9.A.14.3.5 β-2 adrenergic receptor, β2-AR. Activates adenylate cyclase through G proteins. Binds epinephrine with 30x greater affinity than norepenephrine. Functions as an ATP-independent phospholipid flippase (scramblase) (Goren et al. 2014). A parameterized MARTINI program can be used to predict the hinging motions of the protein (Li et al. 2019). The drugs, salmeterol, formoterol and salbutamol, constitute the frontline treatment for asthma and other chronic pulmonary diseases. These drugs activate beta2-AR, and differ significantly in their clinical onset and durations of actions. Membrane lipids facilitate access and binding of the ligands, affecting their molecular recognition and pharmacology (Li et al. 2019). The drugs, salmeterol, formoterol and salbutamol, constitute the frontline treatment for asthma and other chronic pulmonary diseases. These drugs activate beta2-AR, and differ significantly in their clinical onset and durations of actions. Membrane lipids facilitate access and binding of the ligands, affecting their molecular recognition and pharmacology (Szlenk et al. 2021).
|
Accession Number: | P07550 |
Protein Name: | Beta-2 adrenergic receptor |
Length: | 413 |
Molecular Weight: | 46459.00 |
Species: | Homo sapiens (Human) [9606] |
Number of TMSs: | 7 |
Location1 / Topology2 / Orientation3: |
Cell membrane1 / Multi-pass membrane protein2 |
Substrate |
|
---|
1: MGQPGNGSAF LLAPNGSHAP DHDVTQERDE VWVVGMGIVM SLIVLAIVFG NVLVITAIAK
61: FERLQTVTNY FITSLACADL VMGLAVVPFG AAHILMKMWT FGNFWCEFWT SIDVLCVTAS
121: IETLCVIAVD RYFAITSPFK YQSLLTKNKA RVIILMVWIV SGLTSFLPIQ MHWYRATHQE
181: AINCYANETC CDFFTNQAYA IASSIVSFYV PLVIMVFVYS RVFQEAKRQL QKIDKSEGRF
241: HVQNLSQVEQ DGRTGHGLRR SSKFCLKEHK ALKTLGIIMG TFTLCWLPFF IVNIVHVIQD
301: NLIRKEVYIL LNWIGYVNSG FNPLIYCRSP DFRIAFQELL CLRRSSLKAY GNGYSSNGNT
361: GEQSGYHVEQ EKENKLLCED LPGTEDFVGH QGTVPSDNID SQGRNCSTND SLL