GPCR Engineering Yields High-Resolution Structural Insights into β2-Adrenergic Receptor Function

  title={GPCR Engineering Yields High-Resolution Structural Insights into β2-Adrenergic Receptor Function},
  author={D. Rosenbaum and V. Cherezov and M. Hanson and S{\o}ren G. F. Rasmussen and Foon Sun Thian and T. S. Kobilka and Hee-Jung Choi and Xiao-Jie Yao and W. Weis and R. Stevens and B. Kobilka},
  pages={1266 - 1273}
  • D. Rosenbaum, V. Cherezov, +8 authors B. Kobilka
  • Published 2007
  • Chemistry, Medicine
  • Science
  • The β2-adrenergic receptor (β2AR) is a well-studied prototype for heterotrimeric guanine nucleotide–binding protein (G protein)–coupled receptors (GPCRs) that respond to diffusible hormones and neurotransmitters. To overcome the structural flexibility of the β2AR and to facilitate its crystallization, we engineered a β2AR fusion protein in which T4 lysozyme (T4L) replaces most of the third intracellular loop of the GPCR (“β2AR-T4L”) and showed that this protein retains near-native pharmacologic… CONTINUE READING
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