Carbon-11 labeled σ2 receptor ligands for imaging breast cancer

Tu, Zhude; Dence, Carmen S.; Ponde, Datta E.; Jones, Lynne A.; Wheeler, Kenneth T.; Welch, Michael J.; Mach, Robert H.

doi:10.1016/j.nucmedbio.2005.03.008

Cited by 64 publications

(69 citation statements)

References 7 publications

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“…Finally, radiolabeled sigma-2 selective ligands developed in our laboratory have shown promise in imaging studies of murine models of breast cancer, further suggesting that radioligands having a high affinity and high selectivity for sigma-2 receptors have the potential to noninvasively image the proliferative status of solid tumors in vivo with positron emission tomography (PET; refs. [18][19][20].…”

Section: Introductionmentioning

confidence: 99%

“…The localization of sigma-2 receptors in organelles known to play a key role in both caspase-dependent and caspase-independent pathways of cell death provides further support for the investigation of sigma-2 selective ligands as potential cancer chemotherapeutic agents. (18). SW107, N -(9-(6-(5-dimethylamino-1-naphthalensulfonamido))hexyl)-9-azabicyclo[3.3.1]nonan-3a-yl)-N ¶-(2-methoxy-5-methylphenyl)carbamate, was synthesized as described previously (24).…”

Section: Introductionmentioning

confidence: 99%

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Subcellular Localization of Sigma-2 Receptors in Breast Cancer Cells Using Two-Photon and Confocal Microscopy

Zeng¹,

Vangveravong²,

Xu³

et al. 2007

Cancer Research

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113

141

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Sigma-2 receptor agonists have been shown to induce cell death via caspase-dependent and caspase-independent pathways. Unfortunately, there is little information regarding the molecular function of sigma-2 receptors that can explain these results. In this study, two fluorescent probes, SW107 and K05-138, were used to study the subcellular localization of sigma-2 receptors by two-photon and confocal microscopy. The results indicate that sigma-2 receptors colocalize with fluorescent markers of mitochondria, lysosomes, endoplasmic reticulum, and the plasma membrane in both EMT-6 mouse and MDA-MB-435 human breast cancer cells. The fluorescent probe, K05-138, was internalized rapidly, reaching a plateau of fluorescent intensity at 5 min. The internalization of K05-138 was reduced f40% by phenylarsine oxide, an inhibitor of endocytosis. These data suggest that sigma-2 ligands are internalized, in part, by an endocytotic pathway. The localization of sigma-2 receptors in several organelles known to have a role in both caspase-dependent and caspaseindependent pathways of cell death supports the conclusions of previous studies suggesting that sigma-2 receptor ligands should be evaluated as potential cancer chemotherapeutic agents.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Subcellular Localization of Sigma-2 Receptors in Breast Cancer Cells Using Two-Photon and Confocal Microscopy

Zeng¹,

Vangveravong²,

Xu³

et al. 2007

Cancer Research

Self Cite

113

141

View full text Add to dashboard Cite

show abstract

“…In addition, in vivo visualization of receptor density/occupancy with small radiolabeled ligands, which is widely used, can also be classified as a direct imaging approach (27)(28)(29). These examples represent 2 of the first molecular imaging applications used in clinical nuclear medicine.…”

Section: Applicationmentioning

confidence: 99%

Imaging: Strategies, Controversies, and Opportunities

Blasberg

Piwnica-Worms

2012

Clinical Cancer Research

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At a Clinical and Translational Cancer Research Think Tank meeting sponsored by the American Association for Cancer Research in 2010, one of the breakout groups focused on new technologies and imaging. The discussions emphasized new opportunities in translational imaging and its role in the future, rather than established techniques that are currently in clinical practice. New imaging methods under development are changing the approach of imaging science from a focus on the anatomic description of disease to a focus on the molecular basis of disease. Broadly referred to as molecular imaging, these new strategies directly embrace the incorporation of cell and molecular biology concepts and techniques into image generation and can involve the introduction of genes into cells with the explicit intent to image the end products of gene expression with external imaging devices. These new methods hold the promise of providing clinicians with (i) robust linkages between cell and animal models and clinical trials, (ii) in vivo biomarkers that can be measured repeatedly and sequentially over time to observe dynamic disease processes and responses to treatment, and (iii) tools for preselection and patient population enrichment in phase II and III trials to improve outcomes and better direct treatment. These strategies provide real-time pharmacodynamic parameters and can be powerful tools to monitor therapeutic effects in a spatially and tissue-specific manner, which may reduce cost during drug development, because pharmacodynamic studies in animals can inform clinical trials and accelerate the translation process. The Imaging Response Assessment Team (IRAT) program serves as an example of how imaging techniques can be incorporated into clinical trials. IRATs work to advance the role of imaging in assessment of response to therapy and to increase the application of quantitative anatomic, functional, and molecular imaging endpoints in clinical trials, and imaging strategies that will lead to individualized patient care.

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“…The tritium labeled σ 2 selective ligand, [ 3 H]RHM-1, has been used to conduct Scatchard studies of σ 2 receptors in tumors and normal tissues ( Figure 3A) [37,38]. The in vitro receptor binding studies indicate that Figure 4B) based on the conformationally-flexible benzamide analogs have been generated and evaluated in murine breast tumor models [39].…”

Section: In Vitro Binding and In Vivo Imaging Studies Of σ 2 Receptorsmentioning

confidence: 99%

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

Zeng¹,

Xu²,

Mach³

2011

Breast Cancer - Recent Advances in Biology, Imaging and Therapeutics

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Carbon-11 labeled σ2 receptor ligands for imaging breast cancer

Cited by 64 publications

References 7 publications

Subcellular Localization of Sigma-2 Receptors in Breast Cancer Cells Using Two-Photon and Confocal Microscopy

Subcellular Localization of Sigma-2 Receptors in Breast Cancer Cells Using Two-Photon and Confocal Microscopy

Imaging: Strategies, Controversies, and Opportunities

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

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