Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Indira Nederpelt"'
Autor:
Maria Kuzikov, Wilbert de Witte, Sheraz Gul, Laura H. Heitman, Elizabeth C. M. de Lange, Adriaan P. IJzerman, Indira Nederpelt, Bruno Tuijt, Schnider Patrick
Publikováno v:
Scientific Reports, Vol 7, Iss 1, Pp 1-10 (2017)
Scientific Reports, 7, 14169
Scientific Reports
Scientific Reports, 7, 14169
Scientific Reports
An important question in drug discovery is how to overcome the significant challenge of high drug attrition rates due to lack of efficacy and safety. A missing link in the understanding of determinants for drug efficacy is the relation between drug-t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a57a8529ae41e068091b69d94d3f296
http://link.springer.com/article/10.1038/s41598-017-14257-4
http://link.springer.com/article/10.1038/s41598-017-14257-4
Publikováno v:
Biochemical Pharmacology. 118:88-95
Ligand-receptor binding kinetics (i.e. association and dissociation rates) are emerging as important parameters for drug efficacy in vivo. Awareness of the kinetic behavior of endogenous ligands is pivotal, as drugs often have to compete with those.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c88d46445dc8ca1033f76a7aae04c70
https://doi.org/10.1016/j.bcp.2016.08.004
https://doi.org/10.1016/j.bcp.2016.08.004
Autor:
Katrin Nowak-Reppel, Amaury Ernesto Fernandez-Montalvan, Adriaan P. IJzerman, Victoria Georgi, Indira Nederpelt, Felix Schiele, Laura H. Heitman
Publikováno v:
British Journal of Pharmacology
BACKGROUND AND PURPOSE\nDrug-target residence time is an important, yet often overlooked, parameter in drug discovery. Multiple studies have proposed an increased residence time to be beneficial for improved drug efficacy and/or longer duration of ac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e77fc689bf8bf26b1579256c9d412dbc
https://doi.org/10.1111/bph.13342
https://doi.org/10.1111/bph.13342
Autor:
Daria B. Kokh, Leigh A. Stoddart, Robert M. Cooke, Dorothee Andres, Rebecca C. Wade, Gerhard F. Ecker, Steve Hill, Wilhelmus E. A. de Witte, Marta Amaral, Elena Segala, Bernhard Knasmueller, Matthias Frech, Reggie Bosma, Laura H. Heitman, S. Kashif Sadiq, Anke Muller-Fahrnow, Chris de Graaf, Indira Nederpelt, Dong Guo, Adriaan P. IJzerman, Victoria Georgi, Elizabeth C. M. de Lange, Yin Cheong Wong, Lars Richter, Doris A. Schuetz, Rob Leurs
Publikováno v:
Drug Discovery Today, 22(6), 896-911
Schuetz, D A, de Witte, W E A, Wong, Y C, Knasmueller, B, Richter, L, Kokh, D B, Sadiq, S K, Bosma, R, Nederpelt, I, Heitman, L H, Segala, E, Amaral, M, Guo, D, Andres, D, Georgi, V, Stoddart, L A, Hill, S, Cooke, R M, de Graaf, C, Leurs, R, Frech, M, Wade, R C, de Lange, E C M, IJzerman, A P, Müller-Fahrnow, A & Ecker, G F 2017, ' Kinetics for Drug Discovery : an industry-driven effort to target drug residence time ', Drug Discovery Today, vol. 22, no. 6, pp. 896-911 . https://doi.org/10.1016/j.drudis.2017.02.002
Drug Discovery Today
Schuetz, D A, de Witte, W E A, Wong, Y C, Knasmueller, B, Richter, L, Kokh, D B, Sadiq, S K, Bosma, R, Nederpelt, I, Heitman, L H, Segala, E, Amaral, M, Guo, D, Andres, D, Georgi, V, Stoddart, L A, Hill, S, Cooke, R M, de Graaf, C, Leurs, R, Frech, M, Wade, R C, de Lange, E C M, IJzerman, A P, Müller-Fahrnow, A & Ecker, G F 2017, ' Kinetics for Drug Discovery : an industry-driven effort to target drug residence time ', Drug Discovery Today, vol. 22, no. 6, pp. 896-911 . https://doi.org/10.1016/j.drudis.2017.02.002
Drug Discovery Today
A considerable number of approved drugs show non-equilibrium binding characteristics, emphasizing the potential role of drug residence times for in vivo efficacy. Therefore, a detailed understanding of the kinetics of association and dissociation of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d0f239e285cfffe51e30eaad7eaed15
