Kinases
Kinases are major targets for many drugs, including many anti-cancer therapies. They play a very important role in cellular biology, and many diseases are affected by them in some way. The various categories of kinase and their relation to diseases have been compiled by researchers. The molecular basis of their role in diseases is known for quite a few of them, and continues to grow; this knowledge is sometimes referred to as the Kinome.
At OriBase Pharma, we have built an excellent expertise in designing and optimizing novel kinase inhibitors. Our expertise comes from the understanding of the various mechanisms of potential inhibitors and their binding to the kinase. All this knowledge is compiled within our in silico drug design and medicinal chemistry platforms when all the activity states of kinases are represented (DFG-in, DFG-out, and intermediate states). Most small-molecule kinase inhibitors are ATP competitive, which render them more likely to cross-inhibit other kinases in the same family or even kinases from other families. Assessing compound selectivity is therefore critical for drug development.
Thanks to our Selective Lead service coupled with organic chemistry, we are tackling the selectivity issue as early as possible in our medicinal chemistry design of kinase inhibitors. Any kinase inhibitor design process at OriBase Pharma integrates the kinase of interest and also all the related homologous kinases to prioritize only those molecules showing the right inhibition profile for chemistry synthesis.