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 …
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 …
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 …
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 …
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 …
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 …
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 …
strategy to counteract neurodegeneration, cancer progression, and viral infections, including …
Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands
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 …
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 …
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 …
mainly the choroid, but also the ciliary body and the iris. Promising pharmaceutical therapies …