A Highly Selective Staurosporine Derivative Designed by a New Selectivity Filter

Title
A Highly Selective Staurosporine Derivative Designed by a New Selectivity Filter
Authors
Ibrahim M. El-Deeb정수진박병선유영준최기항양영목이상우김인태한동근이소하
Keywords
Staurosporine derivative; Selectivity filter; Kinase selectivity; Cancer
Issue Date
2011-05
Publisher
Bulletin of the Korean Chemical Society
Citation
VOL 32, NO 5, 1709-1714
Abstract
KIST301135 was semi-synthetically prepared by the reaction of Staurosporine with triphosgene in anhydrous dichloromethane. The structure of KIST301135 was confirmed by 1H NMR, 13C NMR, and high resolution mass spectrum. KIST301135 was initially tested in a single dose duplicate mode at a concentration of 20 nM over a panel of 53 kinases against Staurosporine as a positive control. KIST301135 has showed inhibitions above 75% in only 2 kinases (FLT3 and JAK3 kinases) of the 53 tested kinases, while Staurosporine has showed inhibitions above 80% in about 62% of the tested kinases. KIST301135 was retested at a 5-dose testing mode over the 9 kinases inhibited by percentages over 20 at the single dose testing in order to determine its IC50 values. KIST301135 has shown much improved kinase inhibitory selectivity relative to Staurosporine in its potency at JAK3 kinase and CAMK2b kinase.
URI
http://pubs.kist.re.kr/handle/201004/39744
ISSN
0253-2964
Appears in Collections:
KIST Publication > Article
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE