Sigma Receptor (σR) Ligands with Antiproliferative and Anticancer Activity
Molecules, 2017 Sigma receptor (σR) ligands have proven to be useful as cancer diagnostics and anticancer therapeutics and their ligands have been developed as molecular probes in oncology.
Markos-Orestis Georgiadis +3 more
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Recent Developments in Sigma-2 Receptor Compounds for Pain. [PDF]
CureusAfter years of enigmatic pharmacology, non-selective ligands, and uncertain clinical application, sigma receptors have emerged as interesting therapeutic drug discovery-development targets. Two subtypes of sigma receptors have now been cloned, sigma-1 receptor (S1R) and sigma-2 receptor (S2R), and there has been much complementary and converging ...
Raffa RB, Pergolizzi JV.
europepmc +3 more sources
Haem-dependent dimerization of PGRMC1/Sigma-2 receptor facilitates cancer proliferation and chemoresistance [PDF]
Nature Communications, 2016 PGRMC1 binds to EGFR and cytochromes P450, and is known to be involved in cancer proliferation and in drug resistance. Here, the authors determine the structure of the cytosolic domain of PGRMC1, which forms a dimer via haem–haem stacking, and propose ...
Yasuaki Kabe +20 more
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Highly Specific Sigma Receptor Ligands Exhibit Anti-Viral Properties in SARS-CoV-2 Infected Cells
Pathogens, 2021 (1) Background: There is a strong need for prevention and treatment strategies for COVID-19 that are not impacted by SARS-CoV-2 mutations emerging in variants of concern.
David A. Ostrov +15 more
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Ghrelin Decreases Firing Activity of Gonadotropin-Releasing Hormone (GnRH) Neurons in an Estrous Cycle and Endocannabinoid Signaling Dependent Manner. [PDF]
, 2013 The orexigenic peptide, ghrelin is known to influence function of GnRH neurons, however, the direct effects of the hormone upon these neurons have not been explored, yet.
Farkas, Imre +3 more
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Sigma-1 and Sigma-2 Receptor Modulators as Potential Therapeutics for Alzheimer's Disease. [PDF]
ACS Med Chem Lett, 2021 Kargbo RB.
europepmc +4 more sources
KSK-74: Dual Histamine H3 and Sigma-2 Receptor Ligand with Anti-Obesity Potential. [PDF]
Int J Mol Sci, 2022 Many studies involving compounds that enhance histamine release, such as histamine H3 receptor (H3R) antagonists, have shown efficacy in inhibiting weight gain, but none have passed clinical trials. As part of the search for H3 receptor ligands that have additional properties, the aim of this study is to evaluate the activity in the reduction in weight
Mika K +11 more
europepmc +4 more sources
Frontiers in Pharmacology, 2020 Sigma-1 and sigma-2 receptors are emerging therapeutic targets. Although the molecular identity of the sigma-2 receptor has recently been determined, receptor quantitation has used, and continues to use, the sigma-1 selective agents (+) pentazocine or ...
Haider Abbas +5 more
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Development of Tetrahydroindazole-Based Potent and Selective Sigma-2 Receptor Ligands. [PDF]
ChemMedChem, 2019 AbstractThe sigma‐2 receptor has been shown to play important roles in a number of important diseases, including central nervous system (CNS) disorders and cancer. However, mechanisms by which sigma‐2 contributes to these diseases remain unclear.
Iyamu ID +4 more
europepmc +4 more sources
Sigma-2 Receptor as Potential Indicator of Stem Cell Differentiation [PDF]
Molecular Imaging and Biology, 2011 The sigma-2 (σ(2)) receptor is a potential biomarker of proliferative status of solid tumors. Specific synthetic probes using N-substituted-9-azabicyclo [3.3.1]nonan-3α-yl carbamate analogs have been designed and implemented for experimental cancer diagnosis and therapy.We employed the fluorescently labeled σ(2) receptor probe, SW120, to evaluate σ(2 ...
Jodi L, Haller +5 more
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