Small molecule ligands for α9 * and α7 nicotinic receptors: A survey and an update, respectively

Autor: Alessandro Giraudo, Marco Pallavicini, Cristiano Bolchi

Publikováno v: Pharmacological Research, Vol 193, Iss , Pp 106801- (2023)

The α9- and α7-containing nicotinic acetylcholine receptors (nAChRs) mediate numerous physiological and pathological processes by complex mechanisms that are currently the subject of intensive study and debate. In this regard, selective ligands ser

Externí odkaz: https://doaj.org/article/f7a0e677e297462eb22177cef254b91c

Molecular Mingling: Multimodal Predictions of Ligand Promiscuity in Pentameric Ligand-Gated Ion Channels

Autor: Filip Koniuszewski, Florian D. Vogel, Konstantina Bampali, Jure Fabjan, Thomas Seidel, Petra Scholze, Philip B. Schmiedhofer, Thierry Langer, Margot Ernst

Publikováno v: Frontiers in Molecular Biosciences, Vol 9 (2022)

Background: Human pentameric ligand-gated ion channels (pLGICs) comprise nicotinic acetylcholine receptors (nAChRs), 5-hydroxytryptamine type 3 receptors (5-HT3Rs), zinc-activated channels (ZAC), γ-aminobutyric acid type A receptors (GABAARs) and gl

Externí odkaz: https://doaj.org/article/dc54f068c3bd491a9c80831d692e9b36

Allosteric Cannabinoid Receptor 1 (CB1) Ligands Reduce Ocular Pain and Inflammation

Autor: Dinesh Thapa, Elizabeth A. Cairns, Anna-Maria Szczesniak, Pushkar M. Kulkarni, Alex J. Straiker, Ganesh A. Thakur, Melanie E. M. Kelly

Publikováno v: Molecules, Vol 25, Iss 2, p 417 (2020)

Cannabinoid receptor 1 (CB1) activation has been reported to reduce transient receptor potential cation channel subfamily V member 1 (TRPV1)-induced inflammatory responses and is anti-nociceptive and anti-inflammatory in corneal injury. We examined w

Externí odkaz: https://doaj.org/article/5491ec7caf8a4f16b8f314dcc731ee7d

Pharmacological Characterization of Low Molecular Weight Biased Agonists at the Follicle Stimulating Hormone Receptor

Autor: De Pascali, Francesco, Ayoub, Mohammed, Benevelli, Riccardo, Sposini, Silvia, Lehoux, Jordan, Gallay, Nathalie, Raynaud, Pauline, Landomiel, Flavie, Jean-Alphonse, Frédéric, Gauthier, Christophe, Pellissier, Lucie P., Crepieux, Pascale, Poupon, Anne, Inoue, Asuka, Joubert, Nicolas, Viaud-Massuard, Marie-Claude, Casarini, Livio, Simoni, Manuela, Hanyaloglu, Aylin, Nataraja, Selva, Yu, Henry, Palmer, Stephen, Yvinec, Romain, Reiter, Eric

Publikováno v: International Journal of Molecular Sciences
International Journal of Molecular Sciences, Vol 22, Iss 9850, p 9850 (2021)
International Journal of Molecular Sciences, MDPI, 2021, 22 (18), pp.1-23. ⟨10.3390/ijms22189850⟩
Volume 22
Issue 18
International Journal of Molecular Sciences, 2021, 22 (18), pp.1-23. ⟨10.3390/ijms22189850⟩

International audience; Follicle-stimulating hormone receptor (FSHR) plays a key role in reproduction through the activation of multiple signaling pathways. Low molecular weight (LMW) ligands composed of biased agonist properties are highly valuable

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::92cf3951a9cf331b14edf110b692902b
http://europepmc.org/articles/PMC8469697

Ligand Docking Methods to Recognize Allosteric Inhibitors for G-Protein-Coupled Receptors

Autor: S Jayashree, Vikas Tiwari, K. Harini, Sneha Vishwanath, Ramanathan Sowdhamini

Publikováno v: Bioinformatics and Biology Insights
Bioinformatics and Biology Insights, Vol 15 (2021)

G-protein-coupled receptors (GPCRs) are membrane proteins which play an important role in many cellular processes and are excellent drug targets. Despite the existence of several US Food and Drug Administration (FDA)-approved GPCR-targeting drugs, th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2065c4dfcc2e5213d4707d2d975b6cd
http://europepmc.org/articles/PMC8558589