Synthesis of a Novel Antiestrogen Radioligand (<sup>99m</sup>Tc-TOR-DTPA)

Yurt, Fatma; Müftüler, Fazilet Zümrüt Biber; Ünak, Perıhan; Yolcular, S.; Acar, Çiğdem Aydın; Enginar, Hüseyin

doi:10.1089/cbr.2009.0656

Cited by 12 publications

(3 citation statements)

References 27 publications

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“…C3 site of cyclofenil analogues is more tolerant of steric bulk and polar groups than the C4 site according to the binding affinity to both ER α and ER β . Toremifene (TOR), a chlorinated analog of tamoxifen, was coupled with diethylenetriamine pentaacetic acid (DTPA) and then radiolabeled with 99m Tc to form 99m Tc-DTPA-TOR [34]. The SPECT tracer exhibited high breast tissue/background ratio in xenograft tumors.…”

Section: Molecular Probes For Imaging Breast Cancer Specific Targetsmentioning

confidence: 99%

Molecular Imaging Probes for Diagnosis and Therapy Evaluation of Breast Cancer

Meng

2013

International Journal of Biomedical Imaging

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Breast cancer is a major cause of cancer death in women where early detection and accurate assessment of therapy response can improve clinical outcomes. Molecular imaging, which includes PET, SPECT, MRI, and optical modalities, provides noninvasive means of detecting biological processes and molecular events in vivo. Molecular imaging has the potential to enhance our understanding of breast cancer biology and effects of drug action during both preclinical and clinical phases of drug development. This has led to the identification of many molecular imaging probes for key processes in breast cancer. Hormone receptors, growth factor receptor, and angiogenic factors, such as ER, PR, HER2, and VEGFR, have been adopted as imaging targets to detect and stage the breast cancer and to monitor the treatment efficacy. Receptor imaging probes are usually composed of targeting moiety attached to a signaling component such as a radionuclide that can be detected using dedicated instruments. Current molecular imaging probes involved in breast cancer diagnosis and therapy evaluation are reviewed, and future of molecular imaging for the preclinical and clinical is explained.

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Section: Molecular Probes For Imaging Breast Cancer Specific Targetsmentioning

confidence: 99%

Molecular Imaging Probes for Diagnosis and Therapy Evaluation of Breast Cancer

Meng

2013

International Journal of Biomedical Imaging

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“…So, the formation constant of metal‐DTPA complex is about 100 times greater than that of EDTA . Also, contrary to DOTA, which demands on incubation an elevated temperature to form a metal complex, DTPA can complex with cationic metal ions at room temperature …”

Section: Resultsmentioning

confidence: 99%

Preparation and preliminary biological evaluation of ¹⁷⁷Lu‐labeled GluDTPA‐cyclo(RGDfK) for integrin α_νβ₃ receptor‐positive tumor targeting

Kim

Lim

Yun

et al. 2011

Labelled Comp Radiopharmac

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Integrin a n b 3 is a receptor and is highly expressed on activated and proliferating endothelial cells during the growth and metastasis of solid tumors but not on resting endothelial cells and normal organs. Because RGD peptide binds to integrin a n b 3 receptor, a variety of radiolabeled RGD peptides have been evaluated for non-invasive imaging of integrin a n b 3 -positive tumors.In an attempt to develop RGD-based radiopharmaceuticals, a novel GluDTPA-cyclo arginine-glycine-aspartic acid-Dphenylalanine-lysine (GluDTPA-cycloRGDfK) was simply synthesized and radiolabeled with 177 Lu. Also, tumor targeting and retention of the radiolabeled complex were evaluated in U87MG glioma-bearing mice.The 177 Lu-labeled GluDTPA-cyclo(RGDfK) was formulated with a high radiolabeling yield (>98%) under mild condition, and the radiochemical purity was sustained in both saline and serum for over 4 days at 37 C. The radiolabeled compounds were rapidly cleared from the blood pool and non-target tissue. Tumor-to-blood ratio was 12.09 at 2 h post injection and increased to 134.67 at 24 h, while tumor to liver ratio was 2.01 at 24 h similar to that of 2 h.Though it is inappropriate for targeted therapy due to its low uptake in tumor (~1 %ID/g), the acceptable results on radiochemistry and biodistribution propose to take a further assessment for non-invasive imaging and detection of integrin a n b 3 -positive tumors by applying diagnostic radionuclides.

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“…A few of them have even been successfully evaluated in rodents (Arterburn et al 2003 ;Nayak et al 2008 ;Ramesh et al 2006 ;Takahashi et al 2007a , b ;Yurt et al 2009 ;Zhu et al 2010 (Dehdashti et al 1991 ;Jonson and Welch 1998 ;Pomper et al 1988 ;Verhagen et al 1991a (Buckman et al 1995 ). […”

Section: Spectmentioning

confidence: 99%