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Kinetics for Drug Discovery: an industry-driven effort to target drug residence time.
Drug Discov Today. 2017 Jun;22(6):896-911. doi: 10.1016/j.drudis.2017.02.002. Epub 2017 Apr 13.
Drug Discov Today. 2017.
PMID: 28412474
Review.
Mechanistic models enable the rational use of in vitro drug-target binding kinetics for better drug effects in patients.
de Witte WE, Wong YC, Nederpelt I, Heitman LH, Danhof M, van der Graaf PH, Gilissen RA, de Lange EC.
de Witte WE, et al. Among authors: nederpelt i.
Expert Opin Drug Discov. 2016;11(1):45-63. doi: 10.1517/17460441.2016.1100163. Epub 2015 Oct 20.
Expert Opin Drug Discov. 2016.
PMID: 26484747
Review.
Item in Clipboard
Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Nederpelt I, Georgi V, Schiele F, Nowak-Reppel K, Fernández-Montalván AE, IJzerman AP, Heitman LH.
Nederpelt I, et al.
Br J Pharmacol. 2016 Jan;173(1):128-41. doi: 10.1111/bph.13342. Epub 2015 Nov 4.
Br J Pharmacol. 2016.
PMID: 26398856
Free PMC article.
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Kinetic Profile of Neuropeptide-Receptor Interactions.
Nederpelt I, Bunnik J, IJzerman AP, Heitman LH.
Nederpelt I, et al.
Trends Neurosci. 2016 Dec;39(12):830-839. doi: 10.1016/j.tins.2016.09.008. Epub 2016 Oct 25.
Trends Neurosci. 2016.
PMID: 27793433
Review.
Item in Clipboard
From receptor binding kinetics to signal transduction; a missing link in predicting in vivo drug-action.
Nederpelt I, Kuzikov M, de Witte WEA, Schnider P, Tuijt B, Gul S, IJzerman AP, de Lange ECM, Heitman LH.
Nederpelt I, et al.
Sci Rep. 2017 Oct 26;7(1):14169. doi: 10.1038/s41598-017-14257-4.
Sci Rep. 2017.
PMID: 29075004
Free PMC article.
Item in Clipboard
Persistent GnRH receptor activation in pituitary αT3-1 cells analyzed with a label-free technology.
Nederpelt I, Vergroesen RD, IJzerman AP, Heitman LH.
Nederpelt I, et al.
Biosens Bioelectron. 2016 May 15;79:721-7. doi: 10.1016/j.bios.2015.12.066. Epub 2015 Dec 21.
Biosens Bioelectron. 2016.
PMID: 26774084
Item in Clipboard
Kinetic binding and activation profiles of endogenous tachykinins targeting the NK1 receptor.
Nederpelt I, Bleeker D, Tuijt B, IJzerman AP, Heitman LH.
Nederpelt I, et al.
Biochem Pharmacol. 2016 Oct 15;118:88-95. doi: 10.1016/j.bcp.2016.08.004. Epub 2016 Aug 5.
Biochem Pharmacol. 2016.
PMID: 27501920
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Multiple binding sites for small-molecule antagonists at the CC chemokine receptor 2.
Zweemer AJ, Nederpelt I, Vrieling H, Hafith S, Doornbos ML, de Vries H, Abt J, Gross R, Stamos D, Saunders J, Smit MJ, Ijzerman AP, Heitman LH.
Zweemer AJ, et al. Among authors: nederpelt i.
Mol Pharmacol. 2013 Oct;84(4):551-61. doi: 10.1124/mol.113.086850. Epub 2013 Jul 22.
Mol Pharmacol. 2013.
PMID: 23877010
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