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Kinetic Profile of Neuropeptide-Receptor Interactions
- Source :
- Trends in neurosciences. 39(12)
- Publication Year :
- 2016
-
Abstract
- 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 endogenous ligands should be considered. This is because the release and binding kinetics of endogenous ligands in addition to receptor internalization rates are significant contributors to drug–target interactions. Here, we discuss the kinetic profile of three neuropeptides and their receptors; gonadotropin-releasing hormone receptor (GnRHR), neuropeptide Y receptors, and corticotropin-releasing factor receptor 1 (CRF 1 R). These three examples provide new insights into the importance of kinetic profiles which could improve the understanding of desired drug–target binding kinetics and advance drug discovery for various neurological and psychiatric illnesses.
- Subjects :
- 0301 basic medicine
Receptors, Neuropeptide
Chemistry
Drug discovery
General Neuroscience
Kinetics
GNRHR
Neuropeptides
Neuropeptide Y receptor
Receptor–ligand kinetics
03 medical and health sciences
030104 developmental biology
Biochemistry
Hormone receptor
Drug Discovery
Animals
Humans
Receptor
G protein-coupled receptor
Subjects
Details
- ISSN :
- 1878108X
- Volume :
- 39
- Issue :
- 12
- Database :
- OpenAIRE
- Journal :
- Trends in neurosciences
- Accession number :
- edsair.doi.dedup.....28c1f5c49cca506d0c2982bc87a77f68