0424 GMT February 29, 2020
The effect of this class of inhibitors 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. As a result, there is an acute need for strategies to restrict the effect of these highly promising new drugs more selectively to the malignant tumor, medical.wesrch.com wrote.
The aim of the research which was conducted by University of Vienna was to develop an improved tyrosine kinase inhibitor that is actually inactive and which is only activated selectively in the malignant tissue.
This is intended to prevent damage to healthy tissue and therefore minimise side effects for patients. As part of the paper published in the journal Angewandte Chemie [Applied Chemistry], International Edition, a new inhibitor has been successfully synthesised and coordinated to cobalt(III). This leads to initial drug inactivation and, thus, no activity under normal physiological conditions. Only in tumour tissue where, due to the rapid growth, unusually low-oxygen conditions 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.