整合素
肽
化学
结构-活动关系
生物化学
立体化学
计算生物学
细胞生物学
生物物理学
生物
受体
体外
作者
Rossella De Marco,Alessandra Tolomelli,Eusebio Juaristi,Luca Gentilucci
摘要
Integrins are cell surface receptors for proteins of the extracellular matrix and plasma-borne adhesive proteins. Their involvement in diverse pathologies prompted medicinal chemists to develop small-molecule antagonists, and very often such molecules are peptidomimetics designed on the basis of the short native ligand-integrin recognition motifs. This review deals with peptidomimetic integrin ligands composed of α- and β-amino acids. The roles exerted by the β-amino acid components are discussed in terms of biological activity, bioavailability, and selectivity. Special attention is paid to the synthetic accessibility and efficiency of conformationally constrained heterocyclic scaffolds incorporating α/β-amino acid span.
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