Article ; Online: Preclinical evaluation of [
Journal of labelled compounds & radiopharmaceuticals
2020 Volume 64, Issue 4, Page(s) 159–167
Abstract: The cathepsin K (CatK) enzyme is abundantly expressed in osteoclasts, and CatK inhibitors have been developed for the treatment of osteoporosis. In our effort to support discovery and clinical evaluations of a CatK inhibitor, we sought to discover a ... ...
Abstract | The cathepsin K (CatK) enzyme is abundantly expressed in osteoclasts, and CatK inhibitors have been developed for the treatment of osteoporosis. In our effort to support discovery and clinical evaluations of a CatK inhibitor, we sought to discover a radioligand to determine target engagement of the enzyme by therapeutic candidates using positron emission tomography (PET). L-235, a potent and selective CatK inhibitor, was labeled with carbon-11. PET imaging studies recording baseline distribution of [ |
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MeSH term(s) | Animals ; Bone and Bones/diagnostic imaging ; Carbon Radioisotopes/chemistry ; Cathepsin K/antagonists & inhibitors ; Cysteine Proteinase Inhibitors/chemistry ; Drug Evaluation, Preclinical ; Female ; Ligands ; Macaca mulatta ; Osteoporosis/diagnostic imaging ; Positron Emission Tomography Computed Tomography/methods ; Protein Binding ; Rabbits ; Radiopharmaceuticals/adverse effects ; Radiopharmaceuticals/chemistry ; Radiopharmaceuticals/pharmacokinetics ; Tissue Distribution |
Chemical Substances | Carbon Radioisotopes ; Cysteine Proteinase Inhibitors ; Ligands ; Radiopharmaceuticals ; Cathepsin K (EC 3.4.22.38) |
Language | English |
Publishing date | 2020-12-02 |
Publishing country | England |
Document type | Journal Article |
ZDB-ID | 196095-7 |
ISSN | 1099-1344 ; 0362-4803 ; 0022-2135 |
ISSN (online) | 1099-1344 |
ISSN | 0362-4803 ; 0022-2135 |
DOI | 10.1002/jlcr.3896 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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