A1 Vertaisarvioitu alkuperäisartikkeli tieteellisessä lehdessä
Involvement of the first transmembrane segment of human alpha(2)-adrenoceptors in the subtype-selective binding of chlorpromazine, spiperone and spiroxatrine
Tekijät: Laurila JMM, Wissel G, Xhaard H, Ruuskanen JO, Johnson MS, Scheinin M
Kustantaja: WILEY-BLACKWELL
Julkaisuvuosi: 2011
Journal: British Journal of Pharmacology
Tietokannassa oleva lehden nimi: BRITISH JOURNAL OF PHARMACOLOGY
Lehden akronyymi: BRIT J PHARMACOL
Numero sarjassa: 5
Vuosikerta: 164
Numero: 5
Aloitussivu: 1558
Lopetussivu: 1572
Sivujen määrä: 15
ISSN: 0007-1188
DOI: https://doi.org/10.1111/j.1476-5381.2011.01520.x
Tiivistelmä
TM1 is involved in determining the low affinity of some antagonist ligands at the human alpha(2A)-adrenoceptor. The exact mechanism is not known, but the position of TM1 at a large distance from the binding pocket indicates that TM1 does not participate in specific side-chain interactions with amino acids within the binding pocket of the receptor or with ligands bound therein. Instead, molecular models suggest that TM1 has indirect conformational effects related to the charge distribution or overall shape of the binding pocket.
TM1 is involved in determining the low affinity of some antagonist ligands at the human alpha(2A)-adrenoceptor. The exact mechanism is not known, but the position of TM1 at a large distance from the binding pocket indicates that TM1 does not participate in specific side-chain interactions with amino acids within the binding pocket of the receptor or with ligands bound therein. Instead, molecular models suggest that TM1 has indirect conformational effects related to the charge distribution or overall shape of the binding pocket.
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