2-Furoyl-LIGRLO-amide

A potent and selective proteinase-activated receptor 2 agonist

John J. McGuire, Mahmoud Saifeddine, Christopher Triggle, Kimberly Sun, Morley D. Hollenberg

Research output: Contribution to journalArticle

97 Citations (Scopus)

Abstract

A peptide corresponding to a proteinase-activated receptor 2 (PAR 2)-activating peptide with an N-terminal furoyl group modification, 2-furoyl-LIGRLO-NH2, was assessed for PAR2-dependent and -independent biological activities. 2-Furoyl-LIGRLO-NH2 was equally effective to and 10 to 25 times more potent than SLIGRL-NH2 for increasing intracellular calcium in cultured human and rat PAR 2-expressing cells, respectively. In bioassays of tissue PAR 2 activity, measured as arterial vasodilation and hyperpolarization, 2-furoyl-LIGRLO-NH2 was 10 to 300 times more potent than SLIGRL-NH2. Unlike trans-cinnamoyl-LIGRLO-NH2, 2-furoyl-LIGRLO-NH2 did not cause a prominent non-PAR 2-mediated contraction of murine femoral arteries. In conclusion, 2-furoyl-LIGRLO-NH2 represents the most potent and selective activator of PAR2 in biological systems described to date.

Original languageEnglish
Pages (from-to)1124-1131
Number of pages8
JournalJournal of Pharmacology and Experimental Therapeutics
Volume309
Issue number3
DOIs
Publication statusPublished - Jun 2004
Externally publishedYes

Fingerprint

PAR-2 Receptor
Peptides
Femoral Artery
Vasodilation
Biological Assay
Calcium
2-furoyl-LIGRLO-amide
seryl-leucyl-isoleucyl-glycyl--arginyl-leucinamide

ASJC Scopus subject areas

  • Pharmacology

Cite this

2-Furoyl-LIGRLO-amide : A potent and selective proteinase-activated receptor 2 agonist. / McGuire, John J.; Saifeddine, Mahmoud; Triggle, Christopher; Sun, Kimberly; Hollenberg, Morley D.

In: Journal of Pharmacology and Experimental Therapeutics, Vol. 309, No. 3, 06.2004, p. 1124-1131.

Research output: Contribution to journalArticle

McGuire, John J. ; Saifeddine, Mahmoud ; Triggle, Christopher ; Sun, Kimberly ; Hollenberg, Morley D. / 2-Furoyl-LIGRLO-amide : A potent and selective proteinase-activated receptor 2 agonist. In: Journal of Pharmacology and Experimental Therapeutics. 2004 ; Vol. 309, No. 3. pp. 1124-1131.
@article{8101bc72900a4826a8150a002d72f456,
title = "2-Furoyl-LIGRLO-amide: A potent and selective proteinase-activated receptor 2 agonist",
abstract = "A peptide corresponding to a proteinase-activated receptor 2 (PAR 2)-activating peptide with an N-terminal furoyl group modification, 2-furoyl-LIGRLO-NH2, was assessed for PAR2-dependent and -independent biological activities. 2-Furoyl-LIGRLO-NH2 was equally effective to and 10 to 25 times more potent than SLIGRL-NH2 for increasing intracellular calcium in cultured human and rat PAR 2-expressing cells, respectively. In bioassays of tissue PAR 2 activity, measured as arterial vasodilation and hyperpolarization, 2-furoyl-LIGRLO-NH2 was 10 to 300 times more potent than SLIGRL-NH2. Unlike trans-cinnamoyl-LIGRLO-NH2, 2-furoyl-LIGRLO-NH2 did not cause a prominent non-PAR 2-mediated contraction of murine femoral arteries. In conclusion, 2-furoyl-LIGRLO-NH2 represents the most potent and selective activator of PAR2 in biological systems described to date.",
author = "McGuire, {John J.} and Mahmoud Saifeddine and Christopher Triggle and Kimberly Sun and Hollenberg, {Morley D.}",
year = "2004",
month = "6",
doi = "10.1124/jpet.103.064584",
language = "English",
volume = "309",
pages = "1124--1131",
journal = "Journal of Pharmacology and Experimental Therapeutics",
issn = "0022-3565",
publisher = "American Society for Pharmacology and Experimental Therapeutics",
number = "3",

}

TY - JOUR

T1 - 2-Furoyl-LIGRLO-amide

T2 - A potent and selective proteinase-activated receptor 2 agonist

AU - McGuire, John J.

AU - Saifeddine, Mahmoud

AU - Triggle, Christopher

AU - Sun, Kimberly

AU - Hollenberg, Morley D.

PY - 2004/6

Y1 - 2004/6

N2 - A peptide corresponding to a proteinase-activated receptor 2 (PAR 2)-activating peptide with an N-terminal furoyl group modification, 2-furoyl-LIGRLO-NH2, was assessed for PAR2-dependent and -independent biological activities. 2-Furoyl-LIGRLO-NH2 was equally effective to and 10 to 25 times more potent than SLIGRL-NH2 for increasing intracellular calcium in cultured human and rat PAR 2-expressing cells, respectively. In bioassays of tissue PAR 2 activity, measured as arterial vasodilation and hyperpolarization, 2-furoyl-LIGRLO-NH2 was 10 to 300 times more potent than SLIGRL-NH2. Unlike trans-cinnamoyl-LIGRLO-NH2, 2-furoyl-LIGRLO-NH2 did not cause a prominent non-PAR 2-mediated contraction of murine femoral arteries. In conclusion, 2-furoyl-LIGRLO-NH2 represents the most potent and selective activator of PAR2 in biological systems described to date.

AB - A peptide corresponding to a proteinase-activated receptor 2 (PAR 2)-activating peptide with an N-terminal furoyl group modification, 2-furoyl-LIGRLO-NH2, was assessed for PAR2-dependent and -independent biological activities. 2-Furoyl-LIGRLO-NH2 was equally effective to and 10 to 25 times more potent than SLIGRL-NH2 for increasing intracellular calcium in cultured human and rat PAR 2-expressing cells, respectively. In bioassays of tissue PAR 2 activity, measured as arterial vasodilation and hyperpolarization, 2-furoyl-LIGRLO-NH2 was 10 to 300 times more potent than SLIGRL-NH2. Unlike trans-cinnamoyl-LIGRLO-NH2, 2-furoyl-LIGRLO-NH2 did not cause a prominent non-PAR 2-mediated contraction of murine femoral arteries. In conclusion, 2-furoyl-LIGRLO-NH2 represents the most potent and selective activator of PAR2 in biological systems described to date.

UR - http://www.scopus.com/inward/record.url?scp=2442702842&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=2442702842&partnerID=8YFLogxK

U2 - 10.1124/jpet.103.064584

DO - 10.1124/jpet.103.064584

M3 - Article

VL - 309

SP - 1124

EP - 1131

JO - Journal of Pharmacology and Experimental Therapeutics

JF - Journal of Pharmacology and Experimental Therapeutics

SN - 0022-3565

IS - 3

ER -