Article
Orthosteric binding of ρ-Da1a, a natural peptide of snake venom interacting selectively with the α1A-adrenoceptor.
PloS one - 1 Jan 2013
Maïga Arhamatoulaye, Merlin Jon, Marcon Elodie, Rouget Céline, Larregola Maud, Gilquin Bernard, Fruchart-Gaillard Carole, Lajeunesse Evelyne, Marchetti Charles, Lorphelin Alain, Bellanger Laurent, Summers Roger J, Hutchinson Dana S, Evans Bronwyn A, Servent Denis, Gilles Nicolas
Abstract excerpt
ρ-Da1a is a three-finger fold toxin from green mamba venom that is highly selective for the α1A-adrenoceptor. This toxin has atypical pharmacological properties, including incomplete inhibition of (3)H-prazosin or (125)I-HEAT binding and insurmountable antagonist action. We aimed to clarify its mode of action at the α1A-adrenoceptor. The affinity (pKi 9.26) and selectivity of ρ-Da1a for the α1A-adrenoceptor were...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.
