Results 1 to 10 of about 2,474,871 (249)

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
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LPA₃: Pharmacodynamic Differences Between Lysophosphatidic Acid and Oleoyl-Methoxy Glycerophosphothionate: Biased Agonism, Two Sites

Receptors
Background: Lysophosphatidic acid (LPA) receptor 3 (LPA3) is involved in many physiological and pathophysiological actions of this bioactive lipid, particularly in cancer.
K. Helivier Solís, M. Teresa Romero-Ávila, Ruth Rincón-Heredia, Juan Carlos Martínez-Morales, J. Adolfo García-Sáinz   +4 more
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Receptor-Based Strategies for Overcoming Resistance in Cancer Therapy

Receptors
This review article explores the fundamental role of receptor targeting in overcoming drug resistance in cancer therapy, an area of critical concern given the persistently high rates of cancer morbidity and mortality globally.
Naresh Sah, Abdul Althaf Shaik, Ganesh Acharya, Manikantha Dunna, Ashok Silwal, Sejal Sharma, Sabiha Khan, Sounak Bagchi   +7 more
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Role of Transient Receptor Potential Vanilloid Channels in Gastrointestinal Physiology and Pathology

Receptors
Transient Receptor Potential Vanilloid (TRPV) channels represent one of the seven subfamilies of TRP receptors and are widely expressed throughout the human body where they play pivotal roles in various physiological processes.
Omar Tluli, Ahmed Arabi, Humam Emad Rajha, Lana Abugharbieh, Faissal Al Zeir, Maryam Hamdan, Ayeda Abuqaba, Ammar Boudaka   +7 more
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RNase P-Associated External Guide Sequences Inhibit HIV-1 Infection by Shutting Down Human CCR5 Expression

Receptors
Background: External guide sequences (EGSs) are small RNA molecules capable of hybridizing to a target mRNA and rendering the target RNA susceptible to degradation by ribonuclease P (RNase P), a tRNA processing enzyme.
Yujun Liu, Bin Yan, Isadora Zhang, Fenyong Liu   +3 more
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Role of Glucocorticoid Receptor in Triple-Negative Breast Cancer

Receptors
Triple-negative breast cancer (TNBC) is an aggressive tumor among breast cancer subtypes with much lower overall survival at metastasis compared to other subtypes and with limited treatment options due to a lack of targeted therapies. This has led to the
Raj Kumar
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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
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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
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Non-Metabolic Functions of PKM2 Contribute to Cervical Cancer Cell Proliferation Induced by the HPV16 E7 Oncoprotein

Viruses, 2021
Pyruvate kinase M2 (PKM2) mainly catalyzes glycolysis, but it also exerts non-glycolytic functions in several cancers. While it has been shown to interact with the human papillomavirus 16 (HPV16) E7 oncoprotein, the functional significance of PKM2 in HPV-
Seoung-Ae Lee, Charles Ho, Madison Troxler, Chin-Yo Lin, Sang-Hyuk Chung   +4 more
doaj   +1 more source