Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Jacobus P. D. van Veldhoven"'
Autor:
Tamara A. M. Mocking, Wieke M. van Oostveen, Jacobus P. D. van Veldhoven, Hugo Minnee, Cynthia M. Fehres, Charles E. Whitehurst, Adriaan P. IJzerman, Laura H. Heitman
Publikováno v:
Frontiers in Pharmacology, Vol 15 (2024)
The prostaglandin transporter (PGT, SLCO2A1) mediates transport of prostanoids (a.o. prostaglandin E2 (PGE2)) into cells and thereby promotes their degradation. Overexpression of PGT leads to low extracellular PGE2 levels and has been linked to impai
Externí odkaz:
https://doaj.org/article/e0cc08e3ad25430fb31c87cdf54e7ca2
Autor:
Eelke B. Lenselink, Julien Louvel, Anna F. Forti, Jacobus P. D. van Veldhoven, Henk de Vries, Thea Mulder-Krieger, Fiona M. McRobb, Ana Negri, Joseph Goose, Robert Abel, Herman W. T. van Vlijmen, Lingle Wang, Edward Harder, Woody Sherman, Adriaan P. IJzerman, Thijs Beuming
Publikováno v:
ACS Omega, Vol 1, Iss 2, Pp 293-304 (2016)
Externí odkaz:
https://doaj.org/article/5d70f3f686804fd6b931cfc4929e3914
Autor:
Joseph Openy, Adriaan P. IJzerman, Burak Dogan, Ya-Yun Hsiao, Eelke B. Lenselink, Jacobus P. D. van Veldhoven, Natalia V. Ortiz Zacarías, Laura H. Heitman, Lisa S den Hollander
Publikováno v:
Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, 62(24), 11035-11053
Journal of Medicinal Chemistry, 62(24), 11035-11053
CC chemokine receptors 2 (CCR2) and 5 (CCR5) are involved in many inflammatory diseases; however, most CCR2 and CCR5 clinical candidates have been unsuccessful. (Pre)clinical evidence suggests that dual CCR2/CCR5 inhibition might be more effective in
Autor:
Tasia, Amelia, Jacobus P D, van Veldhoven, Matteo, Falsini, Rongfang, Liu, Laura H, Heitman, Gerard J P, van Westen, Elena, Segala, Grégory, Verdon, Robert K Y, Cheng, Robert M, Cooke, Daan, van der Es, Adriaan P, IJzerman
Publikováno v:
Journal of Medicinal Chemistry
In this study, we determined the crystal structure of an engineered human adenosine A2A receptor bound to a partial agonist and compared it to structures cocrystallized with either a full agonist or an antagonist/inverse agonist. The interaction betw
Autor:
Tasia Amelia, Robert K. Y. Cheng, Gerard J. P. van Westen, Rongfang Liu, Elena Segala, Robert M. Cooke, Laura H. Heitman, Jacobus P. D. van Veldhoven, Daan van der Es, Matteo Falsini, Grégory Verdon, Adriaan P. IJzerman
Publikováno v:
Journal of Medicinal Chemistry, 64(7), 3827-3842. American Chemical Society (ACS)
Journal of Medicinal Chemistry
Journal of Medicinal Chemistry
In this study, we determined the crystal structure of an engineered human adenosine A2A receptor bound to a partial agonist and compared it to structures cocrystallized with either a full agonist or an antagonist/inverse agonist. The interaction betw
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a3eaee9ee24339f7b4772a78e3323223
http://hdl.handle.net/1887/3204468
http://hdl.handle.net/1887/3204468
Autor:
Jacobus P. D. van Veldhoven, Constantijn J.E. van Gessel, Dorien Ward-van Oostwaard, Christine L. Mummery, Rongfang Liu, Giulia Campostrini, Milena Bellin, Adriaan P. IJzerman
Publikováno v:
European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, 212:113033. Elsevier BV
European Journal of Medicinal Chemistry, 212. ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
European Journal of Medicinal Chemistry, 212:113033. Elsevier BV
European Journal of Medicinal Chemistry, 212. ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
We synthesized and evaluated three novel series of substituted benzophenones for their allosteric modulation of the human K(v)11.1 (hERG) channel. We compared their effects with reference compound LUF7346 previously shown to shorten the action potent
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a17cbc5b7a058d19fe58d9fbcf3538d
https://hdl.handle.net/1887/3221400
https://hdl.handle.net/1887/3221400
Autor:
Jacobus P D, van Veldhoven, Giulia, Campostrini, Constantijn J E, van Gessel, Dorien, Ward-van Oostwaard, Rongfang, Liu, Christine L, Mummery, Milena, Bellin, Adriaan P, IJzerman
Publikováno v:
European journal of medicinal chemistry. 212
We synthesized and evaluated three novel series of substituted benzophenones for their allosteric modulation of the human K
Autor:
Annelien J.M. Zweemer, Adriaan P. IJzerman, Roy M. Kreekel, Eelke B. Lenselink, Jacobus P. D. van Veldhoven, Natalia V. Ortiz Zacarías, Wijnand J. C. van der Velden, Laura Portner, Laura H. Heitman, Salviana Ullo, Eric van Spronsen, Kenny Oenema, Margo Veenhuizen
Publikováno v:
Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, 61(20), 9146-9161. AMER CHEMICAL SOC
Journal of Medicinal Chemistry, 61(20), 9146-9161. AMER CHEMICAL SOC
The recent crystal structures of CC chemokine receptors 2 and 9 (CCR2 and CCR9) have provided structural evidence for an allosteric, intracellular binding site. The high conservation of residues involved in this site suggests its presence in most che
Autor:
Tina C. Wan, Kenneth A. Jacobson, Lili Du, Zhan Guo Gao, Silvia Paoletta, Elizabeth T. Gizewski, Adriaan P. IJzerman, John A. Auchampach, Jacobus P. D. van Veldhoven, Samantha Barbour
Publikováno v:
Purinergic Signalling. 14:59-71
Activity of the A(3) adenosine receptor (AR) allosteric modulators LUF6000 (2-cyclohexyl-N-(3,4-dichlorophenyl)-1H-imidazo [4,5-c]quinolin-4-amine) and LUF6096 (N-{2-[(3,4-dichlorophenyl)amino]quinolin-4-yl}cyclohexanecarbox-amide) was compared at fo
Autor:
Daan van der Es, Adriaan P. IJzerman, Jelle Offringa, Xue Yang, Laura H. Heitman, Eelke B. Lenselink, Jacobus P. D. van Veldhoven, Boaz J. Kuiper
Publikováno v:
Journal of Medicinal Chemistry, 62(7), 3539-3552
Journal of Medicinal Chemistry
Journal of Medicinal Chemistry
The development of covalent ligands for G protein-coupled receptors (GPCRs) is not a trivial process. Here, we report a streamlined workflow thereto from synthesis to validation, exemplified by the discovery of a covalent antagonist for the human ade
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5bf14842a65be649f77157c82babf912
http://hdl.handle.net/1887/80320
http://hdl.handle.net/1887/80320