期刊
MEDCHEMCOMM
卷 2, 期 5, 页码 396-401出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c0md00264j
关键词
-
资金
- American Cancer Society [RGS-09-057-01-GMC]
Since mutations of Ras genes have a great incidence in human tumours, Ras oncoproteins are a major clinical target for the development of anticancer agents. We have developed synthetic molecules able to inhibit Ras activation. Here we present new, water-soluble Ras inhibitors composed by an aromatic pharmacofore moiety covalently linked to different sugars. New glycosylated compounds bind to Switch 2 region of Ras, also involved in effector binding, inhibit GEF-catalyzed nucleotide exchange on Ras in vitro, and reduce Ras-dependent proliferation of murine fibroblasts. The influence of the sugar unit on Ras binding affinity and on the biological activity of Ras inhibitors has been investigated.
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