Recent advances in the development of sigma receptor ligands as cytotoxic agents: A medicinal chemistry perspective

AN Fallica, V Pittalà, MN Modica… - Journal of Medicinal …, 2021 - ACS Publications
Since their discovery as distinct receptor proteins, the specific physiopathological role of
sigma receptors (σRs) has been deeply investigated. It has been reported that these …

Screening of σ2 Receptor Ligands and In Vivo Evaluation of 11C-Labeled 6,7-Dimethoxy-2-[4-(4-methoxyphenyl)butan-2-yl]-1,2,3,4-tetrahydroisoquinoline for Potential Use as …

HY Kim, JY Lee, CJ Hsieh, A Riad, NJ Izzo… - Journal of Medicinal …, 2022 - ACS Publications
In this study, a panel of 46 compounds containing five different scaffolds known to have high
σ2 receptor affinity were screened. 6, 7-Dimethoxy-2-[4-(4-methoxyphenyl) butan-2-yl]-1, 2 …

Characterization of CM-398, a novel selective sigma-2 receptor ligand, as a potential therapeutic for neuropathic pain

LL Wilson, AR Alleyne, SO Eans, TJ Cirino, HM Stacy… - Molecules, 2022 - mdpi.com
Sigma receptors modulate nociception, offering a potential therapeutic target to treat pain,
but relatively little is known regarding the role of sigma-2 receptors (S2R) in nociception. The …

Haloperidol Metabolite II Valproate Ester (S)-(−)-MRJF22: Preliminary Studies as a Potential Multifunctional Agent Against Uveal Melanoma

C Barbaraci, G Giurdanella, CG Leotta… - Journal of Medicinal …, 2021 - ACS Publications
Increased angiogenesis and vascular endothelial growth factor (VEGF) levels contribute to
higher metastasis and mortality in uveal melanoma (UM), an aggressive malignancy of the …

Combination of heme oxygenase-1 inhibition and sigma receptor modulation for anticancer activity

G Romeo, V Ciaffaglione, E Amata, M Dichiara… - Molecules, 2021 - mdpi.com
Cancer is a multifactorial disease that may be tackled by targeting different signaling
pathways. Heme oxygenase-1 (HO-1) and sigma receptors (σRs) are both overexpressed in …

SIGMAP: an explainable artificial intelligence tool for SIGMA-1 receptor affinity prediction

MC Lomuscio, N Corriero, V Nanna… - RSC Medicinal …, 2024 - pubs.rsc.org
Developing sigma-1 receptor (S1R) modulators is considered a valuable therapeutic
strategy to counteract neurodegeneration, cancer progression, and viral infections, including …

Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands

D Zampieri, S Fortuna, M Romano, E Amata… - Bioorganic & Medicinal …, 2022 - Elsevier
In our continuing effort to develop novel sigma receptor (SR) ligands, we present the design,
synthesis and binding studies of a small library of aminopropylcarboxamide derivatives …

Identification and characterization of MAM03055A: A novel bivalent sigma-2 receptor/TMEM97 ligand with cytotoxic activity

CZ Liu, M Mottinelli, HE Nicholson, BM McVeigh… - European journal of …, 2021 - Elsevier
Abstract Sigma-2 receptor/transmembrane protein 97 (TMEM97) is upregulated in cancer
cells compared to normal cells. Traditional sigma-2 receptor agonists induce apoptosis and …

[HTML][HTML] Nanostructured lipid carrier for the ophthalmic delivery of haloperidol metabolite II valproate ester (±)-MRJF22: A potential strategy in the treatment of uveal …

C Cimino, CG Leotta, A Marrazzo, T Musumeci… - Journal of Drug Delivery …, 2023 - Elsevier
Among the eye tumors, uveal melanoma is one of the most diffuse and aggressive, affecting
mainly the choroid, but also the ciliary body and the iris. Promising pharmaceutical therapies …