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Our structural data showed subtle changes in the binding pose between Vorapaxar and F16357. Transmembrane helices 1, 2, 5, and 7 were most significantly affected; most notably a large kink at F279(5.47) in TM helix 5 of the Vorapaxar complex was completely absent in the F16357 complex. The results of this study facilitate the future development of other therapeutic PAR1 (zeige MARK2 Proteine) antagonists.
Platelets were activated in antineutrophil cytoplasmic antibody (ANCA)-associated vasculitis (AAV) patients, and such activation was at least partially attributed to the thrombin (zeige F2 Proteine)-protease-activated receptors (PARs (zeige EPRS Proteine)) pathway.
Using protein C (zeige PROC Proteine)-factor VII (zeige TH Proteine) chimera demonstrate that APC (zeige APC Proteine) light chain amino acid residues outside the EPCR (zeige PROCR Proteine)-binding site enable cytoprotective PAR1 (zeige MARK2 Proteine) signaling.
Study demonstrated that nerve activation by mucosal biopsy supernatants depends on proteases. This is a common feature of quiescent ulcerative colitis and irritable bowel syndrome (IBS) and may relate to some common gastrointestinal symptoms. However, only proteases in IBS supernatants signal through PAR1 (zeige MARK2 Proteine).
Data show there was no significant correlation of autoantibodies to coagulation factor II thrombin receptor (F2R; protease-activated receptor 1, PAR1) (PAR1-AB) level with , progression-free (PFS) and overall (OS) survival.
we found that activation of the protease-activated receptor 1 (PAR1) induced secretion of TSLP (zeige TSLP Proteine) by the corneal stromal cells... we proposed that TSLP (zeige TSLP Proteine) might function as the link between increased protease activity and inflammatory responses or itch sensation in the
PAR-1 (zeige MARK2 Proteine) in non-small-cell lung cancer is mainly expressed on cells that constitute the pulmonary tumor microenvironment, including vascular endothelial cells, macrophages and stromal fibroblasts.
thrombin (zeige F2 Proteine) binding to PAR-1 (zeige MARK2 Proteine) receptor activated Gi-protein/c (zeige PROC Proteine)-Src (zeige SRC Proteine)/Pyk2 (zeige PTK2B Proteine)/EGFR (zeige EGFR Proteine)/PI3K (zeige PIK3CA Proteine)/Akt (zeige AKT1 Proteine)/p42/p44 (zeige PSMC6 Proteine) MAPK (zeige MAPK3 Proteine) cascade, which in turn elicited AP-1 (zeige FOSB Proteine) activation and ultimately evoked MMP-9 (zeige MMP9 Proteine) expression and cell migration in SK-N-SH cells.
this study demonstrates that TGFbeta (zeige TGFB1 Proteine) is a positive regulator of PAR-1 (zeige MARK2 Proteine) expression in A549 lung adenocarcinoma cells, which in turn increases the sensitivity of these cells to thrombin (zeige F2 Proteine) signalling
Taken together, these results indicated that PAR1 (zeige MARK2 Proteine) signalingmediated cJun (zeige JUN Proteine) activation promotes early apoptosis of HUVEC cells induced by heat stress.
PAR-1 (zeige MARK2 Proteine) plays an important role in the development of diabetic nephropathy (DN) and PAR-1 (zeige MARK2 Proteine) might therefore be an attractive therapeutic target to pursue in DN.
Experimental TCDD-elicited steatohepatitis is associated with coagulation cascade activation and PAR-1 (zeige MARK2 Proteine)-driven hepatic inflammation and fibrosis.
PAR1 in its inactive unligated state functions as a scaffold for TGFbetaRII to downregulate TGF-beta (zeige TGFB1 Proteine) signaling, and thereby promote embryonic stem cell transition to functional endothelial cells.
this study shows that poly I:C treated PAR-1 (zeige MARK2 Proteine)-/- mice given the thrombin (zeige F2 Proteine) inhibitor dabigatran etexilate exhibited less IFNbeta and CXCL10 (zeige CXCL10 Proteine) expression in the spleen and plasma
Brain water content in the ipsilateral hemisphere and the tumor mass were significantly lower in PAR-1 (zeige MARK2 Proteine) KO than WT mice at day 12 after implantation of glioma cells.
The results of this study suggested that polarized microglia occur dynamically after ICH (zeige ACE Proteine) and that PAR-1 (zeige MARK2 Proteine) plays a role in the microglia activation and polarization.
In this study, we found upregulation of several hemostasis-related genes, including the thrombin (zeige F2 Proteine)-activatable receptor PAR-1 (protease-activated receptor-1), in Runx1 (zeige RUNX1 Proteine)/Cbfb (zeige CBFB Proteine)-deleted MLL (zeige MLL Proteine)-AF9 (zeige MLLT3 Proteine) cells. Similar to the effect of Runx1 (zeige RUNX1 Proteine)/Cbfb (zeige CBFB Proteine) deletion, PAR-1 (zeige MARK2 Proteine) overexpression induced CDKN1A/p21 (zeige CDKN1A Proteine) expression and attenuated proliferation in MLL (zeige MLL Proteine)-AF9 (zeige MLLT3 Proteine) cells
our findings define a detrimental role of thrombin (zeige F2 Proteine)-activated PAR-1 (zeige MARK2 Proteine) in wound healing in mice with spinal cord injuries.
thrombin (zeige F2 Proteine)/PAR-1 (zeige MARK2 Proteine) interaction regulated MCP-1 (zeige CPT1B Proteine), TF, MCSF (zeige CSF1 Proteine) and IL-6 (zeige IL6 Proteine) production.
Thrombin (zeige F2 Proteine) upregulates LCN2 (zeige LCN2 Proteine) through protease-activated receptor-1 activation and causes brain damage.
Thrombin stimulates swine smooth muscle cell differentiation from peripheral blood mononuclear cells via protease-activated receptor-1, RhoA, and myocardin.
Thrombin (zeige F2 Proteine) induces a sustained contraction in the normal pulmonary artery, by activating PAR(1) and thereby increasing the sensitivity of the myofilament to Ca(2 (zeige CA2 Proteine)+).
MMP-1 (zeige MMP1 Proteine) promotes VEGFR2 (zeige KDR Proteine) expression and proliferation of endothelial cells through stimulation of PAR-1 and activation of NF-kappaB (zeige NFKB1 Proteine)
PAR1 and PAR2 regulate endothelial NO synthase phosphorylation and activity through G(12/13) and G(q), delineating the signaling pathways by which the proteases act on protease-activated receptors to modulate endothelial functions.
Coagulation factor II receptor is a 7-transmembrane receptor involved in the regulation of thrombotic response. Proteolytic cleavage leads to the activation of the receptor. F2R is a G-protein coupled receptor family member.
protease-activated receptor 1
, proteinase-activated receptor 1
, Thrombin receptor
, coagulation factor II receptor
, thrombin receptor
, protease-activated receptor-1
, coagulation factor II (thrombin) receptor