作者: Serge Zaretsky , Andrei K. Yudin
DOI: 10.1016/J.DDTEC.2017.11.004
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摘要: Constrained peptides pose tremendous value in drug discovery. For example, owing to their large surface areas, they offer novel ways at inhibiting protein-protein interactions. As this field has grown, it become desirable introduce non-peptidic functionality into these rings enable differentiated structure activity relationships and improved pharmacokinetic properties. Recent advances the synthesis of cyclic pseudopeptides include macrocyclization through cysteine alkylation, multicomponent reactions, decarboxylative couplings, stapling chemistry.