Results 61 to 70 of about 1,352 (160)

Progress on the development of Class A GPCR‐biased ligands

British Journal of Pharmacology, Volume 182, Issue 14, Page 3249-3300, July 2025.
Class A G protein‐coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and
Paula Morales, Magdalena M. Scharf, Marcel Bermudez, Attila Egyed, Rafael Franco, Olivia K. Hansen, Nadine Jagerovic, Jan Jakubík, György M. Keserű, Dóra Judit Kiss, Pawel Kozielewicz, Olav Larsen, Maria Majellaro, Ana Mallo‐Abreu, Gemma Navarro, Rubén Prieto‐Díaz, Mette M. Rosenkilde, Eddy Sotelo, Holger Stark, Tobias Werner, Laura M. Wingler   +20 more
wiley   +1 more source

Discovery, characterization and structure-activity relationships of an inhibitor of inward rectifier potassium (Kir) channels with preference for Kir2.3, Kir3.X and Kir7.1 [PDF]

, 2011
The inward rectifier family of potassium (Kir) channels is comprised of at least 16 family members exhibiting broad and often overlapping cellular, tissue or organ distributions.
Jerod S Denton, L. Michelle Lewis, Corey Hopkins, Thuy T. Nguyen, Rishin Kadakia, Craig W. Lindsley, Rene Raphemot, Rocco Gogliotti, Daniel F. Lonergan, Thomas Utley, C. David Weaver, Jerod S. Denton   +11 more
core   +1 more source

Discovery of an inward rectifying potassium channel inhibitor with preference for Kir2.3, Kir3.X and Kir7.1

The FASEB Journal, 2012
Inward rectifying potassium (Kir) channels play key physiological roles in diverse cell types and may represent novel drug targets for disease. In cardiac myocytes, Kir channels contribute to the resting membrane potential and the late repolarization phase of the action potential.
Rene Raphemot, Daniel Lonergan, Thuy T. Nguyen, Thomas J. Utley, Rocco Gogliotti, Corey R. Hopkins, Michelle Lewis, Craig W. Lindsley, C. David Weaver, Jerod S. Denton   +9 more
openaire   +1 more source

GABAB Receptor: Structure, Biological Functions, and Therapy for Diseases

MedComm, Volume 6, Issue 5, May 2025.
Within the GABAergic system, GABABRs are potential therapeutic targets for dealing multiple metabolic and binge eating disorders and food addiction. Allosteric modulators and small peptides targeting GABABR signaling pathways may be developed as attractive drug candidates that avoid the side effects of agents that directly bind these receptors ...
Weijie Xie, Yuan Li, Xinyue Wang, Elena Blokhina, Evgeny Krupitsky, Marina Vetrova, Ji Hu, Ti‐Fei Yuan, Jue Chen, Hua Wang, Xiangfang Chen   +10 more
wiley   +1 more source

Modulation of Kir3 by lipids and tyrosine phosphorylation

, 2000
Thesis (Ph. D.)--University of Washington, 2000Neurotransmitters, hormones and growth factors act on ion channels to modulate excitable tissue. When a ligand binds a receptor it may activate ion channels in the membrane to initiate multiple intracellular
Rogalski, Sherri Lynn
core  

Transient outward K+ current (ITO) reduction prolongs action potentials and promotes afterdepolarisations: a dynamic-clamp study in human and rabbit cardiac atrial myocytes [PDF]

, 2012
Background and aim: Human atrial transient outward K+ current (ITO) is decreased in a variety of cardiac pathologies, but how ITO reduction alters action potentials (AP) and arrhythmia mechanisms is poorly understood, owing to non-selectivity of ITO ...
Marshall, G.E., Dempster, J., Smith, G.L., Rankin, A.C., Workman, A.J.   +4 more
core   +1 more source

Ethosuximide: Subunit‐ and Gβγ‐dependent blocker and reporter of allosteric changes in GIRK channels

British Journal of Pharmacology, Volume 182, Issue 8, Page 1704-1718, April 2025.
Background and Purpose The antiepileptic drug ethosuximide (ETX) suppresses epileptiform activity in a mouse model of GNB1 syndrome, caused by mutations in Gβ1 protein, likely through the inhibition of G‐protein gated K+ (GIRK) channels. Here, we investigated the mechanism of ETX inhibition (block) of different GIRKs.
Boris Shalomov, Theres Friesacher, Daniel Yakubovich, J. Carlo Combista, Haritha P. Reddy, Shoham Dabbah, Harald Bernsteiner, Eva‐Maria Zangerl‐Plessl, Anna Stary‐Weinzinger, Nathan Dascal   +9 more
wiley   +1 more source

Conformational dynamics of KIR3.1/KIR3.2 channel activation via delta-opioid receptors (DORs)

, 2013
This study assessed how conformational information encoded by ligand binding to δ-opioid receptors (DORs) is transmitted to Kir3.1/Kir3.2 channels. HEK293 cells were transfected with bioluminescence resonance energy transfer (BRET) donor/acceptor pairs ...
RICHARD LALONDE M, AUDET N, AMRAEI M, HOGUE M, BALBONI, GIANFRANCO, PINEYRO G., SLENO R, HÉBERT T. E, BOUVIER M, SCHILLER P. W, NAGI K   +10 more
core   +1 more source

Artificial Compartments Encapsulating Enzymatic Reactions: Towards the Construction of Artificial Organelles

ChemPlusChem, Volume 90, Issue 2, February 2025.
This review article summarizes the cellular compartments, and the current progress of artificial compartments constructed by using liposomes, polymersomes, proteins, nucleic acids, and hybrid materials. The perspectives for the future development of artificial compartments towards the construction of artificial organelles or cells were discussed ...
Peng Lin, Shiwei Zhang, Futa Komatsubara, Hiroaki Konishi, Eiji Nakata, Takashi Morii   +5 more
wiley   +1 more source

Etude computationnelle de la relation structure-fonction des canaux Kir3 et application dans la conception de canaux Kir3 sensibles à la lumière

, 2019
This doctoral thesis focuses on a family of transmembrane proteins expressed as tetrameric assemblies which function as selective potassium ion channels – the potassium inward rectifier member 3 (Kir3).
Todorov, Zlatomir
core