Document Detail

Synthesis and biological evaluation of water-soluble progesterone-conjugated probes for magnetic resonance imaging of hormone related cancers.
MedLine Citation:
PMID:  21972997     Owner:  NLM     Status:  MEDLINE    
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.
Preeti A Sukerkar; Keith W MacRenaris; Taryn R Townsend; Roshan A Ahmed; Joanna E Burdette; Thomas J Meade
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Publication Detail:
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:
Title:  Bioconjugate chemistry     Volume:  22     ISSN:  1520-4812     ISO Abbreviation:  Bioconjug. Chem.     Publication Date:  2011 Nov 
Date Detail:
Created Date:  2011-11-17     Completed Date:  2012-03-19     Revised Date:  2014-09-21    
Medline Journal Info:
Nlm Unique ID:  9010319     Medline TA:  Bioconjug Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  2304-16     Citation Subset:  IM    
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MeSH Terms
Azides / chemical synthesis,  chemistry,  metabolism
Click Chemistry / methods
Contrast Media / chemical synthesis*,  chemistry*,  metabolism
Europium / chemistry
Gadolinium / chemistry
Magnetic Resonance Imaging / methods*
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
1S10RR025624-01/RR/NCRR NIH HHS; P30 CA060553/CA/NCI NIH HHS; R01 EB005866/EB/NIBIB NIH HHS; R01 EB005866-07/EB/NIBIB NIH HHS; R01EB005866/EB/NIBIB NIH HHS; R21 CA143331/CA/NCI NIH HHS; R21 CA143331-02/CA/NCI NIH HHS; R21CA143331/CA/NCI NIH HHS; U54 CA151880/CA/NCI NIH HHS
Reg. No./Substance:
0/Azides; 0/Contrast Media; 0/Receptors, Progesterone; 059QF0KO0R/Water; 444W947O8O/Europium; 4G7DS2Q64Y/Progesterone; AU0V1LM3JT/Gadolinium

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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