https://doi.org/10.1016/j.drudis.2017.02.002
https://doi.org/10.1016/j.drudis.2017.02.002
Autor:
Maarten L. J. Doornbos, Annelien J.M. Zweemer, Dean Stamos, Hilde Vrieling, Jeffrey Abt, John Saunders, Indira Nederpelt, Sarah Hafith, Henk de Vries, Laura H. Heitman, Martine J. Smit, Raymond S. Gross, Adriaan P. IJzerman
Publikováno v:
Molecular Pharmacology, 2013(84), 551-561. American Society for Pharmacology and Experimental Therapeutics
Zweemer, A J, Nederpelt, I, Vrieling, H, Hafith, S, Doornbos, M L, de Vries, H, Abt, J, Gross, R, Stamos, D, Saunders, J, Smit, M J, IJzerman, A P & Heitman, L H 2013, ' Multiple Binding Sites for Small Molecule Antagonists at the Chemokine Receptor CCR2 ', Molecular Pharmacology, vol. 2013, no. 84, pp. 551-561 . https://doi.org/10.1124/mol.113.086850
Zweemer, A J, Nederpelt, I, Vrieling, H, Hafith, S, Doornbos, M L, de Vries, H, Abt, J, Gross, R, Stamos, D, Saunders, J, Smit, M J, IJzerman, A P & Heitman, L H 2013, ' Multiple Binding Sites for Small Molecule Antagonists at the Chemokine Receptor CCR2 ', Molecular Pharmacology, vol. 2013, no. 84, pp. 551-561 . https://doi.org/10.1124/mol.113.086850
The chemokine receptor CCR2 is a G protein-coupled receptor that is activated primarily by the endogenous CC chemokine ligand 2 (CCL2). Many different small-molecule antagonists have been developed to inhibit this receptor, as it is involved in a var
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::876056dc6ab3615ab4c65f282a968413
https://doi.org/10.1124/mol.113.086850
https://doi.org/10.1124/mol.113.086850
Publikováno v:
Trends in neurosciences. 39(12)
Currently, drug discovery focusses only on quantifying pharmacological parameters, sometimes including binding kinetics, of drug candidates. For a complete understanding of a drug's desired binding kinetics, the kinetics of both the target and its en
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::28c1f5c49cca506d0c2982bc87a77f68
https://pubmed.ncbi.nlm.nih.gov/27793433
https://pubmed.ncbi.nlm.nih.gov/27793433
The gonadotropin-releasing hormone (GnRH) receptor is a drug target for certain hormone-dependent diseases such as prostate cancer. In this study, we examined the activation profiles of the endogenous ligand, GnRH and a well-known marketed analog, bu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3886bb741c380f826b3c21755c480161
https://hdl.handle.net/1887/43662
https://hdl.handle.net/1887/43662
Autor:
Meindert Danhof, Indira Nederpelt, Piet H. van der Graaf, Yin Cheong Wong, Ron Gilissen, Wilhelmus E. A. de Witte, Elizabeth C. M. de Lange, Laura H. Heitman
Publikováno v:
Expert opinion on drug discovery
Expert opinion on drug discovery, 11(1), 45-63
Expert opinion on drug discovery, 11(1), 45-63
INTRODUCTION\nDrug-target binding kinetics are major determinants of the time course of drug action for several drugs, as clearly described for the irreversible binders omeprazole and aspirin. This supports the increasing interest to incorporate newl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb3556d8bc7be65da16ac07e0166446c
https://pubmed.ncbi.nlm.nih.gov/26484747
https://pubmed.ncbi.nlm.nih.gov/26484747
Autor:
Indira, Nederpelt, Victoria, Georgi, Felix, Schiele, Katrin, Nowak-Reppel, Amaury E, Fernández-Montalván, Adriaan P, IJzerman, Laura H, Heitman
Publikováno v:
British journal of pharmacology. 173(1)
Drug-target residence time is an important, yet often overlooked, parameter in drug discovery. Multiple studies have proposed an increased residence time to be beneficial for improved drug efficacy and/or longer duration of action. Currently, there a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::ed0dd98b1355f383cb2ed44f8c6af99f
https://pubmed.ncbi.nlm.nih.gov/26398856
https://pubmed.ncbi.nlm.nih.gov/26398856