Structure-activity relationships of mixed σ1R/σ2R ligands with antiproliferative and anticancer effects

AN Fallica, V Ciaffaglione, MN Modica, V Pittalà… - Bioorganic & Medicinal …, 2022 - Elsevier
The overexpression of σ receptors (σRs) in various types of tumors has prompted a deep
investigation of their role in cancer pathophysiology. Consequently, σR ligands have been …

Transmembrane protein TMEM97 and epigenetic reader BAHCC1 constitute an axis that supports pro-inflammatory cytokine expression

J Li, H Shen, LW Guo - Cellular Signalling, 2024 - Elsevier
Pro-inflammatory cytokine production by the retinal pigment epithelium (RPE) is a key
etiology in retinal degenerative diseases, yet the underlying mechanisms are not well …

Sigma Receptor Ligands Are Potent Antiprion Compounds that Act Independently of Sigma Receptor Binding

RCC Mercer, NTT Le, DG Fraser… - ACS Chemical …, 2024 - ACS Publications
Prion diseases are invariably fatal neurodegenerative diseases of humans and other
animals for which there are no effective treatment options. Previous work from our laboratory …

Loss of sigma-2 receptor/TMEM97 is associated with neuropathic injury-induced depression-like behaviors in female mice

VM Hong, AD Rade, SM Yan, A Bhaskara, MS Yousuf… - Eneuro, 2024 - eneuro.org
Previous studies have shown that ligands that bind to sigma-2 receptor/TMEM97
(s2R/TMEM97), a transmembrane protein, have anxiolytic/antidepressant-like properties …

The Ukrainian factor in early-stage drug discovery in the context of Russian invasion: The case of Enamine Ltd

IS Kondratov, YS Moroz, OO Grygorenko… - ACS Medicinal …, 2022 - ACS Publications
Ukrainian companies occupy an important niche in the global drug discovery process;
however, before the Russian invasion, the role of Ukraine was not obvious. The biggest …

New pharmacological strategies against pancreatic adenocarcinoma: The multifunctional thiosemicarbazone FA4

DP Anobile, M Niso, A Puerta, SM Fraga Rodrigues… - Molecules, 2022 - mdpi.com
A new sigma-2 (σ2) receptor ligand (FA4) was efficiently synthesized and evaluated for
cytotoxic, proapoptotic, and antimigratory activity on pancreatic ductal adenocarcinoma …

Retinal Photoreceptor Protection in an AMD-Related Mouse Model by Selective Sigma-1 or Sigma-2 Receptor Modulation

TA Mavlyutov, J Li, X Liu, H Shen, H Yang… - Genes, 2022 - mdpi.com
The structurally and genetically distinct sigma-1 receptor (S1R) and sigma-2 receptor (S2R)
comprise a unique class of drug binding sites. Their alleles are associated with human …

The molecular mechanism of the effects of the anti-neuropathic ligands on the modulation of the Sigma-2 receptor: An in-silico study

P Dashtestani, L Karami - International Journal of Biological …, 2024 - Elsevier
Neuropathic pain (NP) is a prevalent medical condition that lacks an effective treatment.
Recently, the Sigma-2 receptor (S2R) has been proposed as a potential therapeutic target …

Exploring the combinatorial explosion of amine–acid reaction space via graph editing

R Zhang, B Mahjour, A Outlaw, A McGrath… - Communications …, 2024 - nature.com
Amines and carboxylic acids are abundant chemical feedstocks that are nearly exclusively
united via the amide coupling reaction. The disproportionate use of the amide coupling …

Discovery of 3-oxo-1, 2, 3, 4-tetrahydropyrido [1, 2-a] pyrazin derivatives as SARS-CoV-2 main protease inhibitors through virtual screening and biological evaluation

X Dou, Q Sun, Y Liu, Y Lu, C Zhang, G Xu, Y Xu… - Bioorganic & Medicinal …, 2024 - Elsevier
The COVID-19 caused by SARS-CoV-2 has led to a global pandemic that continues to
impact societies and economies worldwide. The main protease (M pro) plays a crucial role …