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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-3Œ-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.
For the full report by Liu et al. in Cancer Biology & Therapy, visit the following link: https://www.landesbioscience.com/journals/cbt/article/26721/relevant and high-impact original research with a special focus on the
Published by Landes Bioscience since 2002, Cancer Biology & Therapy publishes molecular basis of cancer, including articles with translational relevance to diagnosis or therapy. Established in 2002, Landes Bioscience is an Austin, Texas-based publisher of biology research journals and books.
