GRK Mediates μ-Opioid Receptor Plasma Membrane Reorganization
Frontiers in Molecular Neuroscience, 2019 Differential regulation of the μ-opioid receptor (MOP) has been linked to the development of opioid tolerance and dependence which both limit the clinical use of opioid analgesics.
Arisbel B. Gondin +8 more
doaj +1 more source
Genetically Encoded Photo-cross-linkers Map the Binding Site of an Allosteric Drug on a G Protein-Coupled Receptor [PDF]
, 2012 G protein-coupled receptors (GPCRs) are dynamic membrane proteins that bind extracellular molecules to transduce signals. Although GPCRs represent the largest class of therapeutic targets, only a small percentage of their ligand-binding sites are ...
Abrol, Ravinder +5 more
core +1 more source
Nuclear receptors: recent drug discovery for cancer therapies.
Endocrine reviews, 2019 Nuclear receptors (NRs) are transcription factors actively involved in many aspects of human physiology and pathology, serving as sensors of stimuli, master regulators of downstream molecular events and hubs governing complex gene regulatory networks ...
Linjie Zhao +2 more
semanticscholar +1 more source
Receptor-mediated targeting of magnetic nanoparticles using insulin as a surface ligand to prevent endocytosis [PDF]
, 2003 Superparamagnetic iron oxide nanoparticles have been used for many years as magnetic resonance imaging contrast agents or in drug delivery applications.
Berry, C.C. +3 more
core +1 more source
Customizing the therapeutic response of signaling networks to promote antitumor responses by drug combinations [PDF]
, 2014 Drug resistance, de novo and acquired, pervades cellular signaling networks (SNs) from one signaling motif to another as a result of cancer progression and/or drug intervention.
Bown, James L. +4 more
core +3 more sources
Adhesion G Protein-Coupled Receptors as Drug Targets.
Annual Review of Pharmacology and Toxicology, 2018 The adhesion G protein-coupled receptors (aGPCRs) are an evolutionarily ancient family of receptors that play key roles in many different physiological processes.
Ryan H Purcell, Randy A. Hall
semanticscholar +1 more source
Molecular Simulations and Drug Discovery of Adenosine Receptors
Molecules, 2022 G protein-coupled receptors (GPCRs) represent the largest family of human membrane proteins. Four subtypes of adenosine receptors (ARs), the A1AR, A2AAR, A2BAR and A3AR, each with a unique pharmacological profile and distribution within the tissues in ...
Jinan Wang +4 more
doaj +1 more source
Structure-Function Analyses of Human Bitter Taste Receptors—Where Do We Stand?
Molecules, 2020 The finding that bitter taste receptors are expressed in numerous tissues outside the oral cavity and fulfill important roles in metabolic regulation, innate immunity and respiratory control, have made these receptors important targets for drug discovery.
Maik Behrens, Florian Ziegler
doaj +1 more source
Clinical trials with endothelin receptor antagonists: What went wrong and where can we improve? [PDF]
, 2012 In the early 1990s, within three years of cloning of endothelin receptors, orally active endothelin receptor antagonists (ERAs) were tested in humans and the first clinical trial of ERA therapy in humans was published in 1995.
Barton, Matthias +4 more
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Pregnane Xenobiotic Receptors and Their Effect on Drug Elimination from the Organism
Prague Medical Report, 2013 Nuclear receptors are intracellular proteins which, having been activated by their more or less specific ligands, regulate (usually increase) the transcription of target genes.
Martin Šíma, I. Netíková, O. Slanař
doaj +1 more source