Publications by authors named "Geert Sterk"

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The Role of Water Networks in Phosphodiesterase Inhibitor Dissociation and Kinetic Selectivity.
Antoni R Blaazer, Abhimanyu K Singh, Lorena Zara, Pierre Boronat, Lady J Bautista, Geert Jan Sterk

ChemMedChem· November 2024

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Adhesion of promotes a rapid change in developmental fate driven by cAMP signaling.
Shane Denecke, Madeline F Malfara, Kelly R Hodges, Nikki A Holmes, Andre R Williams, Geert Jan Sterk

mSphere· October 2024

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Lead Optimization of the 5-Phenylpyrazolopyrimidinone NPD-2975 toward Compounds with Improved Antitrypanosomal Efficacy.
Yang Zheng, Magali van den Kerkhof, Mohamed Ibrahim, Iwan J P De Esch, Louis Maes, Geert Jan Sterk

J Med Chem· February 2024

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Discovery of 5-Phenylpyrazolopyrimidinone Analogs as Potent Antitrypanosomal Agents with In Vivo Efficacy.
Yang Zheng, Magali van den Kerkhof, Tiffany van der Meer, Sheraz Gul, Maria Kuzikov, Geert Jan Sterk

J Med Chem· August 2023

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Structural Optimization of BIPPO Analogs as Potent Antimalarials.
Yang Zheng, An Matheeussen, Louis Maes, Guy Caljon, Geert Jan Sterk

Molecules· June 2023

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To Target or Not to Target Cyclic Nucleotide Phosphodiesterase 4A?
Yang Zheng, Susanne Schroeder, Georgi K Kanev, Sanaa S Botros, Samia William, Geert Jan Sterk

Int J Mol Sci· April 2023

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New Dual Inhibitors of Bacterial Topoisomerases with Broad-Spectrum Antibacterial Activity and In Vivo Efficacy against Vancomycin-Intermediate .
Martina Durcik, Andrej Emanuel Cotman, Žan Toplak, Štefan Možina, Žiga Skok, Geert Jan Sterk

J Med Chem· March 2023

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Discovery and Hit-to-Lead Optimization of Benzothiazole Scaffold-Based DNA Gyrase Inhibitors with Potent Activity against and .
Andrej Emanuel Cotman, Martina Durcik, Davide Benedetto Tiz, Federica Fulgheri, Daniela Secci, Geert Jan Sterk

J Med Chem· January 2023

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3-nitroimidazo[1,2-b]pyridazine as a novel scaffold for antiparasitics with sub-nanomolar anti-Giardia lamblia activity.
Yang Zheng, Joachim Müller, Stefan Kunz, Marco Siderius, Louis Maes, Geert Jan Sterk

Int J Parasitol Drugs Drug Resist· August 2022

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Structure Activity Relationship of -Substituted Phenyldihydropyrazolones Against Amastigotes.
Maarten Sijm, Louis Maes, Iwan J P de Esch, Guy Caljon, Geert Jan Sterk

Front Chem· April 2021

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Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with Activity against Intracellular Trypanosomatids.
Julianna Siciliano de Araújo, Raiza Brandão Peres, Patrícia Bernardino da Silva, Marcos Meuser Batista, Geert Jan Sterk

Antimicrob Agents Chemother· February 2021

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Spatial and Spatiotemporal Variability of Regional Background Ultrafine Particle Concentrations in the Netherlands.
Esther van de Beek, Jules Kerckhoffs, Gerard Hoek, Geert Sterk, Kees Meliefste

Environ Sci Technol· January 2021

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Discovery of Diaryl Ether Substituted Tetrahydrophthalazinones as TbrPDEB1 Inhibitors Following Structure-Based Virtual Screening.
Erik de Heuvel, Albert J Kooistra, Ewald Edink, Sjors van Klaveren, Jeffrey Stuijt, Geert Jan Sterk

Front Chem· January 2021

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Efficacy of Novel Pyrazolone Phosphodiesterase Inhibitors in Experimental Mouse Models of Trypanosoma cruzi.
Julianna Siciliano de Araújo, Cristiane França da Silva, Denise da Gama Jaén Batista, Aline Nefertiti, Ludmila Ferreira de Almeida Fiuza, Geert Jan Sterk

Antimicrob Agents Chemother· August 2020

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Structure-Activity Relationship of Phenylpyrazolones against Trypanosoma cruzi.
Maarten Sijm, Geert Jan Sterk, Guy Caljon, Louis Maes, Iwan J P de Esch

ChemMedChem· July 2020

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Cloning and functional complementation of ten Schistosoma mansoni phosphodiesterases expressed in the mammalian host stages.
Jane C Munday, Stefan Kunz, Titilola D Kalejaiye, Marco Siderius, Susanne Schroeder, Geert Jan Sterk

PLoS Negl Trop Dis· July 2020

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Evaluation of phthalazinone phosphodiesterase inhibitors with improved activity and selectivity against Trypanosoma cruzi.
Julianna Siciliano De Araújo, Patrícia Bernardino da Silva, Marcos Meuser Batista, Raiza Brandão Peres, Camila Cardoso-Santos, Geert Jan Sterk

J Antimicrob Chemother· April 2020

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Regional versus local wind speed and direction at a narrow beach with a high and steep foredune.
Winnie de Winter, Jasper Donker, Geert Sterk, Job van Beem, Gerben Ruessink

PLoS One· April 2020

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Identification of Phenylpyrazolone Dimers as a New Class of Anti-Trypanosoma cruzi Agents.
Maarten Sijm, Julianna Siciliano de Araújo, Alba Ramos Llorca, Kristina Orrling, Lydia Stiny, Geert Jan Sterk

ChemMedChem· September 2019

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Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors (Part 2).
Erik de Heuvel, Abhimanyu K Singh, Pierre Boronat, Albert J Kooistra, Tiffany van der Meer, Geert Jan Sterk

Bioorg Med Chem· September 2019

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Screening of a PDE-focused library identifies imidazoles with in vitro and in vivo antischistosomal activity.
Sanaa S Botros, Samia William, Abdel-Nasser A Sabra, Naglaa M El-Lakkany, Sayed H Seif El-Din, Geert J Sterk

Int J Parasitol Drugs Drug Resist· April 2019

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Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity.
Antoni R Blaazer, Abhimanyu K Singh, Erik de Heuvel, Ewald Edink, Kristina M Orrling, Geert Jan Sterk

J Med Chem· May 2018

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The single cyclic nucleotide-specific phosphodiesterase of the intestinal parasite Giardia lamblia represents a potential drug target.
Stefan Kunz, Vreni Balmer, Geert Jan Sterk, Michael P Pollastri, Rob Leurs

PLoS Negl Trop Dis· September 2017

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Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo.
Michael Soeberdt, Peter Molenveld, Roy P M Storcken, Renaud Bouzanne des Mazery, Geert Jan Sterk

J Med Chem· March 2017

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Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals.
Johan Veerman, Toine van den Bergh, Kristina M Orrling, Chimed Jansen, Paul Cos, Geert Jan Sterk

Bioorg Med Chem· April 2016

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