Chimed Jansen

发表

PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.

Georgi K. Kanev, I. D. de Esch, R. Leurs, 2016, Journal of medicinal chemistry.

Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity

I. D. de Esch, R. Leurs, H. D. de Koning, 2018, Journal of medicinal chemistry.

Discovery of novel Trypanosoma brucei phosphodiesterase B 1 inhibitors by virtual screening against the unliganded TbrPDEB 1 crystal structure Chapter 4

Huanchen Wang, Chimed Jansen, 2015 .

Lysyl-tRNA synthetase, a target for urgently needed M. tuberculosis drugs

Robert H Bates, L. Stojanovski, K. Read, 2022, Nature Communications.

Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma

A. Hill, Frederick R. C. Simeons, L. Stojanovski, 2017 .

Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis

Juan A. Bueren-Calabuig, Andrei V. Pisliakov, David W. Gray, 2019, Proceedings of the National Academy of Sciences.

Biochemical and Structural Characterization of Selective Allosteric Inhibitors of the Plasmodium falciparum Drug Target, Prolyl-tRNA-synthetase

David W. Gray, K. Read, I. Gilbert, 2016, ACS infectious diseases.

Structure-based design, synthesis and structure-activity relationships of dibenzosuberyl- and benzoate-substituted tropines as ligands for acetylcholine-binding protein.

I. D. de Esch, O. Zuiderveld, R. Leurs, 2012, Bioorganic & medicinal chemistry letters.

The heat is on: thermodynamic analysis in fragment-based drug discovery.

Iwan J. P. de Esch, Rob Leurs, Ewald Edink, 2010, Drug discovery today. Technologies.

Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi

A. Hill, Frederick R. C. Simeons, L. Stojanovski, 2017, Journal of medicinal chemistry.

Fragment-Based Screening in Tandem with Phenotypic Screening Provides Novel Antiparasitic Hits

Rob Leurs, Marco Siderius, Ewald Edink, 2015, Journal of biomolecular screening.

Chapter 3 Thermodynamic analysis in fragment-based drug discovery

R. Leurs, I. D. Esch, Chimed Jansen, 2011 .

Molecular basis of RNA guanine-7 methyltransferase (RNMT) activation by RAM

Juan A. Bueren-Calabuig, Andrei V. Pisliakov, V. Cowling, 2016, Nucleic acids research.

Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals.

I. D. de Esch, R. Leurs, E. Chatelain, 2016, Bioorganic & medicinal chemistry.

Discovery of novel Trypanosoma brucei phosphodiesterase B1 inhibitors by virtual screening against the unliganded TbrPDEB1 crystal structure.

Chris de Graaf, Rob Leurs, Iwan J P de Esch, 2013, Journal of medicinal chemistry.

Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1.

Rob Leurs, Emily Adams, Paul Cos, 2012, Journal of medicinal chemistry.

Fragment-Based Screening in Tandem with Phenotypic Screening Provides Novel Antiparasitic Hits

I. D. de Esch, R. Leurs, M. Siderius, 2015, Journal of biomolecular screening.

Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1.

I. D. de Esch, R. Leurs, E. Chatelain, 2012, Journal of medicinal chemistry.

Discovery of novel Trypanosoma brucei phosphodiesterase B1 inhibitors by virtual screening against the unliganded TbrPDEB1 crystal structure.

H. Ke, I. D. de Esch, R. Leurs, 2013, Journal of medicinal chemistry.