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Novel Tyrosine Kinase Inhibitors Reduce Side Effects in Cancer Therapy

Author: Zhang Qing
by Zhang Qing
Posted: Oct 12, 2014

A recently published research reports that investigators have developed a novel strategy for reducing the often serious side effects of an important class of modern anticancer drugs -- tyrosine kinase inhibitors. The novel drug is supposed to restrict its activity with high selectivity to the malignant tumor.

Severe side effect is one of biggest problems in modern cancer therapy, and ultimately leads to treatment having to be stopped. Targeted cancer drug is based on the specific inhibition of proteins that are over-activated in cancer cells and which drive abnormal cell growth. However, clinical practice has shown that, as a result of the physiological functions of these proteins in healthy tissue, their inhibition can cause severe side effects.

Facing such challenge, scientists have been successfully synthesized a new inhibitor that is coordinated to cobalt(III). This leads to initial drug inactivation and, thus, no activity under normal physiological conditions. Only in tumour tissue where low-oxygen conditions unusually prevail, the inactive cobalt(III) compound is reduced to cobalt(II) and as a result releases the active drug. The tumour-selective effectiveness of this approach has been demonstrated both in living cells and in tumor-bearing organisms.

So far, there has been no comparable strategy for reducing the (severe) side effects of tyrosine kinase inhibitors. As a result, there is hope that, in future, the approach presented here will improve the tolerance of the therapy and allow this treatment to benefit patients who have previously had to discontinue it.

To date, there are no approved targeted therapies for malignant small cell lung cancer (SCLC), due to no treatment advances in 30 years. However, Two novel researches lay the foundation for future research and have the potential to advance treatments for this highly malignant cancer.

A study, entitled with "RET Mutation and Expression in Small Cell Lung Cancer," was published in the journal Thoracic Oncology and found a new mutation in SCLC which may play a role in the disease development. The researchers found that the genetic mutation, called RET (rearranged during transfection), was linked to rapid cell growth.

The other study, published in Plos One, outlines a novel approach to identify new drug therapies for SCLC based on tumors' genomic profiles. The research team discovered new molecular targets for treating the disease by extracting data from SCLC tumors to examine drug sensitivity. Through this analysis, they outlined a promising new approach to predict which cancer-fighting drugs would be the most broadly effective at slowing tumor growth.

The two studies enabled us to identify which molecules are implicated in driver mutation and which drugs may be the most useful in which types of tumors. Small cell lung cancer is one of the fastest growing cancers and these studies have yielded small but important therapeutic insights into this disease.

About the Author

Numerologist Warda is hooked on OG-L002 fishing, collecting. And lastly her encouragement comes from socializing along with her companions.

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Author: Zhang Qing

Zhang Qing

Member since: Oct 29, 2013
Published articles: 172

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