Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
Results
Showing 1 to 13 of 13 for “"PAR1"”.
-
Re-evaluation of the in vitro activity of the protease activated receptor-1 (PAR1) pepducin PZ-128
… formation. Protease-activated receptor 1 (PAR1) is a key target due to its role in thrombin-mediated platelet activation.;PZ-128 is a cell penetrable pepducin that targets PAR1 and has entered phase II clinical trials, however, adverse effects in trial subjects have emerged that warrant …
-
Ο ρόλος της θρομβίνης και των υποδοχέων της στην αγγειογένεση και στην ανάπτυξη και μετάσταση του καρκίνου
Απο τις απαρχές της μελέτης του PAR1, είχε βρεθεί οτι βρίσκεται σε στενή συνάφεια με τον καρκίνο, με ποικιλία πειραμάτων που έγιναν σε καρκινικές σειρές και σε διάφορα πειραματικά μοντέλα ζώων. Οι σκοποί της παρούσας εργασίας μπορούν να συνοψιστούν ως εξης: Η διερεύνηση της έκφρασης του υποδοχέα 1 …
-
Signaling By Protease-Activated Receptors in Gastrointestinal Smooth Muscle
… kinase activity and inhibited cAMP formation. PAR1-stimulated PI hydrolysis was abolished in cells expressing Gαq minigene, but was not affected in cells expressing Gαi minigene or in cells treated with pertussis toxin (PTx). PAR2-stimulated PI hydrolysis was partially inhibited in cells …
-
The role of C-terminal cysteines in regulating human proteinase-activated receptor-1 function
… have been identified so far in this group—PAR1, PAR2, PAR3 and PAR4. Palmitoylation is the reversible covalent attachment of fatty acids to the cysteine residues of some GPCRs via a thioester linkage; resulting in a fourth intracellular loop. Although recent evidence has suggested that …
-
Characterisation of the conformational landscape of the β1-adrenergic receptor and development of a strategy towards NMR studies of the protease-activated receptor 1
… target, the human Protease activated receptor 1 (PAR1). The PAR1 is mostly associated with regulation of haemostasis and as such a high potential target for clinical research. I established the construct, expression, purification and 19F labelling of the PAR1 and obtained initial 19F NMR spectra. …
-
Structural And Functional Studies On Thrombin Allostery
… The case of protease-activated receptor: PAR1) is particularly relevant in view of the plethora of biological effects associated with its activation by thrombin. We present the crystal structure of thrombin in complex with a 30-residue long uncleaved extracellular fragment of PAR1. The …
-
Investigating novel therapeutic targets for treatment of visceral pain.
… with the protease activated receptor-1 (PAR1) receptor antagonist SCH 79797. However, neither the application of MMP1 or the PAR1 agonist, TRAP-6 produced a direct activation of colonic afferent activity despite expression of PAR1 receptors in colonic projecting sensory neurons. Further …
-
Identification of a vascular smooth muscle cell transition associated with fibrous cap formation and induced by thrombin receptor activation
… From this, protease-activated receptor-1 (PAR1) emerged as a candidate regulator of fcVSMC generation. PAR1 was expressed in VSMCs within the fibrous caps of human plaques and its activation by thrombin in cultured human VSMCs induced expression of contractile, ECM and other genes …
-
IKAROS and LEUKEMIA
… by deletions of the pseudoautosomal region 1 (PAR1), and JAK2 mutations were significantly overrepresented in abnIKZF1-positive cases and that the presence of PAR1 deletions conferred a poor prognostic impact. Thus, in order to ascertain correctly the clinical ramifications of abnIKZF1 in …
-
Πειραματική πρόκληση νεοαγγείωσης του κερατοειδούς
… μετά την πρωτεολυτική ενεργοποίηση του PAR1 υποδοχέα και περιέχει μια έντονα υδρόφοβη και μια έντονα υδρόφιλη περιοχή (αλληλουχία αμινοξέων). Πρόσφατα, αποδείχθηκε ότι η παρστατίνη είναι ένας ισχυρός αναστολέας της αγγειογένεσης. Ο σκοπός αυτής της εργασίας ήταν η ανάπτυξη ενός μοντέλου …
-
A study of the regulation of oestrogen receptor alpha by tissue factor in breast cancer cells
… of the ERK1/2 pathway, but was independent of PAR1 and PAR2 activation. Furthermore, exogenous TF suppressed oestradiol-mediated cell proliferation through a pathway partly mediated through PAR2 activation, and also reversed the inhibitory influence of oestradiol on cell invasion. Exogenous TF …