Cancer Cells Stopped, Nerve Cells Regenerated...New Drug
http://www.medicalnewstoday.com/releases/246931.php
Cancer Cells Stopped, Nerve Cells Regenerated By New Candidate Drug
Comments
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Very interesting and very challenging. That's why we do not have targetted therapy for TNBC yet. Well scientists are doing their job, FDA is doing their job. Personally I'd be happier if the drug leaves neuron cells alone too, then it's more likely to be safer."Despite this knowledge, past efforts to develop an effective small-molecule inhibitor for RhoA have failed, explained Zheng, who has studied Rho GTPases for over two decades. Most roadblocks stem from a lack of specificity in how researchers have been able to target RhoA, a resulting lack of efficiency in affecting molecular processes, problems with toxicity, and the inability to find a workable drug design.
For the current study, Zheng and his colleagues started with the extensive body of research from Cincinnati Children's and other institutions describing the processes and functions of Rho GTPases. They then used high-throughput computerized molecular screening and computerized drug design to reveal a druggable target site. This also provided a preliminary virtual simulation on the potential effectiveness of candidate drugs.
A key challenge to binding a small-molecule inhibitor to RhoA is the protein's globular structure and lack of surface pocket areas suitable for easy binding, Zheng said. The unique chemical structure of the lead compound identified by researchers, Rhosin, allows it to effectively bind to two shallow surface grooves on RhoA. This enables the candidate drug to take root and begin affecting cells. The two-legged configuration of Rosin also describes a useful drug design strategy for more effectively targeting difficult molecular sites like RhoA. "
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I found this article off to the right or cp418's original post. Seems to be slight headway into therapies every day.
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