Kinetic Profile of Neuropeptide-Receptor Interactions
| Autor: | Julia Bunnik, Laura H. Heitman, Indira Nederpelt, Adriaan P. IJzerman |
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| Rok vydání: | 2016 |
| Předmět: |
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 |
| Zdroj: | Trends in neurosciences. 39(12) |
| ISSN: | 1878-108X |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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