Openings of the rat recombinant alpha1 homomeric glycine receptor as a function of the number of sgonist molecules bound [PDF]
, 2002 The functional properties of rat homomeric {alpha}1 glycine receptors were investigated using whole-cell and outside-out recording from human embryonic kidney cells transfected with rat {alpha}1 subunit cDNA.
Beato, M. +3 more
core
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
Dual targeting of RET and SRC synergizes in RET fusion‐positive cancer cells
Molecular Oncology, EarlyView.Despite the strong activity of selective RET tyrosine kinase inhibitors (TKIs), resistance of RET fusion‐positive (RET+) lung cancer and thyroid cancer frequently occurs and is mainly driven by RET‐independent bypass mechanisms. Son et al. show that SRC TKIs significantly inhibit PAK and AKT survival signaling and enhance the efficacy of RET TKIs in ...
Juhyeon Son +13 more
wiley +1 more source
Distinct roles for inhibition in spatial and temporal tuning of local edge detectors in the rabbit retina. [PDF]
, 2014 This paper examines the role of inhibition in generating the receptive-field properties of local edge detector (LED) ganglion cells in the rabbit retina. We confirm that the feed-forward inhibition is largely glycinergic but, contrary to a recent report,
Buldyrev, Ilya +5 more
core +9 more sources
MoleculesThe N-methyl-D-aspartate (NMDA) glutamate receptor is a major target of ethanol, and it is implicated in learning and memory formation, and other cognitive functions. Glycine acts as a co-agonist for this receptor.
Joanna Filarowska-Jurko +9 more
doaj +1 more source
The activation mechanism of alpha 1 homomeric glycine receptors [PDF]
, 2004 The glycine receptor mediates fast synaptic inhibition in the spinal cord and brainstem. Its activation mechanism is not known, despite the physiological importance of this receptor and the fact that it can serve as a prototype for other homopentameric ...
Beato, M +3 more
core
Cell surface interactome analysis identifies TSPAN4 as a negative regulator of PD‐L1 in melanoma
Molecular Oncology, EarlyView.Using cell surface proximity biotinylation, we identified tetraspanin TSPAN4 within the PD‐L1 interactome of melanoma cells. TSPAN4 negatively regulates PD‐L1 expression and lateral mobility by limiting its interaction with CMTM6 and promoting PD‐L1 degradation.
Guus A. Franken +7 more
wiley +1 more source
Biomolecules, 2021 Cisplatin, which is a chemotherapy drug listed on the World Health Organisation’s List of Essential Medicines, commonly induces dose-limiting side effects including chemotherapy-induced peripheral neuropathy (CIPN) that has a major negative impact on ...
Andy Kuo +3 more
doaj +1 more source
Molecular Requirements for Ethanol Differential Allosteric Modulation of Ligand-Gated Ion Channels Based on Selective G Beta Gamma Modulation [PDF]
, 2010 It is now believed that the allosteric modulation produced by ethanol in glycine receptors (GlyRs) depends on alcohol binding to discrete sites within the protein structure.
Aguayo, Luis G +6 more
core +1 more source
A comparison of glycine-and ivermectin-mediated conformational changes in the glycine receptor ligand-binding domain [PDF]
, 2012 Glycine receptor chloride channels are Cys-loop receptor proteins that isomerize between a low affinity closed state and a high affinity ion-conducting state.
Lynch, Joseph W., Wang, Qian
core +1 more source