Membrane proteins perform a host of vital cellular functions. Deciphering the molecular
mechanisms whereby they fulfill these functions requires detailed biophysical and structural …

This review compares the biological and physiological function of Sigma receptors [σRs] and
their potential therapeutic roles. Sigma receptors are widespread in the central nervous …

In an attempt to extend recent studies showing that some clinically evaluated histamine H3
receptor (H3R) antagonists possess nanomolar affinity at sigma-1 receptors (σ1R), we …

Calcium exchanges and homeostasis are finely regulated between cellular organelles and
in response to physiological signals. Besides ionophores, including voltage-gated Ca 2+ …

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 …

Neuropathic pain is one of the most debilitating forms of chronic pain, resulting from an
injury or disease of the somatosensory nervous system, which induces abnormal painful …

The sigma-2 receptor has been cloned and identified as Tmem97, which is a
transmembrane protein involved in intracellular Ca 2+ regulation and cholesterol …

E-52862 is a selective σ1R antagonist currently undergoing phase II clinical trials for
neuropathic pain and represents a potential first-in-class analgesic. Here, we investigated …

The synthesis and pharmacological activity of a new series of isoxazolylpyrimidines as
sigma-2 receptor (σ2R) ligands are reported. Modification of a new hit retrieved in an HTS …

Sigma1 (also known as sigma-1 receptor, Sig1R, σ1 receptor) is a unique pharmacologically
regulated integral membrane chaperone or scaffolding protein. The majority of publications …