COVALENT PROTEIN MAPPING FRAGMENT LIBRARY
concept published FBLD 2012
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In Vitro Chemistry
The acrylamide functional group has a mild reactivity and selectivity in Michael reactions. The partner can be another small molecule or a protein with appropriate free functional groups (e.g.nucleophiles). InFarmatik's experience in acrylamide library construction resulted a fragment library, which could be used in NOE protein interaction studies or self-assembly systems
Covalent Protein Mapping & Labeling
concept published PF 2011, based upon acrylamide chemistry Shokat et al publised the their work on development selective inhibitor against G12C mutant K-Ras. InFarmatik, Inc.perpared simiar fragment based approach of targeting Cystein mutant enzymes for InhiBillion project.
Selective Michael reaction of acryl amides allows invitro chemistry in the presence of enzymes. The sterical enforcement drives combinatorial reactions of mixtures toward synthesis of selective inhibitors of the targeted ezymes by completenig reactants for a perfect pocket fill.
Target Guided Synthesis
A complete technonlogy based upon click reactions. Manetsch at all developed the techninque of the self-assembly systems using easy massspec detection.
INFARMATIK,INC. is to intruduce new technology scope in covalent fragment screening. In collaboration with EvoBlocks, new series of covalent fragments and new covalent fragment types will be introduced in Q4.