| Synthesis and biological evaluation of water-soluble progesterone-conjugated probes for magnetic resonance imaging of hormone related cancers. | |
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MedLine Citation:
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PMID: 21972997 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Progesterone receptor (PR) is strongly associated with disease prognosis and therapeutic efficacy in hormone-related diseases such as endometriosis and breast, ovarian, and uterine cancers. Receptor status is currently determined by immunohistochemistry assays. However, noninvasive PR imaging agents could improve disease detection and help elucidate pathological molecular pathways, leading to new therapies and animal disease models. A series of water-soluble PR-targeted magnetic resonance imaging (MRI) probes were synthesized using Cu(I)-catalyzed click chemistry and evaluated in vitro and in vivo. These agents demonstrated activation of PR in vitro and preferential accumulation in PR(+) compared to PR(-) human breast cancer cells with low toxicity. In xenograft tumor models, the agents demonstrated enhanced signal intensity in PR(+) tumors compared to PR(-) tumors. The results suggest that these agents may be promising MRI probes for PR(+) diseases. |
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Authors:
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Preeti A Sukerkar; Keith W MacRenaris; Taryn R Townsend; Roshan A Ahmed; Joanna E Burdette; Thomas J Meade |
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Publication Detail:
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Type: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S. Date: 2011-10-05 |
Journal Detail:
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Title: Bioconjugate chemistry Volume: 22 ISSN: 1520-4812 ISO Abbreviation: Bioconjug. Chem. Publication Date: 2011 Nov |
Date Detail:
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Created Date: 2011-11-17 Completed Date: 2012-03-19 Revised Date: 2013-02-19 |
Medline Journal Info:
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Nlm Unique ID: 9010319 Medline TA: Bioconjug Chem Country: United States |
Other Details:
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Languages: eng Pagination: 2304-16 Citation Subset: IM |
Affiliation:
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Department of Chemistry, Northwestern University, 2145 Sheridan Road, Evanston, Illinois 60208, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Azides / chemical synthesis, chemistry, metabolism Click Chemistry / methods Contrast Media / chemical synthesis*, chemistry*, metabolism Europium / chemistry Female Gadolinium / chemistry Humans Magnetic Resonance Imaging / methods* Mice Mice, Inbred BALB C Mice, Nude Molecular Structure Neoplasm Transplantation Neoplasms, Experimental / diagnosis, metabolism*, pathology* Progesterone / chemistry*, metabolism Receptors, Progesterone / genetics, metabolism Water / chemistry* |
| Grant Support | |
ID/Acronym/Agency:
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1S10RR025624-01/RR/NCRR NIH HHS; P30 CA060553/CA/NCI NIH HHS; R01 EB005866-07/EB/NIBIB NIH HHS; R01EB005866/EB/NIBIB NIH HHS; R21 CA143331-02/CA/NCI NIH HHS; R21CA143331/CA/NCI NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Azides; 0/Contrast Media; 0/Receptors, Progesterone; 57-83-0/Progesterone; 7440-53-1/Europium; 7440-54-2/Gadolinium; 7732-18-5/Water |
| Comments/Corrections | |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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