Synthesis and preliminary biological evaluation of MMP inhibitor radiotracers [11C]methyl-halo-CGS 27023A analogs, new potential PET breast cancer imaging agents

Zheng, Qi; Fei, Xiangshu; Li, Xuan; Wang, Ji Quan; Sun, Hui; Mock, Bruce H.; Stone, K. Lee; Martinez, Tanya D.; Miller, Kathy D.; Sledge, George W.; Hutchins, Gary D.

doi:10.1016/s0969-8051(02)00338-4

Cited by 74 publications

(34 citation statements)

References 30 publications

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“…Zheng et al have labeled potent MMPIs such as [ 11 C] MSMA or [ 11 C] CGS25966 and observed high levels of non-specific bindings of both inhibitors in mouse models of breast cancer [28]. These results conflicted with previous in vitro studies performed with the same reagents that demonstrated inhibitory effectiveness for several MMP subtypes [29].…”

Section: Pet and Spectmentioning

confidence: 98%

Imaging matrix metalloproteinases in cancer

Scherer

McIntyre

Matrisian

2008

Cancer Metastasis Rev

155

138

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Early detection of both primary tumors and metastatic disease remains a major challenge in the diagnosis and staging of cancer. The recognition of the role of MMPs in both the growth and metastasis of tumors has guided the development not only of therapeutic strategies utilizing synthetic, small-molecule MMP inhibitors (MMPIs), but has also catalyzed methods to detect and image tumors in vivo by means of tumor-associated proteolytic activity. These imaging approaches target MMPs involved in cancer progression via contrast agents linked to MMPIs or to MMP selective and specific substrates with sensitivity enhanced by amplification during enzymatic processing. This review draws attention to a variety of strategies utilized to image MMP activity in vivo.

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Section: Pet and Spectmentioning

confidence: 98%

Imaging matrix metalloproteinases in cancer

Scherer

McIntyre

Matrisian

2008

Cancer Metastasis Rev

155

138

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show abstract

“…As with many imaging agents, the proof of principle of imaging of MMPs was obtained in tumors. [81][82][83][84][85][86][87] Substantial studies with MMP imaging have been undertaken in the imaging of atherosclerotic plaques wherein the MMPs have been implicated in plaque instability and fibrous cap thinning. Schäfers et al reported the feasibility of MMP imaging using 123 I-labeled broad-spectrum MMP inhibitor (CGS 27023A) in a carotid ligation model of atherosclerosis in ApoE −/− mice.…”

Section: Imaging Matrix-degrading Enzymesmentioning

confidence: 99%

Molecular Imaging of the Cardiac Extracellular Matrix

Haas

Arbustini

Fuster

et al. 2014

Circulation Research

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“…Therefore, the development of MMP-targeted tracers has been focused on constructs that will selectively bind to the active MMP catalytic domain. 14,[17][18][19][20] Chen et al 20 recently demonstrated the feasibility of ex vivo imaging of MMP activity after MI using a near-infrared fluorescent probe that is activated by the cleavage of 2 of the gelatinases (MMP2 and MMP9). However, application of MMP-targeted radiotracers or near-infrared fluorescent probes for in vivo myocardial imaging after an MI has not been performed previously.…”

Section: Role Of Mmp Activation In Post-mi Remodelingmentioning

confidence: 99%