PLoS ONE, 2012 In addition to both the α1 adrenergic receptor and N-methyl-D-aspartate (NMDA) receptor antagonists, ifenprodil binds to the sigma receptor subtypes 1 and 2.
Tamaki Ishima, Kenji Hashimoto
doaj +1 more source
Sigma1 Targeting to Suppress Aberrant Androgen Receptor Signaling in Prostate Cancer. [PDF]
, 2017 Suppression of androgen receptor (AR) activity in prostate cancer by androgen depletion or direct AR antagonist treatment, although initially effective, leads to incurable castration-resistant prostate cancer (CRPC) via compensatory mechanisms including ...
Anderson, Kelsey N. +10 more
core +1 more source
Metabotropic glutamate receptor 2/3 (mGluR2/3) activation suppresses TRPV1 sensitization in mouse, but not human sensory neurons [PDF]
, 2018 The use of human tissue to validate putative analgesic targets identified in rodents is a promising strategy for improving the historically poor translational record of preclinical pain research.
Baranger, David A.A. +5 more
core +2 more sources
Molecular Oncology, EarlyView.ERRFI1, a neural crest (NC)‐associated gene, was upregulated in melanoma and negatively correlated with the expression of melanocytic differentiation markers and the susceptibility of melanoma cells toward BRAF inhibitors (BRAFi). Knocking down ERRFI1 significantly increased the sensitivity of melanoma cells to BRAFi.
Nina Wang +8 more
wiley +1 more source
Sigma-2 receptor ligands QSAR model dataset
Data in Brief, 2017 The data have been obtained from the Sigma-2 Receptor Selective Ligands Database (S2RSLDB) and refined according to the QSAR requirements. These data provide information about a set of 548 Sigma-2 (σ2) receptor ligands selective over Sigma-1 (σ1 ...
Antonio Rescifina +7 more
doaj +1 more source
Pharmaceutical Fronts, 2021 A total of 20 novel aryl piperazine derivatives were designed and synthesized, and their structures were confirmed by mass spectrometry and nuclear magnetic resonance analyses. Their 5-HT1A and sigma-1 receptor affinities were determined, and six of them
Yan-Na Ni +7 more
doaj +1 more source
Increasing the Receptor Tyrosine Kinase EphB2 Prevents Amyloid-β-induced Depletion of Cell Surface Glutamate Receptors by a Mechanism That Requires the PDZ-binding Motif of EphB2 and Neuronal Activity. [PDF]
, 2015 Diverse lines of evidence suggest that amyloid-β (Aβ) peptides causally contribute to the pathogenesis of Alzheimer disease (AD), the most frequent neurodegenerative disorder.
Johnson, Erik +4 more
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Exploiting metabolic adaptations to overcome dabrafenib treatment resistance in melanoma cells
Molecular Oncology, EarlyView.We show that dabrafenib‐resistant melanoma cells undergo mitochondrial remodeling, leading to elevated respiration and ROS production balanced by stronger antioxidant defenses. This altered redox state promotes survival despite mitochondrial damage but renders resistant cells highly vulnerable to ROS‐inducing compounds such as PEITC, highlighting redox
Silvia Eller +17 more
wiley +1 more source
The Evaluation of AZ66, A Highly Selective Sigma-1 and Sigma-2 Receptor Antagonist, For Its Anti-Convulsive Effects in C57BL/6 Mice [PDF]
, 2017 The Evaluation of AZ66, A Highly Selective Sigma-1 and Sigma-2 Antagonist, for Anticonvulsive Effects in C57Bl/6 Mice (Under the direction of Lisa Wilson and Dr. Christopher McCurdy) Sigma receptors have become a popular subject for research the past
Stone, Jamie
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Albumin uptake in human podocytes: a possible role for the cubilin-amnionless (CUBAM) complex [PDF]
, 2017 Albumin re-uptake is a receptor-mediated pathway located in renal proximal tubuli. There is increasing evidence of glomerular protein handling by podocytes, but little is known about the mechanism behind this process.
ANGLANI, FRANCA +8 more
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