NDLI: Activation of Adhesion G Protein-coupled Receptors AGONIST SPECIFICITY OF STACHEL SEQUENCE-DERIVED PEPTIDES

Content Provider	Journal of Biological Chemistry (JBC)
Author	Demberg, Lilian M. Winkler, Jana Wilde, Caroline Simon, Kay-Uwe Schön, Julia Rothemund, Sven Schöneberg, Torsten Prömel, Simone Liebscher, Ines
Abstract	Members of the adhesion G protein-coupled receptor (aGPCR) family carry an agonistic sequence within their large ectodomains. Peptides derived from this region, called the Stachel sequence, can activate the respective receptor. As the conserved core region of the Stachel sequence is highly similar between aGPCRs, the agonist specificity of Stachel sequence-derived peptides was tested between family members using cell culture-based second messenger assays. Stachel peptides derived from aGPCRs of subfamily VI (GPR110/ADGRF1, GPR116/ADGRF5) and subfamily VIII (GPR64/ADGRG2, GPR126/ADGRG6) are able to activate more than one member of the respective subfamily supporting their evolutionary relationship and defining them as pharmacological receptor subtypes. Extended functional analyses of the Stachel sequences and derived peptides revealed agonist promiscuity, not only within, but also between aGPCR subfamilies. For example, the Stachel-derived peptide of GPR110 (subfamily VI) can activate GPR64 and GPR126 (both subfamily VIII). Our results indicate that key residues in the Stachel sequence are very similar between aGPCRs allowing for agonist promiscuity of several Stachel-derived peptides. Therefore, aGPCRs appear to be pharmacologically more closely related than previously thought. Our findings have direct implications for many aGPCR studies, as potential functional overlap has to be considered for in vitro and in vivo studies. However, it also offers the possibility of a broader use of more potent peptides when the original Stachel sequence is less effective.
Related Links	http://www.jbc.org/content/292/11/4383.abstract
Ending Page	4394
Starting Page	4383
Page Count	12
File Format	HTM / HTML PDF
ISSN	00219258
Journal	Journal of Biological Chemistry (JBC)
Issue Number	11
Volume Number	292
DOI	10.1074/jbc.M116.763656
e-ISSN	1083351X
Language	English
Publisher	American Society for Biochemistry and Molecular Biology
Publisher Date	2017-03-17
Access Restriction	Open
Subject Keyword	Adhesion Cyclic AMP (cAMP) G protein G protein-coupled receptor (GPCR) Inositol phosphate NFAT transcription factor Peptides Signal transduction Signal Transduction
Alternative Title	Activation of Adhesion G Protein-coupled Receptors
Content Type	Text
Resource Type	Article
Subject	Cell Biology Biochemistry Molecular Biology

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