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Unnatural amino acids, utilized as building blocks, conformational constraints, molecular scaffolds or pharmacologically active products, represent a nearly infinite array of diverse structural elements for the development of new leads in peptidic and non-peptidic compounds. Small-molecule combinatorial libraries containing unnatural amino acid residues already have shown remarkable impact on drug discovery processes. Novel, short-chain peptide ligand mimetics with both enhanced biological activity and proteolytic resistance are drug candidates in today’s pharmaceutical pipelines. Optimized and fine-tuned analogues of peptidic substrates, inhibitors or effectors are also excellent analytical tools for investigating signal transduction pathways or gene regulation. Our fast-growing, innovative line of unnatural amino acids includes:
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