Výsledky vyhledávání - "Ad P. Ijzerman"

Pan-cancer in silico analysis of somatic mutations in G-protein coupled receptors: The effect of evolutionary conservation and natural variance

Autor: Kai Ye, M. Gorostiola González, Xuesong Wang, H.W.T. (Herman) van Vlijmen, G. J. P. van Westen, Hugo Gutiérrez-de-Terán, Laura H. Heitman, Brandon J. Bongers, Ad P. IJzerman, Willem Jespers

G protein-coupled receptors (GPCRs) form the most frequently exploited drug target family, moreover they are often found mutated in cancer. Here we used an aggregated dataset of mutations found in cancer patient samples derived from the Genomic Data

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f29c80164bd58fa293b5ddab586a0c5c
https://doi.org/10.1101/2021.10.25.465693

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LUF7244 plus Dofetilide Rescues Aberrant Kv11.1 Trafficking and Produces Functional IKv11.1

Autor: Doreth Fransen, Brian P. Delisle, Ad P. Ijzerman, Willem B. van Ham, Yuan Ji, Craig T. January, Tyona D. Golden, Anna Stary-Weinzinger, Laura H. Heitman, Muge Qile, Marien J C Houtman, Marcel A.G. van der Heyden, Fee Romunde

Publikováno v: Molecular Pharmacology, 97(6), 355-364

Kv11.1 (hERG) channels play a critical role in repolarization of cardiomyocytes during the cardiac action potential (AP). Drug mediated Kv11.1 blockade results in AP prolongation, which poses an increased risk of sudden cardiac death. Many drugs, lik

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8f19409ef10ac6ca1a07fb97b8399be9
http://hdl.handle.net/1887/3200949

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TLR-Induced IL-12 and CCL2 Production by Myeloid Cells Is Dependent on Adenosine A(3) Receptor-Mediated Signaling

Autor: Dimitri A. Diavatopoulos, Ella A. Zuiderwijk-Sick, Elles Simonetti, Hans J. P. M. Koenen, Céline van der Putten, Sacha A. F. T. van Hijum, Jeffrey J. Bajramovic, Ad P. IJzerman, Lejla Sukurova, Johannes M. van Noort, Saskia M. Burm, Jennifer Veth

Publikováno v: Journal of Immunology, 202, 2421-2430
Journal of Immunology, 202, 8, pp. 2421-2430

TLR-induced signaling potently activates cells of the innate immune system and is subject to regulation at different levels. Inflammatory conditions are associated with increased levels of extracellular adenosine, which can modulate TLR-induced produ

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc634871be18e0fe56dad6265efdf403
http://hdl.handle.net/2066/202858

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LUF7244, an allosteric modulator/activator of K

Autor: Muge, Qile, Henriette D M, Beekman, David J, Sprenkeler, Marien J C, Houtman, Willem B, van Ham, Anna, Stary-Weinzinger, Stanislav, Beyl, Steffen, Hering, Dirk-Jan, van den Berg, Elizabeth C M, de Lange, Laura H, Heitman, Ad P, IJzerman, Marc A, Vos, Marcel A G, van der Heyden

Publikováno v: British Journal of Pharmacology

Background and Purpose Kv11.1 (hERG) channel blockade is an adverse effect of many drugs and lead compounds, associated with lethal cardiac arrhythmias. LUF7244 is a negative allosteric modulator/activator of Kv11.1 channels that inhibits early after

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::66ac4c668312463df84314187799a0a6
https://pubmed.ncbi.nlm.nih.gov/31339551

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TLR-Induced IL-12 and CCL2 Production by Myeloid Cells Is Dependent on Adenosine A

Autor: Céline, van der Putten, Jennifer, Veth, Lejla, Sukurova, Ella A, Zuiderwijk-Sick, Elles, Simonetti, Hans J P M, Koenen, Saskia M, Burm, Johannes M, van Noort, Ad P, IJzerman, Sacha A F T, van Hijum, Dimitri, Diavatopoulos, Jeffrey J, Bajramovic

Publikováno v: Journal of immunology (Baltimore, Md. : 1950). 202(8)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::0a923c8ffb96fc620df25cd372e1efde
https://pubmed.ncbi.nlm.nih.gov/30804043

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A covalent antagonist for the human adenosine A2A receptor

Autor: Thomas J M Michiels, Laura H. Heitman, Xue Yang, Julien Louvel, Ad P. IJzerman, Eelke B. Lenselink, Guo Dong

Publikováno v: Purinergic signalling, 13(2), 191-201
Purinergic Signalling, 13(2), 191-201. SPRINGER
Purinergic Signalling, 13(2), 191-201
Purinergic signalling

The structure of the human A2A adenosine receptor has been elucidated by X-ray crystallography with a high affinity non-xanthine antagonist, ZM241385, bound to it. This template molecule served as a starting point for the incorporation of reactive mo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::313d0b8828eaed6bc6f96956526f217f
https://hdl.handle.net/1887/64259

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Kv11.1 (hERG)-induced cardiotoxicity: a molecular insight from a binding kinetics study of prototypical Kv11.1 (hERG) inhibitors

Autor: Zhiyi Yu, Laura H. Heitman, Ad P. IJzerman

Publikováno v: British Journal of Pharmacology

BACKGROUND AND PURPOSE\nDrug-induced arrhythmia due to blockade of the Kv 11.1 channel (also known as the hERG K(+) channel) is a frequent side effect. Previous studies have primarily focused on equilibrium parameters, i.e. affinity or potency, of dr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::236c48a9979a08e0539e3c057cdaf23a
https://doi.org/10.1111/bph.12967

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A yeast screening method to decipher the interaction between the adenosine A2B receptor and the C-terminus of different G protein α-subunits

Autor: Eelke B. Lenselink, Rongfang Liu, Nick J. A. Groenewoud, Ad P. IJzerman, Miriam C. Peeters

Publikováno v: Purinergic Signalling. 10:441-453

The expression of human G protein-coupled receptors (GPCRs) in Saccharomyces cerevisiae containing chimeric yeast/mammalian Gα subunits provides a useful tool for the study of GPCR activation. In this study, we used a one-GPCR-one-G protein yeast sc

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eff5c18ba840cd59340c69a2490efc1c
https://doi.org/10.1007/s11302-014-9407-6

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LUF7244, an allosteric modulator/activator of K v11.1 channels, counteracts dofetilide-induced torsades de pointes arrhythmia in the chronic atrioventricular block dog model

Autor: Marien J C Houtman, Laura H. Heitman, Marc A. Vos, Elizabeth C. M. de Lange, Stanislav Beyl, Ad P. IJzerman, Steffen Hering, David J Sprenkeler, Muge Qile, Willem B. van Ham, Marcel A.G. van der Heyden, Henriette D.M. Beekman, Anna Stary-Weinzinger, Dirk-Jan van den Berg

Publikováno v: British Journal of Pharmacology, 176(19), 3871-3885
British Journal of Pharmacology
British Journal of Pharmacology, 176(19), 3871. Wiley-Blackwell

Background and PurposeKv11.1 (hERG) channel blockade is an adverse effect of many drugs and lead compounds, associated with lethal cardiac arrhythmias. LUF7244 is a negative allosteric modulator/activator of Kv11.1 channels that inhibits early afterd

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e979ff2166a7fb461226b7ed48c7dda
https://hdl.handle.net/1874/387119

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