In vitro and in vivo pharmacological activities of 14-o-phenylpropyloxymorphone, a potent mixed mu/delta/kappa-opioid receptor agonist with reduced constipation in mice [PDF]
, 2018 Pain, particularly chronic pain, is still an unsolved medical condition. Central goals in pain control are to provide analgesia of adequate efficacy and to reduce complications associated with the currently available drugs.
Lattanzi, Roberta +4 more
core +2 more sources
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
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
Systems analysis of drug-induced receptor tyrosine kinase reprogramming following targeted mono- and combination anti-cancer therapy [PDF]
, 2014 The receptor tyrosine kinases (RTKs) are key drivers of cancer progression and targets for drug therapy. A major challenge in anti-RTK treatment is the dependence of drug effectiveness on co-expression of multiple RTKs which defines resistance to single ...
Bown, James L. +8 more
core +6 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
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
Mapping the druggable allosteric space of G-protein coupled receptors: a fragment-based molecular dynamics approach. [PDF]
, 2010 To address the problem of specificity in G-protein coupled receptor (GPCR) drug discovery, there has been tremendous recent interest in allosteric drugs that bind at sites topographically distinct from the orthosteric site. Unfortunately, structure-based
Ivetac, Anthony, McCammon, J Andrew
core +2 more sources
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
Molecules, 2021 Membrane proteins such as G protein-coupled receptors (GPCRs) exert fundamental biological functions and are involved in a multitude of physiological responses, making these receptors ideal drug targets.
Yann Waltenspühl +3 more
doaj +1 more source
Hydrocarbon molar water solubility predicts NMDA vs. GABAA receptor modulation. [PDF]
, 2014 BackgroundMany anesthetics modulate 3-transmembrane (such as NMDA) and 4-transmembrane (such as GABAA) receptors. Clinical and experimental anesthetics exhibiting receptor family specificity often have low water solubility. We hypothesized that the molar
Brosnan, Robert J, Pham, Trung L
core +2 more sources