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

• Main Authors: Maruf Ahmed (Author), Habib Abul Muntasir (Author), Murad Hossain (Author), Masaji Ishiguro (Author), Tadazumi Komiyama (Author), Ikunobu Muramatsu (Author), Hitoshi Kurose (Author), Takafumi Nagatomo (Author)
• Format: Book
• Published: Elsevier, 2006-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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 constit...