Synthesis, screening and crystallization of small molecules targeting protein-protein interactions

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The aim of this project section is the synthesis, screening, and optimization of small organic compounds suitable for pharmacological interference with protein-protein interactions. Biologically active compounds will then be crystallized with their target proteins for structure determination of the corresponding protein-ligand complex. For this purpose, chemically synthesized and commercially available small-molecule compound libraries are provided, assay methodologies are developed, and the appropriate infrastructure for high-throughput screening is made available. Certain of the projects proposed herein will require the design and synthesis of focussed libraries. Bioassays suitable for high-throughput screening (HTS) are developed in collaboration with individual research groups. Primary hits are further evaluated in secondary assays and crystallization screens. Three-dimensional structures will guide the synthetic optimization of compounds that serve äs improved tools for the functional investigation of proteins.