Results 141 to 150 of about 1,421 (164)
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Targeting σ2R/TMEM97 with novel aminotetralins
European Journal of Medicinal Chemistry, 2022Initially associated with cancer diagnosis and therapy, the sigma 2 receptor (σ2R) has recently been implicated in several disorders of the central nervous system (CNS). It remained a poorly characterized target until we identified it as the transmembrane protein 97 (TMEM97). As part of a program to identify novel compounds that bind with high affinity
Michael D. Wood +2 more
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Sigma 2 Receptor/Tmem97 Agonists Produce Long Lasting Antineuropathic Pain Effects in Mice [PDF]
ACS Chemical Neuroscience, 2017 Neuropathic pain is an important medical problem with few effective treatments. The sigma 1 receptor (σ1R) is known to be a potential target for neuropathic pain therapeutics, and antagonists for this receptor are effective in preclinical models and are currently in phase II clinical trials.
Theodore John Price +2 more
exaly +3 more sources
European Journal of Medicinal Chemistry, 2021
Sigma-2 receptor (σ2R/TMEM97) has been implicated to play important roles in multiple cellular dysfunctions, such as cell neoplastic proliferation, neuro-inflammation, neurodegeneration, etc. Selective σ2 ligands are believed to be promising pharmacological tools to regulate or diagnose various disorders.
Wen-hui, Aladdin Riad, Robert H Mach
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Sigma-2 receptor (σ2R/TMEM97) has been implicated to play important roles in multiple cellular dysfunctions, such as cell neoplastic proliferation, neuro-inflammation, neurodegeneration, etc. Selective σ2 ligands are believed to be promising pharmacological tools to regulate or diagnose various disorders.
Wen-hui, Aladdin Riad, Robert H Mach
exaly +3 more sources
RNA interference against TMEM97 inhibits cell proliferation, migration, and invasion in glioma cells
Tumor Biology, 2015 Gliomas are the most common form of primary brain tumor in the adult central nervous system. Altered expression and prognostic value of transmembrane protein 97 (TMEM97) has been recently reported in different types of human tumors. However, the association of TMEM97and glioma is poorly defined. Here, we reported that TMEM97 was significantly increased
Wei Sun, Xuehua Ding, Zheng Cai
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Structure-affinity relationships of stereoisomers of norbenzomorphan-derived σ2R/TMEM97 modulators
European Journal of Medicinal Chemistry, 2023The sigma 2 receptor (σ2R), which is identical to transmembrane protein 97 (TMEM97), is attracting increasing interest as a possible therapeutic target for various indications in neuroscience. In continuation of a program to identify novel compounds that bind with high affinity and selectivity to σ2R/TMEM97, we performed structure-affinity-relationship
Yan Lu, Qi Gu, Stephen F. Martin
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The Biological Function of Sigma-2 Receptor/TMEM97 and Its Utility in PET Imaging Studies in Cancer [PDF]
Cancers, 2020 The sigma-2 receptor was originally defined pharmacologically and recently identified as TMEM97. TMEM97 has been validated as a biomarker of proliferative status and the radioligand of TMEM97, [18F]ISO-1, has been developed and validated as a PET imaging biomarker of proliferative status of tumors and as a predictor of the cancer therapy response. [18F]
Aladdin Riad, Robert H Mach
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Abstract 5281: Role of TMEM97/Sigma-2 receptor in prostate cancer
Cancer Research, 2023Abstract Introduction: Prostate cancer is the most common cancer in men. About one in eight men will be diagnosed with prostate cancer in his lifetime, and one in forty-one men will die of it. Sigma 2 receptor (σ2R) has been implicated in carcinogenesis including prostate cancer.
Xiangwei Fang +5 more
openaire +1 more source
European Journal of Pharmacology, 2021
Sigma-2 receptor/transmembrane protein 97 (TMEM97) is upregulated in cancer cells compared to normal cells. Traditional sigma-2 receptor agonists induce apoptosis and autophagy, making them of interest in cancer therapy. Recently, we reported a novel metabolically stimulative function of the sigma-2 receptor, showing increased 3-(4,5 dimethylthiazol-2 ...
Cheri Z Liu +2 more
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Sigma-2 receptor/transmembrane protein 97 (TMEM97) is upregulated in cancer cells compared to normal cells. Traditional sigma-2 receptor agonists induce apoptosis and autophagy, making them of interest in cancer therapy. Recently, we reported a novel metabolically stimulative function of the sigma-2 receptor, showing increased 3-(4,5 dimethylthiazol-2 ...
Cheri Z Liu +2 more
exaly +3 more sources
Reduction of TMEM97 increases NPC1 protein levels and restores cholesterol trafficking in Niemann-pick type C1 disease cells [PDF]
Human Molecular Genetics, 2016 Niemann-Pick type C disease (NP-C) is a progressive lysosomal lipid storage disease caused by mutations in the NPC1 and NPC2 genes. NPC1 is essential for transporting cholesterol and other lipids out of lysosomes, but little is known about the mechanisms that control its cellular abundance and localization.
Darius Ebrahimi-Fakhari +2 more
exaly +3 more sources
Structure-Affinity relationships of novel σ2R/TMEM97 ligands
Bioorganic ChemistryThe sigma 2 receptor (σ2R), which was recently identified as the transmembrane protein 97 (TMEM97), is increasingly attracting interest as a possible therapeutic target for indications in neuroscience. Toward identifying novel modulators of σ2R/TMEM97, we prepared a collection of benzoxazocine, benzomorphan, and methanobenzazepine ligands related to ...
Grant D. Walby +3 more
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