BRD2 regulation of sigma-2 receptor upon cholesterol deprivation [PDF]
Life Science Alliance, 2021 Upon cholesterol deprivation, epigenetic bookmark reader BRD2 and master transcription factor SREBP2 form a complex at bookmarked chromatin (H3K27ac), thereby activating the transcription of the sigma-2 receptor—a recently unveiled player in cholesterol ...
Hongtao Shen +8 more
doaj +7 more sources
The Sigma 2 receptor promotes and the Sigma 1 receptor inhibits mu-opioid receptor-mediated antinociception [PDF]
Molecular Brain, 2020 The Sigma-1 receptor (σ1R) has emerged as an interesting pharmacological target because it inhibits analgesia mediated by mu-opioid receptors (MOR), and also facilitates the development of neuropathic pain.
Pilar Sánchez-Blázquez +4 more
doaj +6 more sources
Sigma-2 receptor ligands QSAR model dataset [PDF]
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 +5 more sources
Cocaine Effects on Dopaminergic Transmission Depend on a Balance between Sigma-1 and Sigma-2 Receptor Expression [PDF]
Frontiers in Molecular Neuroscience, 2018 Sigma σ1 and σ2 receptors are targets of cocaine. Despite sharing a similar name, the two receptors are structurally unrelated and their physiological role is unknown.
David Aguinaga +11 more
doaj +5 more sources
Adamantane-derived scaffolds targeting the sigma-2 receptor; an in vitro and in silico study [PDF]
Saudi Pharmaceutical Journal, 2021 Novel adamantane-based compounds were synthesized and assessed as potential sigma-2 receptor ligands. Molecular docking and 50 ns molecular dynamic simulation were carried out to determine the binding modes, mechanism of interaction, and stability of ...
Mohammed A. Alamri, Mubarak A. Alamri
doaj +2 more sources
Characterization of CM-398, a Novel Selective Sigma-2 Receptor Ligand, as a Potential Therapeutic for Neuropathic Pain [PDF]
Molecules, 2022 Sigma receptors modulate nociception, offering a potential therapeutic target to treat pain, but relatively little is known regarding the role of sigma-2 receptors (S2R) in nociception.
Lisa L. Wilson +8 more
doaj +2 more sources
Lysosomal Membrane Permeabilization is an Early Event in Sigma-2 Receptor Ligand Mediated Cell Death in Pancreatic Cancer [PDF]
Journal of Experimental & Clinical Cancer Research, 2012 Background Sigma-2 receptor ligands have been studied for treatment of pancreatic cancer because they are preferentially internalized by proliferating cells and induce apoptosis.
Hornick John R +7 more
doaj +4 more sources
Sigma-2 Receptor—A Potential Target for Cancer/Alzheimer’s Disease Treatment via Its Regulation of Cholesterol Homeostasis [PDF]
Molecules, 2020 The sigma receptors were classified into sigma-1 and sigma-2 receptor based on their different pharmacological profiles. In the past two decades, our understanding of the biological and pharmacological properties of the sigma-1 receptor is increasing ...
Kai Yang +5 more
doaj +2 more sources
Novel Sigma-2 receptor ligand A011 overcomes MDR in adriamycin-resistant human breast cancer cells by modulating ABCB1 and ABCG2 transporter function [PDF]
Frontiers in Pharmacology, 2022 Multidrug resistance (MDR) is thought to be one of the main reasons for the failure of chemotherapy in cancers. ATP-binding cassette subfamily B member 1 (ABCB1) or P-glycoprotein (P-gp) and ATP-binding cassette subfamily G member 2 (ABCG2) play ...
Zhanwei Zeng +14 more
doaj +2 more sources
A Structure- and Ligand-Based Virtual Screening of a Database of “Small” Marine Natural Products for the Identification of “Blue” Sigma-2 Receptor Ligands [PDF]
Marine Drugs, 2018 Sigma receptors are a fascinating receptor protein class whose ligands are actually under clinical evaluation for the modulation of opioid analgesia and their use as positron emission tomography radiotracers.
Giuseppe Floresta +6 more
doaj +2 more sources