NDLI: Cell-Penetrating Mimics of Agonist-Activated G-Protein Coupled Receptors

Content Provider	Springer Nature Link
Author	Östlund, Pernilla Kilk, Kalle Lindgren, Maria Hällbrink, Mattias Jiang, Yang Budihna, Metka Cerne, Katarina Bavec, Aljosa Östenson, Claes Göran Zorko, Matjaz Langel, Ülo
Copyright Year	2005
Abstract	Cell-penetrating peptides have proven themselves as valuable vectors for intracellular delivery. Relatively little is known about the frequency of cell-penetrating sequences in native proteins and their functional role. By computational comparison of peptide sequences, we recently predicted that intracellular loops of G-protein coupled receptors (GPCR) have high probability for occurrence of cell-penetrating motifs. Since the loops are also receptor and G-protein interaction sites, we postulated that the short cell-penetrating peptides, derived from GPCR, when applied extracellularly can pass the membrane and modulate G-protein activity similarly to parent receptor proteins. Two model systems were analyzed as proofs of the principle. A peptide based on the C-terminal intracellular sequence of the rat angiotensin receptor (AT1AR) is shown to internalize into live cells and elicit blood vessel contraction even in the presence of AT1AR antagonist Sar$^{1}$-Thr$^{8}$-angiotensin II. The peptide interacts with the same selectivity towards G-protein subtypes as agonist-activated AT1AR and blockade of phospholipase C abolishes its effect. Another cell-penetrating peptide, G53-2 derived from human glucagon-like peptide receptor (GLP-1R) is shown to induce insulin release from isolated pancreatic islets. The mechanism was again found to be shared with the original GLP-1R, namely G$_{11}$-mediated inositol 1,4,5-triphosphate release pathway. These data reveal a novel possibility to mimic the effects of signalling transmembrane proteins by application of shorter peptide fragments.
Starting Page	237
Ending Page	247
Page Count	11
File Format	PDF
ISSN	15733149
Journal	International Journal of Peptide Research and Therapeutics
Volume Number	11
Issue Number	4
e-ISSN	15733904
Language	English
Publisher	Kluwer Academic Publishers-Plenum Publishers
Publisher Date	2005-01-01
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Angiotensin cell-penetrating peptide glucagon-like peptide 1 G-protein coupled receptors signal transduction Polymer Sciences Biochemistry Animal Anatomy / Morphology / Histology
Content Type	Text
Resource Type	Article
Subject	Analytical Chemistry Drug Discovery Biochemistry Molecular Medicine Bioengineering

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4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
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