Protein tyrosine phosphatases (PTPs) have been challenging targets for inhibitor design, because all PTPs share a highly conserved active site structure, which is positively charged and requires negatively charged moieties for tight binding. In this study, we developed cell-permeable bicyclic peptidyl inhibitors against T-cell PTP (TCPTP), which feature a cell-penetrating motif in one ring and a target-binding sequence in the second ring.

中文翻译：

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来自组合库的T细胞蛋白酪氨酸磷酸酶的细胞可渗透双环肽基抑制剂

蛋白质酪氨酸磷酸酶（PTP）一直是抑制剂设计的挑战性目标，因为所有PTP都具有高度保守的活性位点结构，该结构带正电且需要带负电的部分才能紧密结合。在这项研究中，我们开发了针对T细胞PTP（TCPTP）的细胞渗透性双环肽基抑制剂，其特征在于一个环中具有细胞穿透基序，而第二个环中具有靶标结合序列。