Selective Activity-Based Probes Targeting Fibroblast Activation Protein (FAP)
نویسندگان
چکیده
منابع مشابه
Fibroblast activation protein (FAP) as a novel metabolic target
OBJECTIVE Fibroblast activation protein (FAP) is a serine protease belonging to a S9B prolyl oligopeptidase subfamily. This enzyme has been implicated in cancer development and recently reported to regulate degradation of FGF21, a potent metabolic hormone. Using a known FAP inhibitor, talabostat (TB), we explored the impact of FAP inhibition on metabolic regulation in mice. METHODS To address...
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The protease fibroblast activation protein (FAP) is a specific marker of activated mesenchymal cells in tumour stroma and fibrotic liver. A specific, reliable FAP enzyme assay has been lacking. FAP's unique and restricted cleavage of the post proline bond was exploited to generate a new specific substrate to quantify FAP enzyme activity. This sensitive assay detected no FAP activity in any tiss...
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Mark D. Gorrell, Xin M. Wang, Miriam T. Levy, Eleanor Kable, George Marinos , Guy Cox and Geoffrey W. McCaughan 1. A. W. Morrow Gastroenterology and Liver Centre, Royal Prince Alfred Hospital, Centenary Institute of Cancer Medicine and Cell Biology and the University of Sydney, NSW Australia. 2. Electron Microscope Unit, University of Sydney. 3. Gastroenterology Department, Prince of Wales Hosp...
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Caspases are cysteine proteases that are key effectors in apoptotic cell death. Currently, there is a lack of tools that can be used to monitor the regulation of specific caspases in the context of distinct apoptotic programs. We describe the development of highly selective inhibitors and active site probes and their applications to directly monitor executioner (caspase-3 and -7) and initiator ...
متن کاملFibroblast Activation Protein (FAP) Is Essential for the Migration of Bone Marrow Mesenchymal Stem Cells through RhoA Activation
BACKGROUND The ability of human bone marrow mesenchymal stem cells (BM-MSCs) to migrate and localize specifically to injured tissues is central in developing therapeutic strategies for tissue repair and regeneration. Fibroblast activation protein (FAP) is a cell surface serine protease expressed at sites of tissue remodeling during embryonic development. It is also expressed in BM-MSCs, but not...
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ژورنال
عنوان ژورنال: Proceedings
سال: 2019
ISSN: 2504-3900
DOI: 10.3390/proceedings2019022084