Abstract:
:In the present study, we report the synthesis and biological evaluation of a series of new non-peptide PAR(1) mimetic receptor antagonists, based on conformational analysis of the S(42)FLLR(46) tethered ligand (TL) sequence of PAR(1). These compounds incorporate the key pharmacophore groups in the TL sequence, guanidyl, amino and phenyl, which are essential for triggering receptor activity. Compounds 5 and 15 (50-100 microM) inhibited both TFLLR-amide (10 microM) and thrombin-mediated (0.5 and 1 U/ml; 5 and 10 microM) calcium signaling in a cultured human HEK cell assay.
journal_name
Amino Acidsjournal_title
Amino acidsauthors
Androutsou ME,Saifeddine M,Hollenberg MD,Matsoukas J,Agelis Gdoi
10.1007/s00726-009-0306-zsubject
Has Abstractpub_date
2010-04-01 00:00:00pages
985-90issue
4eissn
0939-4451issn
1438-2199journal_volume
38pub_type
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