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Full-Text Articles in Physical Sciences and Mathematics
Development And Optimization Of Kinetic Target-Guided Synthesis Approaches Targeting Protein-Protein Interactions Of The Bcl-2 Family, Sameer Shamrao Kulkarni
Development And Optimization Of Kinetic Target-Guided Synthesis Approaches Targeting Protein-Protein Interactions Of The Bcl-2 Family, Sameer Shamrao Kulkarni
USF Tampa Graduate Theses and Dissertations
Kinetic target-guided synthesis (TGS) and in situ click chemistry are among unconventional discovery strategies having the potential to streamline the development of protein-protein interaction modulators (PPIMs). In kinetic TGS and in situ click chemistry, the target is directly involved in the assembly of its own potent, bidentate ligand from a pool of reactive fragments. Herein, we report the use and validation of kinetic TGS based on the sulfo-click reaction between thio acids and sulfonyl azides as a screening and synthesis platform for the identification of high-quality PPIMs. Starting from a randomly designed library consisting of nine thio acids and nine …