Sigma-1 and dopamine D2/D3 receptor occupancy of pridopidine in healthy volunteers and patients with Huntington disease: a [18F] fluspidine and [18F] fallypride PET study
Sign Up to like & getrecommendations! Published in 2020 at "European Journal of Nuclear Medicine and Molecular Imaging"
DOI: 10.1007/s00259-020-05030-3
Abstract: Pridopidine is an investigational drug for Huntington disease (HD). Pridopidine was originally thought to act as a dopamine stabilizer. However, pridopidine shows highest affinity to the sigma-1 receptor (S1R) and enhances neuroprotection via the S1R… read more here.
Keywords: pet; 18f fluspidine; pridopidine; s1r ... See more keywords
APEX2- tagging of Sigma 1-receptor indicates subcellular protein topology with cytosolic N-terminus and ER luminal C-terminus
Sign Up to like & getrecommendations! Published in 2017 at "Protein & Cell"
DOI: 10.1007/s13238-017-0468-5
Abstract: Deciphering the role of any protein in a cell requires knowledge of the structure, subcellular localization, and the topological orientation of the protein within the relevant cells. The Sigma-1 receptor (S1R) largely localized to the… read more here.
Keywords: protein; terminus; topology; s1r ... See more keywords
Comprehensive 3D-QSAR Model Predicts Binding Affinity of Structurally Diverse Sigma 1 Receptor Ligands
Sign Up to like & getrecommendations! Published in 2019 at "Journal of chemical information and modeling"
DOI: 10.1021/acs.jcim.8b00521
Abstract: The Sigma 1 Receptor (S1R) has attracted intense interest as a pharmaceutical target for various therapeutic indications, including the treatment of neuropathic pain and the potentiation of opioid analgesia. Efforts by drug developers to rationally… read more here.
Keywords: s1r antagonists; qsar model; structurally diverse; model ... See more keywords
Development of a Novel σ1 Receptor Biosensor Based on Its Heterodimerization with Binding Immunoglobulin Protein in Living Cells.
Sign Up to like & getrecommendations! Published in 2023 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.3c00206
Abstract: The σ1 receptor (S1R) is a ligand-regulated non-opioid intracellular receptor involved in several pathological conditions. The development of S1R-based drugs as therapeutic agents is a challenge due to the lack of simple functional assays to… read more here.
Keywords: s1r; heterodimerization; binding immunoglobulin; s1r bip ... See more keywords
Sigma‐1 receptor protects against ferroptosis in hepatocellular carcinoma cells
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Cellular and Molecular Medicine"
DOI: 10.1111/jcmm.14594
Abstract: Sigma‐1 receptor (S1R) regulates reactive oxygen species (ROS) accumulation via nuclear factor erythroid 2‐related factor 2 (NRF2), which plays a vital role in ferroptosis. Sorafenib is a strong inducer of ferroptosis but not of apoptosis.… read more here.
Keywords: hepatocellular carcinoma; ferroptosis hepatocellular; hcc cells; ferroptosis ... See more keywords
Docking, Interaction Fingerprint, and Three-Dimensional Quantitative Structure–Activity Relationship (3D-QSAR) of Sigma1 Receptor Ligands, Analogs of the Neuroprotective Agent RC-33
Sign Up to like & getrecommendations! Published in 2019 at "Frontiers in Chemistry"
DOI: 10.3389/fchem.2019.00496
Abstract: The human Sigma1 receptor (S1R), which has been identified as a target with an important role in neuropsychological disorders, was first crystallized 3 years ago. Since S1R structure has no relation with another previous crystallized… read more here.
Keywords: s1r; activity relationship; structure activity; structure ... See more keywords