1024017-23-9Relevant academic research and scientific papers
Towards Optimized Bioavailability of 99mTc-Labeled Barbiturates for Non-invasive Imaging of Matrix Metalloproteinase Activity
Austrup, Melanie,Daniliuc, Constantin Gabriel,Faust, Andreas,Haufe, Günter,Hermann, Sven,Honold, Lisa,Konken, Christian Paul,Kopka, Klaus,Sch?fers, Michael,Schwegmann, Katrin,Zinnhardt, Bastian
, (2021/11/12)
Introduction: Dysregulated activity of matrix metalloproteinases (MMPs) drives a variety of pathophysiological conditions. Non-invasive imaging of MMP activity in vivo promises diagnostic and prognostic value. However, current targeting strategies by smal
A new generation of radiofluorinated pyrimidine-2,4,6-triones as MMP-targeted radiotracers for positron emission tomography
Schrigten, Daniela,Breyholz, Hans-J?rg,Wagner, Stefan,Hermann, Sven,Schober, Otmar,Sch?fers, Michael,Haufe, G?nter,Kopka, Klaus
, p. 223 - 232 (2012/03/11)
Radiolabeled C-5-disubstituted pyrimidine-2,4,6-triones have recently been suggested by our group as a class of potent matrix metalloproteinase (MMP) targeted radiotracers that can noninvasively visualize activated MMPs by means of positron emission tomography (PET). MMPs belong to the zinc- and calcium-dependent endopeptidases which are involved in the proteolytic degradation of components of the extracellular matrix (ECM) but also are capable of processing and releasing bioactive molecules such as growth factors, proteinase inhibitors, and cytokines. Locally increased levels of activated MMPs modulate and contribute to the progression of various diseases, such as cancer, atherosclerosis, stroke, arthritis, and others. Therefore, activated MMPs are suitable biological targets for the specific and noninvasive visualization of aforementioned pathologies in vivo. On the basis of our recent results, we here describe a series of new fluorinated pyrimidine-2,4,6-triones of the second generation with maintained MMP inhibition potencies (IC50 = 4-605 nM), which are fine-tuned toward more hydrophilic versions, and show the improved biodistribution behavior of one selected radiofluorinated pyrimidine-2,4,6-trione by means of small-animal PET.
Radiofluorinated pyrimidine-2,4,6-triones as molecular probes for noninvasive MMP-targeted imaging
Breyholz, Hans-Joerg,Wagner, Stefan,Faust, Andreas,Riemann, Burkhard,Hoeltke, Carsten,Hermann, Sven,Schober, Otmar,Schaefers, Michael,Kopka, Klaus
scheme or table, p. 777 - 789 (2011/01/05)
Matrix metalloproteinases (MMPs) are zinc- and calcium-dependent endopeptidases. Representing a subfamily of the metzincin superfamily, MMPs are involved in the proteolytic degradation of components of the extracellular matrix. Unregulated MMP expression,
