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Beta-Blockers Show Inverse Agonism to a Novel Constitutively Active Mutant of β1-Adrenoceptor

Authors :
Maruf Ahmed
Habib Abul Muntasir
Murad Hossain
Masaji Ishiguro
Tadazumi Komiyama
Ikunobu Muramatsu
Hitoshi Kurose
Takafumi Nagatomo
Source :
Journal of Pharmacological Sciences, Vol 102, Iss 2, Pp 167-172 (2006)
Publication Year :
2006
Publisher :
Elsevier, 2006.

Abstract

We obtained a new mutant of the β1-adrenergic receptor (β1-AR) by point mutations that can constitutively activate β1-AR. Aspartate104 of the β1-AR in the 2nd transmembrane was replaced with alanine. The β1-AR mutant expressed in human embryonic kidney (HEK)-293 cells displayed high level of constitutive activity with respect to wild-type (P

Subjects

Subjects :
Therapeutics. Pharmacology
RM1-950

Details

Language :
English
ISSN :
13478613
Volume :
102
Issue :
2
Database :
Directory of Open Access Journals
Journal :
Journal of Pharmacological Sciences
Publication Type :
Academic Journal
Accession number :
edsdoj.3d634c84f06347f5abb44f6077455725
Document Type :
article
Full Text :
https://doi.org/10.1254/jphs.FP0060640