Wed, 19 Feb 2020, 16:00 CET (Berlin)

Dr. Alwin Hartman, Principal Scientist at BioSolveIT, St. Augustin, Germany

New applications of dynamic combinatorial chemistry to medicinal chemistry

Applying dynamic combinatorial chemistry (DCC) to medicinal chemistry projects can be a helpful strategy for finding starting points in the drug-discovery process. Especially, when DCC is combined with structure-based or fragment-based drug design approaches, potent compounds can be obtained.

As relevant drug target, 14-3-3 proteins play a role in several diseases and many biological processes. Proteins of this family engage in protein-protein interactions (PPIs), and can do so with numerous different binding partners. By forming these PPIs, these proteins regulate their binding partner’s activity. The activity can be both up- or down-regulated. Finding modulators of PPIs is very challenging via traditional screening approaches.

In this webinar we will briefly introduce DCC, followed by the first application of DCC to a PPI, where we found small-molecule modulators of the PPI of 14-3-3/ synaptopodin. These hit compounds were then evaluated for their biochemical properties via surface plasmon resonance (SPR) and fluorescence polarization (FP) assay.

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