Allosteric modulators of the hERG K+ channel

Autor: Laura H. Heitman, Zhiyi Yu, Elisabeth Klaasse, Adriaan P. IJzerman

Publikováno v: Toxicology and Applied Pharmacology. 274:78-86

Drugs that block the cardiac K(+) channel encoded by the human ether-a-go-go gene (hERG) have been associated with QT interval prolongation leading to proarrhythmia, and in some cases, sudden cardiac death. Because of special structural features of t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0e7d929a135732dbcfe5aae33c91278c
https://doi.org/10.1016/j.taap.2013.10.024

Understanding of Molecular Substructures that Contribute to hERG K+ Channel Blockade: Synthesis and Biological Evaluation of E-4031 Analogues

Autor: Olaf Scheel, Elisabeth Klaasse, Johannes Brussee, Maris Vilums, Adriaan P. IJzerman, Jeroen Overman

Publikováno v: ChemMedChem. 7:107-113

Cardiotoxicity is a common side effect of a large variety of drugs that is often caused by off-target human ether-à-go-go-related gene (hERG) potassium channel blockade. In this study, we designed and synthesized a series of derivatives of the class

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::daed0ec8de5de99597404fd51ffd9ef7
https://doi.org/10.1002/cmdc.201100366

Prospective Validation of a Comprehensive In silico hERG Model and its Applications to Commercial Compound and Drug Databases

Autor: Munikumar Reddy Doddareddy, Andreas Bender, Shagufta, Elisabeth Klaasse, Adriaan P. IJzerman

Publikováno v: ChemMedChem. 5:716-729

Ligand-based in silico hERG models were generated for 2 644 compounds using linear discriminant analysis (LDA) and support vector machines (SVM). As a result, the dataset used for the model generation is the largest publicly available (see Supporting

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::636e8c83e372f5d90c891d670ab20bb7
https://doi.org/10.1002/cmdc.201000024

Allosteric modulation and constitutive activity of fusion proteins between the adenosine A1 receptor and different 351Cys-mutated Gi α-subunits

Autor: Anna Lorenzen, Graeme Milligan, Rianne A.F. de Ligt, Rob Leurs, Ad P. IJzerman, Sophie F. Roerink, Elisabeth Klaasse

Publikováno v: Klaasse, E, de Ligt, R A, Roerink, S F, Lorenzen, A, Milligan, G, Leurs, R & AP, I J 2004, ' Allosteric modulation and constitutive activity of fusion proteins between the adenosine A1 receptor and different 351Cys-mutated Gi alpha-subunits ', European Journal of Pharmacology, vol. 499, no. 1-2, pp. 91-8 . https://doi.org/10.1016/j.ejphar.2004.07.108
European Journal of Pharmacology, 499(1-2), 91-8. Elsevier

We studied fusion proteins between the human adenosine A1 receptor and different 351Cys-mutated G(i1) alpha-subunits (A1-Gialpha) with respect to two important concepts in receptor pharmacology, i.e. allosteric modulation and constitutive activity/in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::912525f9344991cca5011c6e7efc63f8
https://doi.org/10.1016/j.ejphar.2004.07.108

Internalization and desensitization of adenosine receptors

Autor: Elisabeth Klaasse, Margot W. Beukers, Willem J. de Grip, Adriaan P. IJzerman

Publikováno v: Purinergic Signalling, 4, 21-37
Purinergic Signalling, 4, 1, pp. 21-37
Purinergic Signalling, 4(1), 21-37
Purinergic Signalling

Contains fulltext : 69662.pdf (Publisher’s version ) (Closed access) Until now, more than 800 distinct G protein-coupled receptors (GPCRs) have been identified in the human genome. The four subtypes of the adenosine receptor (A(1), A(2A), A(2B) and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c0dfc01f91303dddc15348a817ba7f09
http://hdl.handle.net/2066/69662