dc.contributor.author | Ndzibongwana, Sethu | |
dc.contributor.author | Ngobese, Samukelo | |
dc.contributor.author | Sayed, Ahmad | |
dc.contributor.author | Shongwe, Ciniso | |
dc.contributor.author | White-Phillips, Simon | |
dc.contributor.author | Joubert, Jacques | |
dc.date.accessioned | 2022-10-27T10:34:51Z | |
dc.date.available | 2022-10-27T10:34:51Z | |
dc.date.issued | 2019 | |
dc.identifier.citation | Ndzibongwana, 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, 4092. https://doi.org/10.3390/molecules24224092 | en_US |
dc.identifier.issn | 1420-3049 | |
dc.identifier.uri | https://doi.org/10.3390/molecules24224092 | |
dc.identifier.uri | http://hdl.handle.net/10566/8081 | |
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.language.iso | en | en_US |
dc.publisher | MDPI | en_US |
dc.subject | Molecular modelling | en_US |
dc.subject | Fluorescent ligand | en_US |
dc.subject | Pharmacy | en_US |
dc.subject | Fluorescent bioassay | en_US |
dc.subject | Amantadine | en_US |
dc.title | Structural analysis, molecular modelling and preliminary competition bnding studies of AM-DAN as a NMDA Receptor PCP-Site Fluorescent Ligand | en_US |
dc.type | Article | en_US |