Zobrazeno 1 - 10
of 130
pro vyhledávání: '"Johannes Brussee"'
Autor:
Dong Guo, Tamara A. M. Mocking, Marta Agliardi, Julien Louvel, Laura H. Heitman, Adriaan P. IJzerman, Roland Kars, Lizi Xia, Henk de Vries, Johannes Brussee, Tan Phát Pham
Publikováno v:
Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, 57(8), 3213-3222
Journal of Medicinal Chemistry, 57(8), 3213-3222
We report the synthesis and evaluation of previously unreported 4-amino-6-aryl-5-cyano-2-thiopyrimidines as selective human adenosine A1 receptor (hA1AR) agonists with tunable binding kinetics, this without affecting their nanomolar affinity for the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe20828dd16ce6081861182f289cea72
https://doi.org/10.1021/jm401643m
https://doi.org/10.1021/jm401643m
Autor:
Elisabeth Klaasse, Johannes Brussee, João F. S. Carvalho, Eelke B. Lenselink, Julien Louvel, Marjolein Soethoudt, Adriaan P. IJzerman, Zhiyi Yu
Publikováno v:
Journal of Medicinal Chemistry. 56:9427-9440
Cardiotoxicity is a side effect that plagues modern drug design and is very often due to the off-target blockade of the human ether-à-go-go related gene (hERG) potassium channel. To better understand the structural determinants of this blockade, we
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1bac0ddd9cffdc2d208621e6ac626c36
https://doi.org/10.1021/jm4010434
https://doi.org/10.1021/jm4010434
Autor:
Michael Emmerich, Alexander Aleman, Adriaan P. IJzerman, Patricia Marqués-Gallego, Eelke van der Horst, Thea Mulder-Krieger, Johannes W. Kruisselbrink, Andreas Bender, Jacobus P. D. van Veldhoven, Johannes Brussee
Publikováno v:
Journal of Chemical Information and Modeling. 52:1713-1721
A novel multiobjective evolutionary algorithm (MOEA) for de novo design was developed and applied to the discovery of new adenosine receptor antagonists. This method consists of several iterative cycles of structure generation, evaluation, and select
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c090acaa0f563d51c7583d290f621972
https://doi.org/10.1021/ci2005115
https://doi.org/10.1021/ci2005115
Publikováno v:
Molecular and Cellular Endocrinology. 351:326-336
The lutropin/choriogonadotrophin receptor (LHCGR) is a family A G protein-coupled receptor (GPCR) which binds the endogenous hormone-ligands at the large extracellular domain. In contrast, several drug-like low-molecular-weight ligands (LMWs) have be
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c74cc46474d33138c71b56bf84e3ee16
https://doi.org/10.1016/j.mce.2012.01.010
https://doi.org/10.1016/j.mce.2012.01.010
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
https://doi.org/10.1002/cmdc.201100366
Autor:
C Klopman, Jonathan Robert Lane, Adriaan P. IJzerman, M J Abdelkadir, Johannes Brussee, C M Artsen, Dieter Wolfram, Clara C. Blad, J P D van Veldhoven
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2736-2739
Nicotinic acid (niacin) has been used for decades as an antidyslipidemic drug in man. Its main target is the hydroxy-carboxylic acid receptor HCA2 (GPR109A), a G protein-coupled receptor. Other acids and esters such as methyl fumarate also interact w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::116945e8f0015fd6218645cd3ef46943
https://doi.org/10.1016/j.bmcl.2010.11.091
https://doi.org/10.1016/j.bmcl.2010.11.091
Autor:
E. G. J. C. Warmerdam, C.G. Kruse, A. Van Der Gen, Johannes Brussee, A. M. C. H. Van Den Nieuwendijk
Publikováno v:
Recueil des Travaux Chimiques des Pays-Bas. 115:20-24
The synthesis of (R)- and (S)-2-hydroxy-3-enoic acid esters [(R)-1a-d and (S)-1a-c] is described. The (R) enantiomers were prepared by a Pinner synthesis from the corresponding (R)-cyanohydrins [(R)-2a-d], which in turn were obtained by R-oxynitrilas
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8234ad11f7b959813a3c377b81e184d0
https://doi.org/10.1002/recl.19961150105
https://doi.org/10.1002/recl.19961150105
Autor:
Johannes Brussee, A. Van Der Gen, Sloothaak Johannes B, G.J.M. van Scharrenburg, E. Smitskamp-Wilms
Publikováno v:
Recueil des Travaux Chimiques des Pays-Bas. 110:209-215
Hydroxynitrile lyases from sweet almond (E.C. 4.1.2.10) and from sorghum bicolor (E.C. 4.1.2.11) have been purified to homogeneity by ion-exchange chromatography. These enzymes catalyse the decomposition of α-hydroxynitriles to aldehydes and hydrocy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1fc916e1d56704dd0e04bef202500405
https://doi.org/10.1002/recl.19911100514
https://doi.org/10.1002/recl.19911100514
Autor:
Judy Lin, Rajeshwar Narlawar, Johannes Brussee, Munikumar Reddy Doddareddy, Adriaan P. IJzerman, J. Robert Lane
Publikováno v:
Journal of Medicinal Chemistry. 53:3028-3037
Many G protein-coupled receptors (GPCRs), including the adenosine A(1) receptor (A(1)AR), have been shown to be allosterically modulated by small molecule ligands. So far, in the absence of structural information, the exact location of the allosteric
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f72ca46c41a20a50a7a64c222ac34840
https://doi.org/10.1021/jm901252a
https://doi.org/10.1021/jm901252a
Autor:
Shagufta, Lukas Nalos, Marcel A.G. van der Heyden, Johannes Brussee, Martin B. Rook, Elisabeth Klaasse, Adriaan P. IJzerman, Dong Guo, Marc A. Vos, Henk de Vries
Publikováno v:
ChemMedChem. 4:1722-1732
In this study we followed a new approach to analyze molecular substructures required for hERG channel blockade. We designed and synthesized 40 analogues of dofetilide (1), a potent hERG potassium channel blocker, and established structure-activity re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fbe01c8143458a77d1706ddbd8df8687
https://doi.org/10.1002/cmdc.200900203
https://doi.org/10.1002/cmdc.200900203