Anavex Life Sciences Corp (AVXL)

[georgejjl]

Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases
Na Ye 1, Wangzhi Qin 1, Sheng Tian 1, Qingfeng Xu 1, Eric A Wold 2, Jia Zhou 2, Xue-Chu Zhen 1
Affiliations collapse
Affiliations
1Jiangsu Key Laboratory of Neuropsychiatric Diseases and College of Pharmaceutical Sciences, Soochow University, Suzhou, Jiangsu 215123, China.
2Chemical Biology Program, Department of Pharmacology and Toxicology, and Center for Addiction Research, University of Texas Medical Branch, Galveston, Texas 77555, United States.
PMID: 33111525 DOI: 10.1021/acs.jmedchem.0c01192
Abstract
The sigma-1 (s1) receptor, an enigmatic protein originally classified as an opioid receptor subtype, is now understood to possess unique structural and functional features of its own and play critical roles to widely impact signaling transduction by interacting with receptors, ion channels, lipids, and kinases. The s1 receptor is implicated in modulating learning, memory, emotion, sensory systems, neuronal development, and cognition and accordingly is now an actively pursued drug target for various neurological and neuropsychiatric disorders. Evaluation of the five selective s1 receptor drug candidates (pridopidine, ANAVEX2-73, SA4503, S1RA, and T-817MA) that have entered clinical trials has shown that reaching clinical approval remains an evasive and important goal. This review provides up-to-date information on the selective targeting of s1 receptors, including their history, function, reported crystal structures, and roles in neurological diseases, as well as a useful collation of new chemical entities as s1 selective orthosteric ligands or allosteric modulators.

https://pubmed.ncbi.nlm.nih.gov/33111525/

Good luck and GOD bless,