Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold
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...
متن کاملIntrahepatic expression of collagen and fibroblast activation protein (FAP) in hepatitis C virus infection.
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...
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...
متن کاملSelective COX-2 Inhibitors: A Review of Their Structure-Activity Relationships
Non-steroidal anti-inflammatory drugs (NSAIDs) are the competitive inhibitors of cyclooxygenase (COX), the enzyme which mediates the bioconversion of arachidonic acid to inflammatory prostaglandins (PGs). Their use is associated with the side effects such as gastrointestinal and renal toxicity. The therapeutic anti-inflammatory action of NSAIDs is produced by the inhibition of COX-2, while the ...
متن کاملSelective COX-2 Inhibitors: A Review of Their Structure-Activity Relationships
Non-steroidal anti-inflammatory drugs (NSAIDs) are the competitive inhibitors of cyclooxygenase (COX), the enzyme which mediates the bioconversion of arachidonic acid to inflammatory prostaglandins (PGs). Their use is associated with the side effects such as gastrointestinal and renal toxicity. The therapeutic anti-inflammatory action of NSAIDs is produced by the inhibition of COX-2, while the ...
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ژورنال
عنوان ژورنال: ACS Medicinal Chemistry Letters
سال: 2013
ISSN: 1948-5875,1948-5875
DOI: 10.1021/ml300410d