Results 1 to 10 of about 2,013,994 (317)

The desensitization pathway of GABAA receptors, one subunit at a time

Nature Communications, 2020
GABAA receptors mediate most inhibitory synaptic transmission in the brain. Here authors used concatemeric α1β2γ2 GABAA receptors to introduce gain-of-desensitization mutations one subunit at a time, revealing non-concerted rearrangements with a key ...
Marc Gielen, Nathalie Barilone, Pierre-Jean Corringer   +2 more
doaj   +1 more source

Combined docking and machine learning identify key molecular determinants of ligand pharmacological activity on β2 adrenoceptor

Pharmacology Research & Perspectives, 2022
G protein‐coupled receptors (GPCRs) are valuable therapeutic targets for many diseases. A central question of GPCR drug discovery is to understand what determines the agonism or antagonism of ligands that bind them.
Mireia Jiménez‐Rosés, Bradley Angus Morgan, Maria Jimenez Sigstad, Thuy Duong Zoe Tran, Rohini Srivastava, Asuman Bunsuz, Leire Borrega‐Román, Pattarin Hompluem, Sean A. Cullum, Clare R. Harwood, Eline J. Koers, David A. Sykes, Iain B. Styles, Dmitry B. Veprintsev   +13 more
doaj   +1 more source

Illumination of a progressive allosteric mechanism mediating the glycine receptor activation

Nature Communications, 2023
Glycine receptors are channel receptors mediating signal transduction between neurons that transit between resting and open states upon neurotransmitter binding.
Sophie Shi, Solène N. Lefebvre, Laurie Peverini, Adrien H. Cerdan, Paula Milán Rodríguez, Marc Gielen, Jean-Pierre Changeux, Marco Cecchini, Pierre-Jean Corringer   +8 more
doaj   +1 more source

Glycosyl Mobile Radical Structures of Folic Acid Receptors Impact the Internalization of Functionalized Folate Amphiphilic Alternating Copolymer in Cancer Cells

Receptors
Folate receptor alpha (FRα) is a glycosylphosphatidylinositol (GPI) membrane-anchored protein containing three N-glycosylated residues at the N47, N139, and N179 termini.
Emilyn B. Aucoin, Elizabeth Skapinker, Abdulrahman M. Yaish, Yunfan Li, Haley L. Kombargi, Daniel Jeyaraj, Pankaj Garg, Nicole Mendonza, Cecile Malardier-Jugroot, Myron R. Szewczuk   +9 more
doaj   +1 more source

Molecular Perspectives on Prostate Cancer: The Role of microRNAs in Androgen Receptor Regulation

Receptors
Prostate cancer (PCa) is the most prevalent cancer among men globally. In addition to environmental risk factors, genetic factors play a crucial role in its development and progression, highlighting the regulation of key genes as an essential aspect. The
Asbiel Felipe Garibaldi-Ríos, Alicia Rivera-Cameras, Luis E. Figuera, Guillermo Moisés Zúñiga-González, Belinda Claudia Gómez-Meda, José Elías García-Ortíz, Martha Patricia Gallegos-Arreola   +6 more
doaj   +1 more source

Systemic Chronic Inflammation: Integrative Strategies for Health Improvement and Prevention of Inflammatory Receptor Overexpression

Receptors
The body’s physiology during physical injuries and diseases depends heavily on the function of acute inflammation. On the other hand, many variables, including iatrogenic, immune system deficiencies, lifestyle, and social and environmental factors, are ...
Abraham Puga-Olguín, María Fernanda Hernández-Hernández, Rafael Fernández-Demeneghi, Carlos Iván López-Miranda, Luis Ángel Flores-Aguilar   +4 more
doaj   +1 more source

Unraveling the Role of CHRNA6, the Neuronal α6 Nicotinic Acetylcholine Receptor Subunit

Receptors
The increased prevalence of electronic cigarettes, particularly among adolescents, has escalated concerns about nicotine addiction. Nicotine, a potent psychostimulant found in tobacco products, exerts its effects by interacting with nicotinic ...
Yasamin Hajy Heydary, Emily M. Castro, Shahrdad Lotfipour, Frances M. Leslie   +3 more
doaj   +1 more source

Functional HER1/HER2-Expressing Murine Tumor Models for Preclinical Evaluation of Targeted Therapies

Receptors
Background: HER1 and HER2 are critical receptors involved in tumorigenesis and the development of targeted therapies for various carcinomas. However, most antibodies and drugs currently in development do not recognize murine orthologs, which restricts ...
Talia Fundora-Barrios, Amanda R. Hechavarría-Bajuelo, Lisset Chao García, Miguel Angel Gonzalez-Cruz, Najara Gonzalez-Suarez, Gretchen Bergado-Baez, Belinda Sánchez-Ramírez   +6 more
doaj   +1 more source

Odorant Receptors and Cancer

Receptors
Odorant receptors (ORs) constitute the largest family of G protein-coupled receptors (GPCRs), with nearly 400 receptors identified in humans. The “omics” era has revealed an unexpected expression of ORs beyond olfactory tissues.
Rafaella G. Naressi, Bettina Malnic, Luciana M. Gutiyama   +2 more
doaj   +1 more source

The Hidden Roles of Receptors in Intercellular Synchronization and Its Mathematical Generality

Receptors
Dictyostelium discoideum (Dicty) is a type of unicellular amoeba, but when starved, a large number of amoebas gather together to form a multicellular organism.
Seido Nagano
doaj   +1 more source