Results 91 to 100 of about 107,657 (326)
, 2015 The mediodorsal thalamus (MD) likely plays an important role in cognition as it receives abundant afferent connections from the amygdala and prefrontal cortex (PFC).
Salt, T.E. +5 more
core +1 more source
Interpreting the effects of DNA polymerase variants at the structural level
Molecular Oncology, EarlyView.Using MAVISp and molecular dynamics simulations, we analyzed over 60 000 missense variants in POLE and POLD1 from ClinVar, COSMIC, cBioPortal, and saturation mutagenesis. Identified mechanistic indicators, including stability, binding, and long‐range, enable structural interpretation, providing ACMG‐like evidence for possible reclassification of VUS ...
Matteo Arnaudi +7 more
wiley +1 more source
Intracellular Binding Site for a Positive Allosteric Modulator of the Dopamine D1 Receptor
Molecular Pharmacology, 2018 The binding site for DETQ [2-(2,6-dichlorophenyl)-1-((1S,3R)-3-(hydroxymethyl)-5-(2-hydroxypropan-2-yl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one], a positive allosteric modulator (PAM) of the dopamine D1 receptor, was identified and compared ...
Xushan Wang +12 more
semanticscholar +1 more source
Neuropeptide receptor positive allosteric modulation in epilepsy: Galanin modulation revealed [PDF]
Proceedings of the National Academy of Sciences, 2010 The therapeutic potential of neuropeptides has long been recognized; some successes have been registered, for example, in the tachykinin, endothelin, somatostatin, angiotensin, calcitonin gene-related peptide (CGRP), orexin, or glucagon-like peptide 1 (GLP1) fields (1), primarily in peripheral applications.
openaire +2 more sources
Loss of proton‐sensing TDAG8 increases tumor progression in mouse models of colon cancer
Molecular Oncology, EarlyView.Loss of the pH‐sensing receptor TDAG8 accelerates colorectal cancer progression in mice. Animals lacking TDAG8 expression had increased tumor growth, DNA damage, and recruitment of tumor‐associated immune cells, including macrophages, neutrophils, and monocytes.
Ermanno Malagola +11 more
wiley +1 more source
Molecular Sites for the Positive Allosteric Modulation of Glycine Receptors by Endocannabinoids
PLoS ONE, 2011 Glycine receptors (GlyRs) are transmitter-gated anion channels of the Cys-loop superfamily which mediate synaptic inhibition at spinal and selected supraspinal sites. Although they serve pivotal functions in motor control and sensory processing, they have yet to be exploited as drug targets partly because of hitherto limited possibilities for ...
Yévenes, G E, Zeilhofer, Hanns Ulrich
openaire +8 more sources
Molecular Oncology, EarlyView.Drug resistance limits treatment success in a subset of lung cancers driven by ROS1 gene alterations. Using patient‐derived cells and computer simulations, we studied three key mutations and how they affect five targeted drugs. The mutations reduced drug effectiveness in different ways by altering protein structure and behavior.
Farhan Ul Haq +8 more
wiley +1 more source
Progress in GABAA receptor agonists for insomnia disorder
Frontiers in PharmacologyInsomnia is the most common sleep disorder in which an individual has trouble falling or staying asleep. Chronic sleep loss interferes with daily functioning and adversely affects health.
Weiyi Wang +5 more
doaj +1 more source
Frontiers in Pharmacology, 2018 mGlu5 receptor-mediated polyphosphoinositide (PI) hydrolysis is classically measured by determining the amount of radioactivity incorporated in inositolmonophosphate (InsP) after labeling of membrane phospholipids with radioactive inositol. Although this
Anna R. Zuena +9 more
doaj +1 more source
Allostery of atypical modulators at oligomeric G protein-coupled receptors
Scientific Reports, 2021 Many G protein-coupled receptors (GPCRs) are therapeutic targets, with most drugs acting at the orthosteric site. Some GPCRs also possess allosteric sites, which have become a focus of drug discovery.
Rabindra V. Shivnaraine +7 more
doaj +1 more source