Proceedings of the National Academy of Sciences · 1994 · 887 citations · 14 references
Life SciencesBiochemistryMolecular BiologyCell SignalingGene ExpressionSignal TransductionCell-surface ReceptorsG Protein-coupled Receptor SignalingLigand BindingMembrane ReceptorsReceptor-ligand InteractionsReceptor-mediated SignalingAgonist ActivityCleavage Site IdentificationDna Sequence AnalysisG Protein-coupled Receptor ActivationG Protein-coupled Receptor BindingG-protein-coupled ReceptorsReceptor-g Protein CouplingReceptors
A DNA sequence encoding a G-protein-coupled receptor was isolated from a mouse genomic library. The predicted protein is similar in structure to the thrombin receptor and has a similar activation mechanism. When expressed in Xenopus laevis oocytes, the receptor was activated by low concentrations of trypsin (EC 3.4.21.4) and by a peptide (SLIGRL) derived from the receptor sequence, but was not activated by thrombin (EC 3.4.21.5). Trypsin failed to activate a mutant receptor in which the presumed cleavage site Arg-34-Ser-35 was changed to an Arg-Pro sequence. The agonist peptide (SLIGRL) activated equally well mutant and wild-type receptors. Northern blot analysis demonstrated receptor transcripts in highly vascularized tissues such as kidney, small intestine, and stomach. Because this, to our knowledge, is the second example, besides the thrombin receptor, of a proteolytically activated seven-transmembrane G-protein-coupled receptor, we have provisionally named it proteinase activated receptor 2.
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A comprehensive set of sequence analysis programs for the VAX
John Devereux, Paul Haeberli, Oliver Smithies · Nucleic Acids Research · 1984 · 14.4K citations · Full text
cDNA eloping of bovine substance-K receptor through oocyte expression system
Yasuo Masu, Kazuhisa Nakayama, Hiromi Tamaki et al. · Nature · 1987 · 743 citations