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3D Physical Model of Beta‐2 Adrenergic Receptorββ
Author(s) -
Acheampong Mary,
Bhikhi Kavitia,
Dueño Daviana,
Glover Bobby,
Harris Lachoy,
Henry Alafia,
Mata Randol,
VanBrakle Marisa,
Granberry Allison,
Beuming Thijs,
Assefa Haregewein
Publication year - 2011
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.25.1_supplement.lb155
Subject(s) - g protein coupled receptor , chemistry , transmembrane protein , extracellular , receptor , intracellular , biophysics , adrenergic receptor , microbiology and biotechnology , stereochemistry , biochemistry , biology
The Beta‐2 Adrenergic Receptor (β 2 AR) is a G‐protein coupled receptor (GPCR) which, when stimulated by a catecholamine, causes the relaxation of various smooth muscles, and the production of glucose by glycogenolysis and gluconeogenesis. Pharmaceuticals acting though β 2 AR are important for treating asthma, chronic obstructive pulmonary disease (COPD), and premature labor. The structure of β 2 AR consists of 7‐transmembrane domains, connected by three extracellular loops and three intracellular loops. At the base of the extracellular loops, buried within the transmembrane helices, there is a predominately hydrophobic binding pocket with several crucial polar residues that interact with ligands. Interestingly, certain polar interactions appear to play a role in the conversion of the receptor from an active to an inactive state. Recent crystallography of β 2 AR has revealed that the active state, relative to the inactive state, shows only minor changes in the binding pocket, whereas critical shifts occur at the cytoplasmic face. These conformational changes lead to a dissociation of the G‐protein from the receptor, which then initiates a signaling cascade. The Hostos‐Lincoln Academy SMART team (Students Modeling A Research Topic) modeled ligands in complex with β 2 AR using 3D printing technology. Supported by grants from the HHMI Precollege Program and the Camille and Henry Dreyfus Foundation.