Results 41 to 50 of about 36,012 (161)
Reversing allosteric communication: From detecting allosteric sites to inducing and tuning targeted allosteric response. [PDF]
PLoS Computational Biology, 2018 The omnipresence of allosteric regulation together with the fundamental role of structural dynamics in this phenomenon have initiated a great interest to the detection of regulatory exosites and design of corresponding effectors.
Wei-Ven Tee +2 more
doaj +1 more source
Molecular Medicine Communications, 2022 Deterioration in cognitive dysfunction in Alzheimer’s disease (AD) patients is associated with microglia-mediated synaptic destruction. Using AD mouse models Spurrier and colleagues discerned the function of the metabotropic glutamate receptor 5 (mGluR5) on synaptic loss and demonstrated that a silent allosteric modulator (SAM) of mGLuR5 when given ...
openaire +1 more source
Allosteric Modulators Hit the TSH Receptor [PDF]
Endocrinology, 2014 The receptor for TSH (TSHR) has captured our interest and imagination since it was first demonstrated to be a major human antigen in autoimmune thyroid disease. The original realization that the immunoglobulin fraction of sera from patients with Graves' disease incorporated unique human autoantibodies to the TSHR led to the unraveling of the great ...
Terry F, Davies +2 more
openaire +2 more sources
Allosteric modulators targeting CNS muscarinic receptors [PDF]
Neuropharmacology, 2018 Muscarinic acetylcholine receptors are G protein-coupled receptors (GPCRs) which are broadly expressed in the central nervous system (CNS) and other tissues in the periphery. They emerge as important drug targets for a number of diseases including Alzheimer's disease, Parkinson's disease, and schizophrenia.
Andreas Bock, Ramona Schrage, Klaus Mohr
openaire +2 more sources
Acta Pharmaceutica Sinica BNeuropathic pain is a debilitating pathological condition that presents significant therapeutic challenges in clinical practice. Unfortunately, current pharmacological treatments for neuropathic pain lack clinical efficacy and often lead to harmful ...
Chunhao Zhu +4 more
doaj +1 more source
Pharmacological Research, 2023 Considerable progress has been made in recent years towards the identification and characterisation of novel subtype-selective modulators of nicotinic acetylcholine receptors (nAChRs).
Victoria R. Sanders, Neil S. Millar
doaj +1 more source
Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor [PDF]
Proceedings of the National Academy of Sciences, 2013 μ-Opioid receptors are among the most studied G protein-coupled receptors because of the therapeutic value of agonists, such as morphine, that are used to treat chronic pain. However, these drugs have significant side effects, such as respiratory suppression, constipation, allodynia, tolerance, and dependence, as well as abuse potential.
Neil T, Burford +7 more
openaire +2 more sources
Cells, 2022 The pregnane X receptor (PXR, NR1I2) is a xenobiotic-activated transcription factor with high levels of expression in the liver. It not only plays a key role in drug metabolism and elimination, but also promotes tumor growth, drug resistance, and ...
Rajamanikkam Kamaraj +3 more
doaj +1 more source
Allosteric Modulation of Metabotropic Glutamate Receptors [PDF]
, 2011 The development of receptor subtype-selective ligands by targeting allosteric sites of G protein-coupled receptors (GPCRs) has proven highly successful in recent years. One GPCR family that has greatly benefited from this approach is the metabotropic glutamate receptors (mGlus).
Douglas J, Sheffler +3 more
openaire +2 more sources
Scientific ReportsAllosteric modulation of muscarinic acetylcholine receptors (mAChR) has been identified as a potential strategy for regulating cholinergic signaling in the treatment of various neurological disorders.
Corey J. Widman +11 more
doaj +1 more source