Selecting protein tyrosine phosphatases as drug targets.

van Huijsduijnen RH; Bombrun A; Swinnen D

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Selecting protein tyrosine phosphatases as drug targets.

机译：选择蛋白质酪氨酸磷酸酶作为药物靶标。

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Protein tyrosine phosphatases (PTPs) have emerged as a new and promising class of signaling targets, since the discovery of PTP1B as a major drug target for diabetes and obesity. Blocking individual PTPs results in the activation of specific tyrosine phosphorylation events, but matching PTPs with such pathways and therapeutic indications is a complex undertaking. The history of PTP1B shows that its unusual knockout phenotype and observations with generic and antisense inhibitors in vivo, but not its classical molecular biology, triggered the rapid development of inhibitors that are today being developed for the clinic.

机译：自从发现PTP1B作为糖尿病和肥胖症的主要药物靶标以来，蛋白质酪氨酸磷酸酶（PTPs）就已经成为一种新型的有希望的信号转导靶标。阻断单个PTP会导致特定酪氨酸磷酸化事件的激活，但是将PTP与此类途径和治疗适应症相匹配是一项复杂的工作。 PTP1B的历史表明，其不寻常的基因敲除表型以及在体内使用普通和反义抑制剂的观察结果，而不是其经典的分子生物学，触发了如今为临床开发的抑制剂的快速发展。

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《Drug discovery today》 |2002年第19期|共7页
作者
van Huijsduijnen RH; Bombrun A; Swinnen D;
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原文格式 PDF
正文语种 eng
中图分类药学;
关键词
Drug Delivery Systems; Protein-Tyrosine-Phosphatase; 药物投与系统; 蛋白质酪氨酸磷酸酶;

机译：Drug Delivery Systems;Protein-Tyrosine-Phosphatase;药物投与系统;蛋白质酪氨酸磷酸酶;

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1. Selecting protein tyrosine phosphatases as drug targets. [J] . van Huijsduijnen RH, Bombrun A, Swinnen D Drug discovery today . 2002,第19期

机译：选择蛋白质酪氨酸磷酸酶作为药物靶标。
2. Design and Synthesis of Imidazolidine-2,4-Dione Derivatives as Selective Inhibitors by Targeting Protein Tyrosine Phosphatase-1B Over T-Cell Protein Tyrosine Phosphatase [J] . Ying Ma, Su-Xia Sun, Xian-Chao Cheng, Chemical biology and drug design . 2013,第5期

机译：以T细胞蛋白酪氨酸磷酸酶为靶标的蛋白酪氨酸磷酸酶-1B设计和合成咪唑烷-2,4-二酮衍生物作为选择性抑制剂
3. Diphenylether derivative as selective inhibitor of protein tyrosine phosphatase 1B (PTP1B) over t-cell protein tyrosine phosphatase (TCPTP) identified through virtual screening. [J] . M V V V Sekhar Reddy, Chakshusmathi Ghadiyaram, Sunil Kumar Panigrahi, Mini reviews in medicinal chemistry . 2013,第11期

机译：通过虚拟筛选确定的二苯醚衍生物作为蛋白质酪氨酸磷酸酶1B（PTP1B）的选择性抑制剂，优于t细胞蛋白质酪氨酸磷酸酶（TCPTP）。
4. Actinodaphnine and Rutacridone as New T-Cell Protein Tyrosine Phosphatase Inhibitors for Drug Development of Obesity [C] . Y Fitrianingrum, D Indarto, R Kusumawati Annual Basic Science International Conference . 2019

机译：Actinodaphnine和Rutacridone作为新的T细胞蛋白酪氨酸磷酸酶抑制剂，用于肥胖的药物发育
5. Interaction of EphA2 with human cytoplasmic protein tyrosine phosphatase (HCPTP) variants and phosphorylation status of EphA2 in cancer cells by quantitative selected reaction monitoring mass spectrometry (SRM MS) [D] . Balasubramaniam, Deepa 2011

机译：EphA2与人胞浆蛋白酪氨酸磷酸酶（HCPTP）变体的相互作用以及癌细胞中EphA2的磷酸化状态的定量选择反应监测质谱（SRM MS）
6. Site-Selective Regulation of Platelet-Derived Growth Factor β Receptor Tyrosine Phosphorylation by T-Cell Protein Tyrosine Phosphatase [O] . Camilla Persson, Catrine Sävenhed, Annie Bourdeau, 2001

机译：T细胞蛋白酪氨酸磷酸酶对血小板衍生生长因子β受体酪氨酸磷酸化的位点选择性调节
7. Site-Selective Regulation of Platelet-Derived Growth Factor β Receptor Tyrosine Phosphorylation by T-Cell Protein Tyrosine Phosphatase [O] . Persson, Camilla, Sävenhed, Catrine, Bourdeau, Annie, 2004

机译：T细胞蛋白酪氨酸磷酸酶对血小板衍生生长因子β受体酪氨酸磷酸化的位点选择性调节

Selecting protein tyrosine phosphatases as drug targets.

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