Small animal positron emission tomography in food sciences

Bergmann, Ralf; Pietzsch, Jens

doi:10.1007/s00726-005-0237-2

Cited by 7 publications

(3 citation statements)

References 239 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…This physical phenomenon allows the construction of images and time-activity curves by coincidence detection of the two photons using a circular array of scintillation detectors (James and Gambhir, 2012 ). This makes PET to a unique method for quantitative tracing compounds in living organisms (Bergmann and Pietzsch, 2005 ). Of note, far reaching progress in clinical PET technology has also led to the design and development of dedicated small animal PET systems that now are abundantly prevalent in biomedical and pharmaceutical research.…”

Section: Recent Trends In the Development Of Cysteine Cathepsin-targementioning

confidence: 99%

Cysteine cathepsins: their role in tumor progression and recent trends in the development of imaging probes

Löser

Pietzsch

2015

Front. Chem.

View full text Add to dashboard Cite

Papain-like cysteine proteases bear an enormous potential as drug discovery targets for both infectious and systemic human diseases. The considerable progress in this field over the last two decades has also raised interest in the visualization of these enzymes in their native context, especially with regard to tumor imaging. After a short introduction to structure and general functions of human cysteine cathepsins, we highlight their importance for drug discovery and development and provide a critical update on the current state of knowledge toward their involvement in tumor progression, with a special emphasis on their role in therapy response. In accordance with a radiopharmaceutical point of view, the main focus of this review article will be the discussion of recently developed fluorescence and radiotracer-based imaging agents together with related molecular probes.

show abstract

Section: Recent Trends In the Development Of Cysteine Cathepsin-targementioning

confidence: 99%

Cysteine cathepsins: their role in tumor progression and recent trends in the development of imaging probes

Löser

Pietzsch

2015

Front. Chem.

View full text Add to dashboard Cite

show abstract

“…Moreover, PET has also entered the field of modern drug development and evaluation. It provides a unique platform to study pharmacokinetics, pharmacodynamics, and the mode of action of novel drugs in both animal models and humans [20]. …”

Section: Introductionmentioning

confidence: 99%

Cell Cycle Regulating Kinase Cdk4 as a Potential Target for Tumor Cell Treatment and Tumor Imaging

Graf

Koehler

Knieß

et al. 2009

Journal of Oncology

View full text Add to dashboard Cite

The cyclin-dependent kinase (Cdk)-cyclin D/retinoblastoma (pRb)/E2F cascade, which controls the G1/S transition of cell cycle, has been found to be altered in many neoplasias. Inhibition of this pathway by using, for example, selective Cdk4 inhibitors has been suggested to be a promising approach for cancer therapy. We hypothesized that appropriately radiolabeled Cdk4 inhibitors are suitable probes for tumor imaging and may be helpful studying cell proliferation processes in vivo by positron emission tomography. Herein, we report the synthesis and biological, biochemical, and radiopharmacological characterizations of two 124I-labeled small molecule Cdk4 inhibitors (8-cyclopentyl-6-iodo-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]-pyrimidin-7-one (CKIA) and 8-cyclopentyl-6-iodo-5-methyl-2-(5-(piperazin-1-yl)-pyridin-2-yl-amino)-8H-pyrido[2,3-d]pyrimidin-7-one (CKIB)). Our data demonstrate a defined and specific inhibition of tumor cell proliferation through CKIA and CKIB by inhibition of the Cdk4/pRb/E2F pathway emphasizing potential therapeutic benefit of CKIA and CKIB. Furthermore, radiopharmacological properties of [124I]CKIA and [124I]CKIB observed in human tumor cells are promising prerequisites for in vivo biodistribution and imaging studies.

show abstract

“…In this context, it represents a promising approach for imaging and quantitative assessment of the metabolic fate and accumulation sites of bioactive compounds, including drugs and nutraceuticals. 18 F-PET enables non-invasive in vivo analysis without tissue destruction and without being influenced by the composition of the tissue studied 2 . In this context, great effort has recently been devoted to the development of new and efficient strategies for the introduction of 18 F atoms into peptides 3–8 and metabolites of interest 9,10 .…”

Section: Introductionmentioning

confidence: 99%