Towards improved drug action : target binding kinetics and functional efficacy at the mGlu2 receptor

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Towards improved drug action : target binding kinetics and functional efficacy at the mGlu2 receptor

Type: Doctoral Thesis
Title: Towards improved drug action : target binding kinetics and functional efficacy at the mGlu2 receptor
Author: Doornbos, M.L.J.
Issue Date: 2018-09-12
Keywords: Pharmacology
Receptors
GPCRs
Kinetics
Efficacy
Allosterism
Label-free
Drug discovery
Covalent.
Abstract: During the course of drug discovery translational steps are made. The translation from in vitro to in vivo experiments is not as predictive as one would desire, resulting in selection of inefficacious compounds but also in overlooking of promising drug candidates. This is not different for the mGlu2 receptor for which no drugs are available on the market so far despite enormous drug discovery efforts. Therefore, there is a need to improve the molecular understanding of key in vitro parameters that drive in vivo efficacy. Hence, this thesis focuses on the concepts of target binding kinetics and functional efficacy of both allosteric and orthosteric ligands of the mGlu2 receptor.
Promotor: Supervisor: IJzerman A.P. Co-Supervisor: Heitman L.H.
Faculty: Leiden Academic Centre for Drug Research (LACDR)
University: Leiden University
Uri: urn:isbn:9789493019546
Handle: http://hdl.handle.net/1887/65384
 

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