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Development of a novel dual JAK/Src kinase inhibitor

Date:
January 6, 2014
Source:
Landes Bioscience
Summary:
Inhibitors of both JAK and Src kinases represent promising targets for cancer therapeutics because of the central importance of these kinases in tumor cell proliferation and survival. This research article describes MLS-2384 which is a synthetic derivative of amarine natural product, 6-bromoindirubin-3-oxime.

Inhibitors of both JAK and Src kinases represent promising targets for cancer therapeutics because of the central importance of these kinases in tumor cell proliferation and survival. Furthermore, in cancer cells activation of JAK has been reported as a compensatory effect in response to Src inhibitor exposure. This implies simultaneous inhibition of both kinases could have a synergy of anti-cancer effects compared to an agent that inhibits one or the other kinases.

The research article by Liu et al describes MLS-2384 which is a synthetic derivative of amarine natural product, 6-bromoindirubin-3′-oxime. MLS-2384 exhibits a dual JAK/Src kinase inhibitory activity, blocks downstream signaling into the STAT3 pathway, and has anti-cancer activity in various human cancer cell lines. These findings have important clinical implications for understanding the mechanisms of action of bromoindirubin derivatives.

The findings also indicate that this new 6-bromoindirubin derivative, MLS-2384, has potential as an anti-tumor therapeutic agent targeting JAK and Src kinases upstream of STAT3 in a wide variety of human cancer cells.


Story Source:

The above story is based on materials provided by Landes Bioscience. Note: Materials may be edited for content and length.


Journal Reference:

  1. Lucy Liu, Nicolas Gaboriaud, Konstantina Vougogianopoulou, Yan Tian, Jun Wu, Wei Wen, Alexios-Leandros Skaltsounis, Richard Jove. MLS-2384, a new 6-bromoindirubin derivative with dual JAK/Src kinase inhibitory activity, suppresses growth of diverse cancer cells. Cancer Biology & Therapy, 2014; 15 (2) DOI: 10.4161/cbt.26721

Cite This Page:

Landes Bioscience. "Development of a novel dual JAK/Src kinase inhibitor." ScienceDaily. ScienceDaily, 6 January 2014. <www.sciencedaily.com/releases/2014/01/140106160123.htm>.
Landes Bioscience. (2014, January 6). Development of a novel dual JAK/Src kinase inhibitor. ScienceDaily. Retrieved September 18, 2014 from www.sciencedaily.com/releases/2014/01/140106160123.htm
Landes Bioscience. "Development of a novel dual JAK/Src kinase inhibitor." ScienceDaily. www.sciencedaily.com/releases/2014/01/140106160123.htm (accessed September 18, 2014).

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