METHODS FOR INDUCING TUMOR REGRESSION, INHIBITING TUMOR GROWTH, AND INDUCING APOPTOSIS IN BREAST TUMORS WITH GERANYLGERANYLTRANSFERASE I INHIBITORS

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专利权人:

Said M. Sebti

发明人:

Said M. Sebti,Andrew D. Hamilton

申请号：

US13194022

公开号：

US20120035184A1

申请日:

2011.07.29

申请国别(地区):

US

年份:

2012

代理人:

摘要：

Methods of inducing tumor regression, inhibiting tumor growth, and inducing apoptosis with selective peptidomimetic inhibitors of geranylgeranyltransferase I (GGTase I), are provided. In one aspect, GGTI-2418 and its methylester GGTI-2417, increase levels of the cyclin-dependent kinase (Cdk) inhibitor p27Kip1 and induce breast tumor regression in vivo. In another aspect, GGTI-2417 inhibits the Cdk2-mediated phosphorylation of p27Kip1 at Thr187 and accumulates p27Kip1 in the nucleus.

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