, A Shanmugham, C Jansen, L Maes, E Edink, ... Journal of biomolecular screening 20 (1), 131-140, 2015 | 33 | 2015 |
Lysyl-tRNA synthetase, a target for urgently needed M. tuberculosis drugs SR Green, SH Davis, S Damerow, CA Engelhart, M Mathieson, ... Nature communications 13 (1), 5992, 2022 | 12 | 2022 |
Structure-based design, synthesis and structure–activity relationships of dibenzosuberyl-and benzoate-substituted tropines as ligands for acetylcholine-binding protein E Edink, A Akdemir, C Jansen, R van Elk, O Zuiderveld, FJJ de Kanter, ... Bioorganic & medicinal chemistry letters 22 (3), 1448-1454, 2012 | 8 | 2012 |
Anti-Infective Agents I Gilbert, B Baragana, N Caldwell, M Taylor, B Forte, M Cocco, C Jansen | | 2023 |
Anti-infective agents B Forte, N Norcross, C Jansen, B Baragana, I Gilbert, L Cleghorn, S Davis, ... US Patent 11,485,720, 2022 | | 2022 |
Anti-infective agents B Forte, N NORCROSS, C JANSEN, B BARAGANA, I Gilbert, ... | | 2022 |
Anti-infective agents B Forte, N Norcross, C Jansen, B Baragana, I Gilbert, L Cleghorn, S Davis, ... US Patent App. 16/311,829, 2019 | | 2019 |
Thermodynamic analysis in fragment-based drug discovery E Edink, C Jansen, R Leurs, IJP de Esch | | |