INHIBILLION project

INFARMATIK, INC. realized in 2010 that cetain functional groups can selectively react with Cystein SH group in suboptimal conditions, if the components reach an appropriate distance stipulated by secondary binding forces. Acryl amides proved to be especially good reaction partners in this coordination assisted  Michael reactions toward SH group, due to optimal reactivity of the acryl amide beta carbon atom. This optimal reactivity means that the carbon is fairly unreactive to SH in pH 7 medium, if no directive secondary forces assist the reaction. Besides, in reactivity studies, InFarmatik Inc. showed that the same beta carbon showed also lo affinity to other nucleophyles, such as NH and OH. 

 

After completing this preliminary study InFarmatik was the first company started to build an acryl amide fragment libary for covalent protein mapping (CPM). Based upon this synthetic experience InFarmatik, elaborated projects with its Hungarian academic and industrial partners based upon selective covalent binding mostly on the area of cancer research. 

 

In 2013 Shokat et al published a succesful application of the covalent binding method for a Cys mutated K-Ras project. Based upon this succesful applicaton of the covalent binding fragment technology, InFarmatik, Inc decided to use some of its in-house resources to finance esearch projects on oncology field. 

 

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