2.1 Structure of Sigma-1 receptor Martin et al. categorized Sigma receptor as a kind of opioid receptor at first in 1967 (McClane and Martin, 1967), but morphine-like drugs such as morphine and naltrexone are poor inhibitors for Sigma receptor. Thus, Sigma-1 receptor is classified as a non...
2022年3月10日,四川大学华西医院生物治疗国家重点实验室/罕见病中心/中西医结合科的孙子宜研究员、周小明研究员团队在Nature Communications上发表了题为“An open-like conformation of the sigma-1 receptor reveals its ligand entry pathway”的研究,展示了非洲爪蟾σ1R的多个晶体结构,包括开放式构象。连同功能结合...
The sigma-1 receptor is a 223 amino acid-long protein with a recently identified structure. The sigma-2 receptor is a genetically unrelated protein with a similarly shaped binding pocket and acts to influence cellular activities similar to the sigma-1 receptor. Both proteins are highly expressed ...
Sigma-1 receptor (Sig-1R) is expressed on endoplasmic reticulum (ER) membranes. Several functions have been attributed to Sig-1R, including regulation of ion channels such as Ca2+ and K+ channels, inhibition of Ca2+ influx through theN-methyl-D-aspartate (NMDA) receptor, modulation of the re...
Sigma-1 receptor chaperones at the ER– mitochondrion interface regulate Ca(2+) signaling and cell survival. Cell 131: 596–610. Hayashi T, Su TP (2008). An update on the development of drugs for neuropsychiatric disorders: focusing on the sigma 1 receptor ligand. Expert Opin Therap Targets...
SIGMA-1 receptorThe sigma 1 receptor (S1R) is a 223-amino-acid-long transmembrane endoplasmic reticulum (ER) protein. The S1R plays an important role in neuronal health and it is an established therapeutic target for neurodegenerative and neuropsychiatric disorders. Despite its importance in ...
Sigma-1 receptor (S1R) is an intracellular, multi-functional, ligand operated protein that also acts as a chaperone. It is considered as a pluripotent drug target in several pathologies. The publication of agonist and antagonist bound receptor structures has paved the way for receptor-based in ...
1995The invention relates to methods for the treatment of central nervous system disorders, neurological disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands...
:The sigma 1 receptor (S1R) is a molecular chaperone protein located in the endoplasmic reticulum and plasma membranes and has been shown to play important roles in various pathological disorders including pain and, as recently discovered, COVID-19. Employing structure- and QSAR-based drug design...
2. Basic information on sigma-1 receptor 2.1. Structure, distribution, and localization Sigma-1 receptors are endoplasmic-reticulum-resident transmembrane proteins, acting as intracellular receptors with chaperone protein function. They are mainly expressed in the central nervous system (hippocampus, hypotha...