Systematic Exploration of Passive Permeability in Tetrapeptides with Hydrogen-Bond-Accepting Amino Acid Side Chains,ChemMedChem

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Systematic Exploration of Passive Permeability in Tetrapeptides with Hydrogen-Bond-Accepting Amino Acid Side Chains
ChemMedChem ( IF 3.6 ) Pub Date : 2022-06-13 , DOI: 10.1002/cmdc.202200204
Hiroki Shimizu _{1,

2} , Adam R Renslo ₁

Affiliation

Peptide breakthrough: Here we explore the passive artificial membrane permeability of 37 synthetic tetrapeptides bearing one or two unnatural amino acids bearing hydrogen bond acceptor (HBA) atoms for possible intramolecular H-bond formation. Permeability values spanning three orders of magnitude provide an empirical dataset of potential interest to medicinal and computational chemists studying the membrane permeability of peptides.

中文翻译：

具有氢键接受氨基酸侧链的四肽被动渗透性的系统探索

肽突破：在这里，我们探索了 37 种合成四肽的被动人工膜渗透性，这些四肽带有一个或两个带有氢键受体 (HBA) 原子的非天然氨基酸，用于可能的分子内氢键形成。跨越三个数量级的渗透率值为研究肽膜渗透性的药物和计算化学家提供了一个可能感兴趣的经验数据集。

更新日期：2022-06-13

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