Development of a membrane-based Gi-CASE biosensor assay for profiling compounds at cannabinoid receptors

Autor: Morgan Scott-Dennis, Fikri A. Rafani, Yicheng Yi, Themiya Perera, Clare R. Harwood, Wolfgang Guba, Arne C. Rufer, Uwe Grether, Dmitry B. Veprintsev, David A. Sykes

Publikováno v: Frontiers in Pharmacology, Vol 14 (2023)

Introduction: The cannabinoid receptor (CBR) subtypes 1 (CB1R) and 2 (CB2R) are key components of the endocannabinoid system (ECS), playing a central role in the control of peripheral pain, inflammation and the immune response, with further roles in

Externí odkaz: https://doaj.org/article/bd3b602001cb48838825a2f74ab966f7

The Heteromeric Complex Formed by Dopamine Receptor D5 and CCR9 Leads the Gut Homing of CD4+ T Cells Upon InflammationSummary

Autor: Gemma Navarro, Alvaro Lladser, Javier Campos, Alexandra Espinoza, Francisco Contreras, Carolina Prado, Iu Raïch, Rodrigo Pacheco, Rafael Franco, Francisco Osorio-Barrios, Ernesto Lopez, Valentina Ugalde

Publikováno v: Cellular and Molecular Gastroenterology and Hepatology, Vol 12, Iss 2, Pp 489-506 (2021)
Cellular and Molecular Gastroenterology and Hepatology

Background and aims: CD4+ T cells constitute central players in inflammatory bowel diseases (IBDs), driving inflammation in the gut mucosa. Current evidence indicates that CCR9 and the integrin α4β7 are necessary and sufficient to imprint colonic h

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17853d8965fd2dd62836241f51298962
http://www.sciencedirect.com/science/article/pii/S2352345X21000771

Characterization of a new WHIM syndrome mutant reveals mechanistic differences in regulation of the chemokine receptor CXCR4

Autor: Jiansong Luo, Francesco De Pascali, G. Wendell Richmond, Amer M. Khojah, Jeffrey L. Benovic

Publikováno v: The Journal of Biological Chemistry

WHIM syndrome is a rare immunodeficiency disorder that is characterized by warts, hypogammaglobulinemia, infections, and myelokathexis. While several gain-of-function mutations that lead to C-terminal truncations, frame shifts and point mutations in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::95b634ebbacc2f86578bb047be09302d
http://europepmc.org/articles/PMC8802859

Synthesis and biological studies of new piperidino-1,2,3-triazole hybrids with 3-aryl isoxazole side chains

Autor: Vennu Narendar, Philippe Juin, A. K. D. Bhavani, Rémy Le Guével, Fabien Gautier, Appala Venkata Ramana Murthy, Nicolas Levoin, Nangunoori Sampath Kumar, René Grée, Chada Raji Reddy, Paul Mosset, Hélène Solhi, Pasula Aparna, Julie Roul

Publikováno v: Bioorganic & Medicinal Chemistry Letters
Bioorganic & Medicinal Chemistry Letters, 2021, 52, pp.128390. ⟨10.1016/j.bmcl.2021.128390⟩

International audience; A small library of new piperidine-triazole hybrids with 3-aryl isoxazole side chains has been designed and synthesized. Their cytotoxicity against a panel of seven cancer cell lines has been established. For the most promising

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ae63b759b6b3265e31ade8013c76432d
https://hal.archives-ouvertes.fr/hal-03414697/document

Lipidated peptides derived from intracellular loops 2 and 3 of the urotensin II receptor act as biased allosteric ligands

Autor: Alain Fournier, Bruce G. Allen, Tuan Anh Hoang, Terence E. Hébert, Ryan D. Martin, Alfonso Carotenuto, Juliana C. C. Dallagnol, Myriam Létourneau, Hassan Nassour, David Chatenet, Étienne Billard, Jason C. Tanny, Ettore Novellino

Publikováno v: The Journal of Biological Chemistry

Over the last decade, the urotensinergic system, composed of one G protein-coupled receptor and two endogenous ligands, has garnered significant attention as a promising new target for the treatment of various cardiovascular diseases. Indeed, this sy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::31fe3abca6a81eb53384d871fe901993
http://europepmc.org/articles/PMC8424217