Premium
Beta‐2 adrenergic receptor: a SMART team modeling project (LB106)
Author(s) -
Ellingwood Lexy Ellingwood,
Sanders Mitchell,
Sanders Katie Sanders,
Vinod Anjan,
Wang James,
Wang John,
Link Tina,
Zhu Mengyuan Zhu
Publication year - 2014
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.28.1_supplement.lb106
Subject(s) - bronchoconstriction , bronchodilation , g protein coupled receptor , agonist , receptor , chemistry , biophysics , asthma , medicine , biology , biochemistry , bronchodilator
Asthma is a condition that affects millions. In response to allergens, the smooth muscles surrounding the lungs undergo bronchoconstriction which reduces the amount of air accessible. Bronchoconstriction can be countered by bronchodilation which results from the side effects of Beta‐2 adrenergic receptor (b2AR) antagonists. B2AR is a type of G protein coupled receptors (GPCRs) that bind to a drug like salmeterol and induce a conformational change that activates signal transduction in the cell that results in the relaxation of smooth muscle in the lungs. In 2012, Brian Kobilka and Bob Lefkowitz received a Nobel prize for their biochemical analysis and structural determination of b2AR. Kobilka used the T4 lysozyme to stabilize the protein and create a clearer view of the protein. The critical residues for agonist binding are Phe290, Asp113, Ser207, Ser203, Asn312 and Phe193. The Walton SMART Team (Students Modeling A Research Topic) modeled the b2AR using 3D printing technology demonstrating the interaction profile between the high affinity agonist BI‐167107 that stabilizes the active state of b2AR. Grant Funding Source : Supported by grants from the NIH‐SEPA and NIH‐CTSA.