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Arylamide derivatives as peptidomimetic inhibitors of calmodulin.
- Source :
-
Organic letters [Org Lett] 2006 Jan 19; Vol. 8 (2), pp. 223-5. - Publication Year :
- 2006
-
Abstract
- [structure: see text] Many peptides bind to calmodulin (CaM) in a helical conformation. Here we describe a group of synthetic inhibitors of CaM based on an arylamide scaffold that is intended to mimic smMLCK, a CaM-binding helical peptide. Compound 1 showed a K(i) value of 7.10 +/- 1.48 nM in a fluorescence polarization assay that monitors the strong association of CaM and its peptide ligand mastoparan X. ((1)H,(15)N)-HSQC NMR spectroscopy experiments suggested that 1 binds to CaM in an analogous fashion to that of smMLCK.
Details
- Language :
- English
- ISSN :
- 1523-7060
- Volume :
- 8
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Organic letters
- Publication Type :
- Academic Journal
- Accession number :
- 16408880
- Full Text :
- https://doi.org/10.1021/ol052478j