| dc.contributor.author | Kumar, Anil | |
| dc.date.accessioned | 2021-10-27T04:11:32Z | |
| dc.date.available | 2021-10-27T04:11:32Z | |
| dc.date.issued | 2006 | |
| dc.identifier.uri | https://pubs.acs.org/doi/10.1021/jm060334k | |
| dc.identifier.uri | http://dspace.bits-pilani.ac.in:8080/xmlui/handle/123456789/2950 | |
| dc.description.abstract | A series of peptide analogues of Ac-CIYKYY (1) were synthesized by functional group modifications in peptide side chains or by introducing conformational constraints, to improve the inhibitory potency against active Src kinase. Ac-CIYKF(4-NO2)Y (2, IC50 = 0.53 μM) and conformationally constrained peptide 31 (IC50 = 0.28 μM) exhibited 750- and 1400-fold higher inhibitory activities, respectively, versus that of 1 (IC50 = 400 μM). Compound 2 exhibited a partial competitive inhibition pattern against ATP. | en_US |
| dc.language.iso | en | en_US |
| dc.publisher | ACS | en_US |
| dc.subject | Chemistry | en_US |
| dc.subject | Peptides and proteins | en_US |
| dc.subject | Monomers | en_US |
| dc.subject | Inhibitors | en_US |
| dc.subject | Functional groups | en_US |
| dc.title | Synthesis and structure-activity relationships of linear and conformationally constrained peptide analogues of CIYKYY as Src tyrosine kinase inhibitors | en_US |
| dc.type | Article | en_US |
| Files | Size | Format | View |
|---|---|---|---|
|
There are no files associated with this item. |
|||