Chemoprevention of colorectal cancer by targeting Janus kinase 3 with a rationally designed small molecule inhibitor.

Abstract

The effects of the rationally designed JAK3 inhibitor JANEX-1 on the development of intestinal tumors in the APC(min) mouse model of familial adenomatous polyposis were examined. At a non-toxic dose level, >4 times lower than its day 30 LD(10), JANEX-1 was highly effective in preventing intestinal tumor development in Min mice, resulting in markedly improved survival outcomes. JAK3 inhibitors may, therefore, be useful in the chemoprevention of colorectal cancer. Here, an overview regarding the potential of JANEX-1 as a chemopreventive agent is provided.

• Authors: Fatih M Uckun, Ilker Dibirdik
• Journal: Nutrition and cancer (Nutr Cancer) Vol. 62 Issue 7 Pg. 968-72 ( 2010) ISSN: 1532-7914 [Electronic] United States
• PMID: 20924972 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Anticarcinogenic Agents
• Protein Kinase Inhibitors
• Quinazolines
• WHI P131
• Janus Kinase 3

Topics

• Animals
• Anticarcinogenic Agents (pharmacology)
• Colorectal Neoplasms (prevention & control)
• Janus Kinase 3 (antagonists & inhibitors)
• Mice
• Mice, Inbred C57BL
• Protein Kinase Inhibitors (pharmacology)
• Quinazolines (pharmacokinetics, pharmacology)