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.
Andrew Thompson | EurekAlert!
Genetic Regulation of the Thymus Function Identified
23.08.2016 | Universität Basel
Sun protection for plants - Plant substances can protect plants against harmful UV radiation
22.08.2016 | Max-Planck-Institut für Molekulare Pflanzenphysiologie
Waveguides are widely used for filtering, confining, guiding, coupling or splitting beams of visible light. However, creating waveguides that could do the same for X-rays has posed tremendous challenges in fabrication, so they are still only in an early stage of development.
In the latest issue of Acta Crystallographica Section A: Foundations and Advances , Sarah Hoffmann-Urlaub and Tim Salditt report the fabrication and testing of...
Electrochemists at TU Graz have managed to use monocrystalline semiconductor silicon as an active storage electrode in lithium batteries. This enables an integrated power supply to be made for microchips with a rechargeable battery.
Small electrical gadgets, such as mobile phones, tablets or notebooks, are indispensable accompaniments of everyday life. Integrated circuits in the interiors...
Recent findings indicating the possible discovery of a previously unknown subatomic particle may be evidence of a fifth fundamental force of nature, according...
A nanocrystalline material that rapidly makes white light out of blue light has been developed by KAUST researchers.
Malignant cancer cells not only proliferate faster than most body cells. They are also more dependent on the most important cellular garbage disposal unit, the proteasome, which degrades defective proteins. Therapies for some types of cancer exploit this dependence: Patients are treated with inhibitors, which block the proteasome. The ensuing pile-up of junk overwhelms the cancer cell, ultimately killing it. Scientists have now succeeded in determining the human proteasome’s 3D structure in unprecedented detail and have deciphered the mechanism by which inhibitors block the proteasome. Their results will pave the way to develop more effective proteasome inhibitors for cancer therapy.
In order to understand how cellular machines such as the proteasome work, it is essential to determine their three-dimensional structure in detail. With its...
12.08.2016 | Event News
02.08.2016 | Event News
29.07.2016 | Event News
23.08.2016 | Information Technology
23.08.2016 | Life Sciences
23.08.2016 | Earth Sciences