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 …

[HTML][HTML] The biological function of sigma-2 receptor/TMEM97 and its utility in PET imaging studies in cancer

C Zeng, A Riad, RH Mach - Cancers, 2020 - mdpi.com
The sigma-2 receptor was originally defined pharmacologically and recently identified as
TMEM97. TMEM97 has been validated as a biomarker of proliferative status and the …

[HTML][HTML] Sigma-2 receptor—A potential target for cancer/Alzheimer's disease treatment via its regulation of cholesterol homeostasis

K Yang, C Zeng, C Wang, M Sun, D Yin, T Sun - Molecules, 2020 - mdpi.com
The sigma receptors were classified into sigma-1 and sigma-2 receptor based on their
different pharmacological profiles. In the past two decades, our understanding of the …

1, 2, 3, 4-Tetrahydroisoquinoline (THIQ) as privileged scaffold for anticancer de novo drug design

Faheem, B Karan Kumar… - Expert Opinion on …, 2021 - Taylor & Francis
Introduction: Cancer is a dreadful disorder that is emerging as one of the leading causes of
mortality across the globe. The complex tumor environment, supplemented with drawbacks …

Development of a Highly Specific 18F-Labeled Radioligand for Imaging of the Sigma-2 Receptor in Brain Tumors

T Wang, J Wang, L Chen, X Zhang, T Mou… - Journal of Medicinal …, 2023 - ACS Publications
Novel ligands with the 6, 7-dimethoxy-1, 2, 3, 4-tetrahydroisoquinoline or 5, 6-
dimethoxyisoindoline pharmacophore were designed and synthesized for evaluation of their …

[HTML][HTML] Non-conventional and investigational PET radiotracers for breast cancer: a systematic review

M Balma, V Liberini, M Racca, R Laudicella… - Frontiers in …, 2022 - frontiersin.org
Breast cancer is one of the most common malignancies in women, with high morbidity and
mortality rates. In breast cancer, the use of novel radiopharmaceuticals in nuclear medicine …

[HTML][HTML] Novel applications of molecular imaging to guide breast cancer therapy

CE Edmonds, SR O'Brien, DA Mankoff, AR Pantel - Cancer Imaging, 2022 - Springer
The goals of precision oncology are to provide targeted drug therapy based on each
individual's specific tumor biology, and to enable the prediction and early assessment of …

[HTML][HTML] BS148 Reduces the Aggressiveness of Metastatic Melanoma via Sigma-2 Receptor Targeting

C Sorbi, S Belluti, CG Atene, F Marocchi… - International Journal of …, 2023 - mdpi.com
The management of advanced-stage melanoma is clinically challenging, mainly because of
its resistance to the currently available therapies. Therefore, it is important to develop …

[HTML][HTML] 18F-fluorodeoxyglucose (FDG) PET or 18F-fluorothymidine (FLT) PET to assess early response to aromatase inhibitors (AI) in women with ER+ operable …

PE Romine, LM Peterson, BF Kurland, DW Byrd… - Breast Cancer …, 2021 - Springer
Purpose This study evaluated the ability of 18 F-Fluorodeoxyglucose (FDG) and 18 F-
Fluorothymidine (FLT) imaging with positron emission tomography (PET) to measure early …

Sigma-2 receptor as a potential drug target

AF Chen, WH Ma, XY Xie… - Current Medicinal …, 2021 - ingentaconnect.com
Sigma-2 receptor plays key roles in promoting tumor cell apoptosis, enhancing efficacy of
anti-tumor drugs, blocking signal transduction controlled by Aβ oligomers, regulating Ca2+ …