Imaging the Sigma-2 Receptor for Diagnosis and Prediction of Therapeutic Response

Zeng, Chenbo; Xu, Jinbin; Mach, Robert H.

doi:10.5772/24438

Cited by 1 publication

(2 citation statements)

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“…The methyl group of the ortho‐methoxy moiety on the benzamide side can be replaced with other alkyl or even large structures without significant losses of sigma‐2 receptor affinities and selectivities, as demonstrated by analogs 18 , 19 , 20 , 21 , 22 . The high affinities of these analogs implicate that there is a significant bulk tolerance within the sigma‐2 receptor binding pocket The oxygen of the ortho‐methoxy group on the benzamide may form intramolecular hydrogen bond with the amide NH, and this phenyl‐amide coplanar structure may be important for high sigma‐2 receptor binding, as confirmed by analog 10 (without ortho‐methoxy and with decreased sigma‐2 receptor affinity) and a constrained cyclo‐amide structure 11 (without ortho‐methoxy, but with a phenyl‐amide coplanar structure, showing good sigma‐2 receptor affinity and selectivity) …”

Section: Structures and Pharmacological Profiles Of Selective Sigma‐2mentioning

confidence: 95%

“…A number of the 6,7‐dimethoxytetrahydroisoquinoline analogs, including 7 , 12 , 13 , 19 , 20 , 21 , and 22 , have been explored for imaging studies by PET and some exciting results were obtained by Mach and colleagues . Compounds 7 ([ 3 H]‐RHM‐1) and 19 ([ 18 F]‐ISO‐1 and [ 125 I]‐ISO‐2) have been extensively studied both in vitro and in vivo for cancer cell proliferation and tumor status monitoring.…”

Section: Structures and Pharmacological Profiles Of Selective Sigma‐2mentioning

confidence: 99%

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Sigma‐2 Receptor Ligands and Their Perspectives in Cancer Diagnosis and Therapy

Huang

Zhang

et al. 2013

Medicinal Research Reviews

100

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The sigma-2 receptor is highly expressed in various rapidly proliferating cancer cells and regarded as a cancer cell biomarker. Selective sigma-2 ligands have been shown to specifically label the tumor sites, induce cancer cells to undergo apoptosis, and inhibit tumor growth. Sigma-2 ligands are potentially useful as cancer diagnostics, anticancer therapeutics, or adjuvant anticancer treatment agents. However, both the cloning of this receptor and the identification of its endogenous ligand have not been successful, and the lack of structural information has severely hindered the understanding of its physiological roles, its signaling pathways, and the development of more selective sigma-2 ligands. Recent data have implicated that sigma-2 binding sites are within the lipid rafts and that PGRMC1 (progesterone receptor membrane component 1) complex and sigma-2 receptor may be coupled with EGFR (epidermal growth factor receptor), mTOR (mammalian target of rapamycin), caspases, and ion channels. Due to its promising applications in cancer management, there are rapidly increasing research efforts that are being directed into this field. This review article updates the current understanding of sigma-2 receptor and its potential physiological roles, applications, interaction with other effectors, with special focuses on the development of sigma-2 ligands, their chemical structures, pharmacological profiles, applications in imaging and anticancer therapy.

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Section: Structures and Pharmacological Profiles Of Selective Sigma‐2mentioning

confidence: 95%

Section: Structures and Pharmacological Profiles Of Selective Sigma‐2mentioning

confidence: 99%