A Single Second Shell Amino Acid Determines Affinity and Kinetics of Linagliptin Binding to Type 4 Dipeptidyl Peptidase and Fibroblast Activation Protein
Sign Up to like & getrecommendations! Published in 2020 at "Chemmedchem"
DOI: 10.1002/cmdc.202000591
Abstract: Drugs targeting type 4 dipeptidyl peptidase (DPP‐4) are beneficial for glycemic control, whereas fibroblast activation protein alpha (FAP‐α) is a potential target for cancer therapies. Unlike other gliptins, linagliptin displays FAP inhibition. We compared biophysical… read more here.
Keywords: amino; amino acid; type dipeptidyl; dipeptidyl peptidase ... See more keywords
β‐catenin‐controlled tubular cell‐derived exosomes play a key role in fibroblast activation via the OPN‐CD44 axis
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Extracellular Vesicles"
DOI: 10.1002/jev2.12203
Abstract: Abstract Tubular injury and peripheral fibroblast activation are the hallmarks of chronic kidney disease (CKD), suggesting intimate communication between the two types of cells. However, the underlying mechanisms remain to be determined. Exosomes play a… read more here.
Keywords: cd44; catenin controlled; role; exosomes play ... See more keywords
Potential disease biomarkers: dipeptidyl peptidase 4 and fibroblast activation protein
Sign Up to like & getrecommendations! Published in 2017 at "Protoplasma"
DOI: 10.1007/s00709-017-1129-5
Abstract: The importance of the dipeptidyl peptidase 4 (DPP4) gene family in regulating critical biochemical pathways continues to emerge. The two most well-studied members of the family, DPP4 and fibroblast activation protein (FAP), have been investigated… read more here.
Keywords: disease biomarkers; disease; potential disease; activation protein ... See more keywords
Evodiamine attenuates TGF-β1-induced fibroblast activation and endothelial to mesenchymal transition
Sign Up to like & getrecommendations! Published in 2017 at "Molecular and Cellular Biochemistry"
DOI: 10.1007/s11010-017-2956-6
Abstract: The aim of this study is to investigate the effect of evodiamine on fibroblast activation in cardiac fibroblasts and endothelial to mesenchymal transition (EndMT) in human umbilical vein endothelial cells (HUVECs). Neonatal rat cardiac fibroblasts… read more here.
Keywords: endothelial mesenchymal; huvecs; cardiac fibroblasts; activation ... See more keywords
A Trifunctional Theranostic Ligand Targeting Fibroblast Activation Protein-α (FAPα)
Sign Up to like & getrecommendations! Published in 2021 at "Molecular Imaging and Biology"
DOI: 10.1007/s11307-021-01593-1
Abstract: Fibroblast activation protein-α (FAPα) is uniquely expressed in activated fibroblasts, including cancer-associated fibroblasts that populate tumor stroma and contribute to proliferation and immunosuppression. Radiolabeled FAPα inhibitors enable imaging of multiple human cancers, but time-dependent clearance… read more here.
Keywords: fap; rps 309; activation protein; ligand ... See more keywords
Myocardial fibroblast activation imaging in light chain cardiac amyloidosis
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Nuclear Cardiology"
DOI: 10.1007/s12350-022-02963-0
Abstract: Light chains (AL) amyloidosis is a rare but lifethreatening disease. Cardiac involvement has the worst prognosis of any involved organ. Early identification of heart involvement may allow for prompt intervention and prevent irreversible myocardial remodeling.… read more here.
Keywords: light; cardiac amyloidosis; amyloidosis; fapi imaging ... See more keywords
Targeting Extracellular Matrix Glycation to Attenuate Fibroblast Activation.
Sign Up to like & getrecommendations! Published in 2022 at "Acta biomaterialia"
DOI: 10.1016/j.actbio.2022.01.040
Abstract: The extracellular matrix (ECM) of the tumor microenvironment undergoes constant remodeling that alters its biochemical and mechano-physical properties. Non-enzymatic glycation can induce the formation of advanced glycation end-products (AGEs), which may cause abnormal ECM turnover… read more here.
Keywords: age; extracellular matrix; glycation; matrix ... See more keywords
Long non-coding RNA Linc00092 inhibits cardiac fibroblast activation by altering glycolysis in an ERK-dependent manner.
Sign Up to like & getrecommendations! Published in 2020 at "Cellular signalling"
DOI: 10.1016/j.cellsig.2020.109708
Abstract: AIMS Cardiac fibroblast (CF) activation is the key event for cardiac fibrosis. The role of glycolysis and the glycolysis-related lncRNAs in CF activation are unknown. Thus, we aimed to investigate the role of glycolysis in… read more here.
Keywords: glycolysis; cardiac fibroblast; hcf activation; linc00092 ... See more keywords
Identification of Fibroblast Activation Protein as an Osteogenic Suppressor and Anti-osteoporosis Drug Target.
Sign Up to like & getrecommendations! Published in 2020 at "Cell reports"
DOI: 10.1016/j.celrep.2020.108252
Abstract: Osteogenic suppressors such as Sclerostin not only regulate skeletal development and regeneration but also serve as anti-osteoporosis drug targets. However, very few druggable suppressors have been identified due to limited understanding of the molecular mechanisms… read more here.
Keywords: anti osteoporosis; drug; fibroblast activation; osteoporosis drug ... See more keywords
The Role of Fibroblast Activation Protein Ligands in Oncologic PET Imaging.
Sign Up to like & getrecommendations! Published in 2021 at "PET clinics"
DOI: 10.1016/j.cpet.2021.03.012
Abstract: Fibroblast activation protein inhibitor emerges as a novel and highly promising agent for diagnostic and possibly theranostic application in various malignant and non-malignant diseases. FAPI impresses with its selective expression in several pathologies, ligand induced… read more here.
Keywords: activation protein; role fibroblast; fibroblast activation;
Knockdown of NLRC5 inhibits renal fibroblast activation via modulating TGF‐&bgr;1/Smad signaling pathway
Sign Up to like & getrecommendations! Published in 2018 at "European Journal of Pharmacology"
DOI: 10.1016/j.ejphar.2018.03.045
Abstract: &NA; NLRC5, the largest member of the Nucleotide‐binding domain and leucine‐rich repeat (NLR) protein family, is recently proven to be a critical modulator in fibrogenesis. However, the role of NLRC5 in renal fibrosis remains unknown.… read more here.
Keywords: bgr; knockdown nlrc5; renal fibroblast; tgf bgr ... See more keywords