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Vol. 61, Issue 5, 1025-1032, May 2002
1b-Adrenergic
Receptor Highlight the Role of the Helix 3/Helix 6 Interface in
Receptor Activation
Institut de Pharmacologie et Toxicologie, Université de
Lausanne, Lausanne, Switzerland (P.J.G., O.R., L.A., S.C.); and
Dipartimento di Chimica, Università di Modena e Reggio Emilia,
Modena, Italy (F.F.)
Computer simulations on a new model of the 
1b-adrenergic receptor
based on the crystal structure of rhodopsin have been combined with
experimental mutagenesis to investigate the role of residues in the
cytosolic half of helix 6 in receptor activation. Our results support
the hypothesis that a salt bridge between the highly conserved arginine
(R1433.50) of the E/DRY motif of helix 3 and a conserved
glutamate (E2896.30) on helix 6 constrains the 1b-AR in
the inactive state. In fact, mutations of E2896.30 that
weakened the R1433.50-E2896.30 interaction
constitutively activated the receptor. The functional effect of
mutating other amino acids on helix 6 (F2866.27,
A2926.33, L2966.37, V2996.40,
V3006.41, and F3036.44) correlates with the
extent of their interaction with helix 3 and in particular with
R1433.50 of the E/DRY sequence.
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