Structural analysis, molecular modelling and preliminary competition binding studies of AM-DAN as a NMDA receptor PCP-Site fluorescent ligand

Simple item page
dc.contributor.authorNdzibongwana, Sethu
dc.contributor.authorNgobese, Samukelo
dc.contributor.authorSayed, Ahmad
dc.date.accessioned2022-11-02T08:50:52Z
dc.date.available2022-11-02T08:50:52Z
dc.date.issued2019
dc.description.abstract: Excitotoxicity related to the dysfunction of the N-methyl-d-aspartate receptor (NMDAR) has been indicated to play an integral role in the pathophysiology of multiple disease states, including neurodegenerative disorders such as Parkinson’s disease. There is a notable gap in the market for novel NMDAR antagonists, however current methods to analyse potential antagonists rely on indirect measurements of calcium flux and hazardous radioligand binding assays. Recently, a fluorescent NMDAR ligand, N-adamantan-1-yl-dimethylamino-1-naphthalenesulfonic acid, known as AM-DAN was developed by our group. Additional studies on this ligand is necessary to evaluate its potential as a biological tool in NMDAR research. Therefore, this study was aimed at conducting structural analyses, fluorescence experiments, high-accuracy NMDAR molecular modelling and NMDAR phencyclidine (PCP) site competition binding studies using AM-DAN. Results revealed that AM-DAN has appropriate structural properties, significant fluorescent ability in various solvents and is able to bind selectively and compete for the PCP-binding site of the NMDAR. Therefore, AM-DAN holds promise as a novel fluorescent ligand to measure the affinity of prospective drugs binding at the NMDAR PCP-site and may circumvent the use of radioligands.en_US
dc.identifier.citationNdzibongwana S, Ngobese S, Sayed A, Shongwe C, White-Phillips S, Joubert J. Structural Analysis, Molecular Modelling and Preliminary Competition Binding Studies of AM-DAN as a NMDA Receptor PCP-Site Fluorescent Ligand. Molecules. 2019; 24(22):4092. https://doi.org/10.3390/molecules24224092en_US
dc.identifier.urihttps//doi.org:/10.3390/molecules24224092
dc.identifier.urihttp://hdl.handle.net/10566/8131
dc.language.isoenen_US
dc.publisherMDPIen_US
dc.subjectNMDARen_US
dc.subjectAmantidineen_US
dc.subjectDansylen_US
dc.titleStructural analysis, molecular modelling and preliminary competition binding studies of AM-DAN as a NMDA receptor PCP-Site fluorescent liganden_US
dc.typeArticleen_US

Files

Original bundle
Now showing 1 - 1 of 1
Thumbnail Image
Name:
shongwe_structural analysismolecular_2019.pdf
Size:
4.1 MB
Format:
Adobe Portable Document Format
Description:
Download
License bundle
Now showing 1 - 1 of 1
No Thumbnail Available
Name:
license.txt
Size:
1.71 KB
Format:
Item-specific license agreed upon to submission
Description:
Download

Collections

Research Articles (Biotechnology)