High Affinity Fluorescent Probe for Proteinase-Activated Receptor 2 (PAR2).


Journal

ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073

Informations de publication

Date de publication:
11 Jul 2019
Historique:
received: 07 03 2019
accepted: 06 06 2019
entrez: 18 7 2019
pubmed: 18 7 2019
medline: 18 7 2019
Statut: epublish

Résumé

PAR2 is a proteolytically activated G protein-coupled receptor (GPCR) that is implicated in various cancers and inflammatory diseases. Ligands with low nanomolar affinity for PAR2 have been developed, but there is a paucity of research on the development of PAR2-targeting imaging probes. Here, we report the development of seven novel PAR2-targeting compounds. Four of these compounds are highly potent and selective PAR2-targeting peptides (EC

Identifiants

pubmed: 31312406
doi: 10.1021/acsmedchemlett.9b00094
pmc: PMC6627725
doi:

Types de publication

Journal Article

Langues

eng

Pagination

1045-1050

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

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Auteurs

Jordan C LeSarge (JC)

Department of Chemistry, Department of Physiology and Pharmacology, Department of Oncology, and Department of Medical Imaging, University of Western Ontario, 1151 Richmond Street, London, Ontario N6A 3K7, Canada.

Pierre Thibeault (P)

Department of Chemistry, Department of Physiology and Pharmacology, Department of Oncology, and Department of Medical Imaging, University of Western Ontario, 1151 Richmond Street, London, Ontario N6A 3K7, Canada.

Mark Milne (M)

London Regional Cancer Program, Lawson Health Research Institute, 800 Commissioners Road East, London, Ontario N6A 5W9, Canada.

Rithwik Ramachandran (R)

Department of Chemistry, Department of Physiology and Pharmacology, Department of Oncology, and Department of Medical Imaging, University of Western Ontario, 1151 Richmond Street, London, Ontario N6A 3K7, Canada.

Leonard G Luyt (LG)

Department of Chemistry, Department of Physiology and Pharmacology, Department of Oncology, and Department of Medical Imaging, University of Western Ontario, 1151 Richmond Street, London, Ontario N6A 3K7, Canada.
Department of Chemistry, Department of Physiology and Pharmacology, Department of Oncology, and Department of Medical Imaging, University of Western Ontario, 1151 Richmond Street, London, Ontario N6A 3K7, Canada.
Department of Chemistry, Department of Physiology and Pharmacology, Department of Oncology, and Department of Medical Imaging, University of Western Ontario, 1151 Richmond Street, London, Ontario N6A 3K7, Canada.
London Regional Cancer Program, Lawson Health Research Institute, 800 Commissioners Road East, London, Ontario N6A 5W9, Canada.

Classifications MeSH