Results 11 to 20 of about 1,197,707 (200)

Discovery of Iboga-Derived Ligands for the Sigma‑2 Receptor [PDF]

ACS Bio & Med Chem Au
Substance use disorder (SUD) is a mental condition that affects a person’s brain and behavior, leading to a lack of control with alcohol, drug, and medication use. The lack of efficacious and novel treatments for SUD is a growing concern. As such, we have synthesized a series of iboga alkaloid derivatives and evaluated their receptor binding profiles ...
Alexander J. Hughes, Julie A. Talbert, Steven D. Townsend   +2 more
doaj   +3 more sources

Sigma-2 receptor/TMEM97 agonist PB221 as an alternative drug for brain tumor [PDF]

BMC Cancer, 2019
Background There are limited effective drugs that can reach the brain to target brain tumors, in particular glioblastoma, which is one of the most difficult cancers to be cured from.
Chia-Chi Liu, Ching-Fang Yu, Shu-Chi Wang, Hsueh-Yin Li, Chiu-Min Lin, Hsia-Han Wang, Carmen Abate, Chi-Shiun Chiang   +7 more
doaj   +6 more sources

The Effect of KSK-94, a Dual Histamine H₃ and Sigma-2 Receptor Ligand, on Adipose Tissue in a Rat Model of Developing Obesity [PDF]

Pharmaceuticals
Background: Numerous studies highlight the critical role that neural histamine plays in feeding behavior, which is controlled by central histamine H3 and H1 receptors. This is the fundamental motivation for the increased interest in creating histamine H3
Magdalena Kotańska, Monika Zadrożna, Monika Kubacka, Kamil Mika, Katarzyna Szczepańska, Barbara Nowak, Alessio Alesci, Anthea Miller, Eugenia Rita Lauriano, Katarzyna Kieć-Kononowicz   +9 more
doaj   +2 more sources

Inhibitory effects of sigma-2 receptor agonists on T lymphocyte activation [PDF]

Frontiers in Pharmacology, 2013
Sigma (σ) receptor ligands are essentially known for their effects on the nervous system although recent studies have shown their potential effects modulating some other pathophysiological processes as cell proliferation, cancer and the immune response ...
Miguel Angel Iñiguez, Carmen ePunzón, Raquel eNieto, Javier eBurgueño, José Miguel Vela, MANUEL eFRESNO   +5 more
doaj   +5 more sources

A Review of the Clinical Progress of CT1812, a Novel Sigma-2 Receptor Antagonist for the Treatment of Alzheimer’s Disease [PDF]

Pharmaceuticals
Alzheimer’s disease (AD) is a neurodegenerative disease marked by the accumulation of toxic amyloid-beta (Aβ) oligomers. These oligomers are thought to cause synaptic dysfunction and contribute to neurodegeneration.
Sara R. Steinfield, Daniel F. Stenn, Helen Chen, Bettina E. Kalisch   +3 more
doaj   +2 more sources

Sigma-2 Receptor Ligand Binding Modulates Association between TSPO and TMEM97. [PDF]

Int J Mol Sci, 2023
Sigma-2 receptor (S2R) is a S2R ligand-binding site historically associated with reportedly 21.5 kDa proteins that have been linked to several diseases, such as cancer, Alzheimer’s disease, and schizophrenia. The S2R is highly expressed in various tumors, where it correlates with the proliferative status of the malignant cells.
Thejer BM, Infantino V, Santarsiero A, Pappalardo I, Abatematteo FS, Teakel S, Van Oosterum A, Mach RH, Denora N, Lee BC, Resta N, Bagnulo R, Niso M, Contino M, Montsch B, Heffeter P, Abate C, Cahill MA.   +17 more
europepmc   +4 more sources

TMEM97/Sigma 2 Receptor Increases Estrogen Receptor α Activity in Promoting Breast Cancer Cell Growth. [PDF]

Cancers (Basel), 2023
Aberrant estrogen receptor (ER) signaling is a major driver of breast tumor growth and progression. Sigma 2 receptor has long been implicated in breast carcinogenesis based on pharmacological studies, but its molecular identity had been elusive until TMEM97 was identified as the receptor.
Zhang Y, Fang X, Wang J, Nie D.
europepmc   +3 more sources

Histatin-1 is an endogenous ligand of the sigma-2 receptor. [PDF]

FEBS J, 2021
The Sigma‐2 receptor (S2R) (a.k.a TMEM97) is an important endoplasmic reticular protein involved in cancer, cholesterol processing, cell migration, and neurodegenerative diseases, including Niemann–Pick Type C. While several S2R pharmacologic agents have been discovered, its recent (2017) cloning has limited biological investigation, and no endogenous ...
Son KN, Lee H, Shah D, Kalmodia S, Miller RC, Ali M, Balasubramaniam A, Cologna SM, Kong H, Shukla D, Aakalu VK.   +10 more
europepmc   +4 more sources

The Sigma-2 Receptor and Progesterone Receptor Membrane Component 1 are Different Binding Sites Derived From Independent Genes

EBioMedicine, 2015
The sigma-2 receptor (S2R) is a potential therapeutic target for cancer and neuronal diseases. However, the identity of the S2R has remained a matter of debate.
Uyen B. Chu, Timur A. Mavlyutov, Ming-Liang Chu, Huan Yang, Amanda Schulman, Christophe Mesangeau, Christopher R. McCurdy, Lian-Wang Guo, Arnold E. Ruoho   +8 more
doaj   +3 more sources

BS148 Reduces the Aggressiveness of Metastatic Melanoma via Sigma-2 Receptor Targeting. [PDF]

Int J Mol Sci, 2023
The management of advanced-stage melanoma is clinically challenging, mainly because of its resistance to the currently available therapies. Therefore, it is important to develop alternative therapeutic strategies. The sigma-2 receptor (S2R) is overexpressed in proliferating tumor cells and represents a promising vulnerability to target. Indeed, we have
Sorbi C, Belluti S, Atene CG, Marocchi F, Linciano P, Roy N, Paradiso E, Casarini L, Ronsisvalle S, Zanocco-Marani T, Brasili L, Lanfrancone L, Imbriano C, Di Rocco G, Franchini S.   +14 more
europepmc   +5 more sources