Beta-Blockers Show Inverse Agonism to a Novel Constitutively Active Mutant of .BETA.1-Adrenoceptor

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概要

• 論文の詳細を見る

• 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<0.05), which could be partially inhibited by some beta-blockers. The constitutive activity of the mutant was confirmed by the finding that the enhanced activity is dependent on the level of receptor expression. The results of this study might have interesting implications for future studies aiming at elucidating the activation process of the β1-AR as well as the mechanism of action of beta-blockers.

• 公益社団法人 日本薬理学会の論文

著者

• Ahmed Maruf

  Pharmacy Department University Of Rajshahi

• ISHIGURO Masaji

  Suntory Institute for Bioorganic Research

• Muramatsu Ikunobu

  Division Of Pharmacology Department Of Biochemistry And Bioinformative Sciences School Of Medicine U

• Muntasir Habib

  Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App

• Nagatomo Takafumi

  Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App

• Komiyama Tadazumi

  Department Of Biochemistry Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App

• Hossain Murad

  Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App

• Kurose Hitoshi

  Department Of Pharmacology And Toxicology Faculty Of Pharmaceutical Sciences Kyushu University

• Ishiguro Masaji

  Suntory Institute for Bioorganic Research, Japan

• Muntasir Habib

  Department of Pharmacology, Faculty of Pharmaceutical Sciences, Niigata University of Pharmacy and Applied Life Sciences, Japan

• Komiyama Tadazumi

  Department of Biochemistry, Faculty of Pharmaceutical Sciences, Niigata University of Pharmacy and Applied Life Sciences, Japan

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