Targeted functional imaging of estrogen receptors with 99mTc-GAP-EDL

Takahashi, Nobukazu; Yang, David J.; Kohanim, Saady; Oh, Chang Sok; Yu, Dongfang; Azhdarinia, Ali; Kurihara, Hiroaki; Zhang, Xiaochun; Chang, Joe Y.; Kim, E. Edmund

doi:10.1007/s00259-006-0191-6

Cited by 23 publications

(17 citation statements)

References 28 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Further, the values for DES and dienestrol themselves are consistent with a preferential inhibition of the MDA non-estrogen cancer cell line. DES is effective against estrogen receptor positive (ER+) tumors such as the MCF-7 cell line [37,38,39,40,41,42,43,44,45,46]. It is possible that some of the drug is bound to the estrogen receptors in the MCF-7 cells making the drug unavailable to act within the cell.…”

Section: Resultsmentioning

confidence: 99%

Structural Consideration in Designing Organotin Polyethers to Arrest the Growth of Breast Cancer Cells In Vitro

et al. 2011

View full text Add to dashboard Cite

The ability to inhibit cancer is inherent in organotin materials yet the structural relationships that regulate/direct this activity remains unknown. We measured antitumor activity using a matched pair of cell lines MDA-MB-231 cells that are estrogen-independent, estrogen receptor negative and MCF-7 cells, a cell line that is estrogen receptor (ER) positive. Those polyethers that contained a O-phenyl unit were able to significantly inhibit the non-estrogen sensitive cell line but were much less effective against the estrogen sensitive cell line; that is, the human breast cancer cell line MDA-MB-231 showed better test results for polymers derived from diols containing the O-phenyl moiety than the breast cancer cell line MCF-7, a well-characterized estrogen receptor positive control cell line. Those polyethers that did not contain the O-phenyl unit inhibited both cell lines approximately the same. The differential activity of the O-phenyl-containing polyethers is likely due to the estrogen-sensitive cells combining with some of the organotin polyethers minimizing their ability to inhibit cell growth.

show abstract

Section: Resultsmentioning

confidence: 99%

Structural Consideration in Designing Organotin Polyethers to Arrest the Growth of Breast Cancer Cells In Vitro

et al. 2011

View full text Add to dashboard Cite

show abstract

“…99m Tc-DTPA-estradioldemonstrated a KD much higher than typically reported values of estradiol itself (0.1-1.0 nM) [25,26], but was comparable to the affinity of a similar estrogen receptor (11 ± 1.5) nM [10]. Further, GAP-EDL was found to accumulate into ER+ 13762 (rat mammary carcinoma) tumors with a tumor-to-muscle ratio of 7.92 ± 0.56 at 4 h [21]; and 99m Tc-estradiol-pyridin-2-yl has been shown to target MCF-7 tumors with a tumor-to-muscle ratio of 5.67 ± 1.06 at 3 h post-injection [10].…”

Section: Accepted Manuscriptmentioning

confidence: 46%

“…The chelator DTPA was introduced to estradiolvia DTPA anhydride under mild conditions of pH and temperatures. Previous studies have suggested that 3-acetonitrile estradiol could be produced via an ER-mediated process, and that 99m Tc-labeled estradiol could be a useful agent for imaging ER status [21,22]. Compared with previous estradiol probes, DTPA-estradiol is a small molecule with a suitable molecular weight.…”

Section: Accepted Manuscriptmentioning

confidence: 98%

“…Compared with previous estradiol probes, DTPA-estradiol is a small molecule with a suitable molecular weight. It does not alter biodistribution or tumor uptake patterns [21]. In addition, unlike other studies highlighting the difficulty of preparing 99m Tc-labeled derivatives with high specific activity or yields [9,11], 99m Tc-DTPA-estradiol was prepared easily, with a satisfactory yield and labeling efficiency.…”

Section: Accepted Manuscriptmentioning

confidence: 99%

See 1 more Smart Citation

99m Tc-labeled estradiol as an estrogen receptor probe: Preparation and preclinical evaluation

Xia

Feng

et al. 2016

Nuclear Medicine and Biology

View full text Add to dashboard Cite

“…PET/CT and SPECT/CT agents show high specific activities because they are made through a nuclear transformation and use carrier free forms of isotopes. Moreover, PET/CT and SPECT/CT chelator-based agents do not produce detectable pharmacologic effects but provide important information concerning the characterization of varieties diseases, such as vascular angiogenesis [4][5][6], hypoxia [7][8][9], apoptosis [10][11], cellular signaling and transcriptional activity [12][13][14]. PET/CT and SPECT/CT may assist in the determination of optimal therapeutic dosing, differential diagnosis between inflammation/infection and recurrence, sensitive or resistant to treatment response, grading of tumors, and the prediction of treatment response by selecting patient who may or may not respond to therapy.…”

Section: Importance Of Nuclear Molecular Imaging In Oncologymentioning

confidence: 99%

Molecular Imaging Kits for Hexosamine Biosynthetic Pathway in Oncology

Yang

Kong²,

Oka³

et al. 2012

curr med chem

View full text Add to dashboard Cite

Noninvasive imaging assessment of tumor cell proliferation could be helpful in the evaluation of tumor growth potential, the degree of malignancy, and could provide an early assessment of treatment response prior to changes in tumor size determined by computed tomography (CT), magnetic resonance imaging (MRI), Positron emission tomography (PET), Single-Photon emission computed tomography (SPECT) or ultrasonography, respectfully. Understanding of tumor proliferative activity, in turn, could aid in the selection of optimal therapy by estimating patient prognosis and selecting the proper management. PET/CT imaging of (18)F-fluoro-2-deoxy-glucose (FDG) is recognized as a technology for diagnosing the presence and extent of several cancer types. Recently, radiolabeled glucosamine analogues were introduced as a promising SPECT agent to complement FDG imaging to increase specificity and improve the accuracy of lesion size in oncology applications. Radiolabeled glucosamine analogues were developed to localize in the nuclear components of cells primarily via the hexosamine biosynthetic pathway whereas glucose localizes in the cytoplasm of cells through the glycolytic/TCA pathway. This paper reviews novel kit-based radiolabeled glucosamine analogues for metabolic imaging of tumor lesions. The novel radiolabeled glucosamine analogues may increase the specificity in oncology applications and can influence patient diagnosis, planning and monitoring of cancer treatment.

show abstract

Targeted functional imaging of estrogen receptors with 99mTc-GAP-EDL

Abstract: Cellular or tumor uptake of (99m)Tc-GAP-EDL occurs via an ER-mediated process. (99m)Tc-GAP-EDL is a useful agent for imaging functional ER(+) disease.

Cited by 23 publications

References 28 publications

Structural Consideration in Designing Organotin Polyethers to Arrest the Growth of Breast Cancer Cells In Vitro

Structural Consideration in Designing Organotin Polyethers to Arrest the Growth of Breast Cancer Cells In Vitro

99m Tc-labeled estradiol as an estrogen receptor probe: Preparation and preclinical evaluation

Molecular Imaging Kits for Hexosamine Biosynthetic Pathway in Oncology

Contact Info

Product

Resources

About