Quinolones modulate ghrelin receptor signaling: potential for a novel small molecule scaffold in the treatment of cachexia [PDF]
, 2018 Cachexia is a metabolic wasting disorder characterized by progressive weight loss, muscle atrophy, fatigue, weakness, and appetite loss. Cachexia is associated with almost all major chronic illnesses including cancer, heart failure, obstructive ...
Cano, Rafael +8 more
core +3 more sources
Dysfunction in endoplasmic reticulum-mitochondria crosstalk underlies SIGMAR1 loss of function mediated motor neuron degeneration [PDF]
, 2017 Mutations in SIGMAR1, which encodes the Sigma 1 receptor, cause a familial form of amyotrophic lateral sclerosis, but the underlying molecular mechanisms are unclear. Bernard-Marissal et al.
Azzedine, Hamid +3 more
core
GPER agonist G-1 decreases adrenocortical carcinoma (ACC) cell growth in vitro and in vivo [PDF]
, 2015 We have previously demonstrated that estrogen receptor (ER) alpha (ESR1) increases proliferation of adrenocortical carcinoma (ACC) through both an estrogen-dependent and -independent (induced by IGF-II/IGF1R pathways) manner.
Amendola, Donatella +16 more
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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
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
Behavioral and pharmacological characterization of a mouse model of palatable diet alternation [PDF]
, 2017 Obesity and eating disorders represent a severe problem in Western societies. Both the increased availability of highly palatable foods and dieting are major risk factors contributing to the epidemic disorders of feeding. The purpose of this study was to
Schlain, Gabrielle Star
core
Targeting interleukin-1β protects from aortic aneurysms induced by disrupted transforming growth factor β signaling [PDF]
, 2017 Aortic aneurysms are life-threatening conditions with effective treatments mainly limited to emergency surgery or trans-arterial endovascular stent grafts, thus calling for the identification of specific molecular targets.
Bizzotto, Dario +13 more
core +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
Functional selectivity of GPCR-directed drug action through location bias. [PDF]
, 2017 G-protein-coupled receptors (GPCRs) are increasingly recognized to operate from intracellular membranes as well as the plasma membrane. The β 2 -adrenergic GPCR can activate G s -linked cyclic AMP (G s -cAMP) signaling from endosomes.
Conti, Marco +6 more
core +3 more sources