Submonomer synthesis of azapeptide ligands of the Insulin Receptor Tyrosine Kinase domain

KurianL.A.; SilvaT.A.; SabatinoD.

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Submonomer synthesis of azapeptide ligands of the Insulin Receptor Tyrosine Kinase domain

机译：胰岛素受体酪氨酸激酶结构域的氮杂肽配体的亚单体合成

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Azapeptide ligands of the Insulin Receptor Tyrosine Kinase (IRTK) were developed by solid-phase submonomer azapeptide synthesis in sufficient isolated yields (36-55%) and purities 95% for structure-activity relationship studies. The azapeptides adopted folded geometries with some proportion of random coil according to CD and NMR spectroscopy. In vitro phosphorylation of the IRTK domain in the presence of azapeptides produced a lead inhibitor, Ac-DIazaYET-NH2 (～50% at 400 μM) whereas the [aza-DOPA 3] and [aza-Glu4] analogs were found to stimulate IRTK phosphorylations. Thus, azapeptide ligands of the IRTK provide important modulatory activity of this important class of enzymes for anti-cancer and related applications in drug discovery.

机译：胰岛素受体酪氨酸激酶（IRTK）的氮杂肽配体是通过固相亚单体氮杂肽合成而开发的，具有足够的分离收率（36-55％），纯度> 95％，用于结构-活性关系研究。根据CD和NMR光谱，氮杂肽采用折叠的几何形状并具有一定比例的无规卷曲。在存在氮杂肽的情况下，IRTK结构域的体外磷酸化产生了铅抑制剂Ac-DIazaYET-NH2（在400μM时约为50％），而发现[aza-DOPA 3]和[aza-Glu4]类似物可以刺激IRTK。磷酸化。因此，IRTK的氮杂肽配体为药物开发中的抗癌和相关应用提供了这一重要酶类的重要调节活性。

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《Bioorganic and Medicinal Chemistry Letters》 |2014年第17期|共5页
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KurianL.A.; SilvaT.A.; SabatinoD.;
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正文语种 eng
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Azapeptide; Insulin Receptor Tyrosine Kinase; IRTK inhibition; Peptidomimetics;

机译：阿扎肽;胰岛素受体酪氨酸激酶;IRTK抑制;拟肽;

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1. Submonomer synthesis of azapeptide ligands of the Insulin Receptor Tyrosine Kinase domain [J] . KurianL.A., SilvaT.A., SabatinoD. Bioorganic and Medicinal Chemistry Letters . 2014,第17期

机译：胰岛素受体酪氨酸激酶结构域的氮杂肽配体的亚单体合成
2. Comparative modeling of the phosphatase and kinase domains of protein tyrosine phosphatase and insulin receptor kinase from Drosophila melanogaster (DPTP61fm), and a computational study of their mutual interactions [J] . Hati S, Bhattacharyya S, Price JV, Biochemistry and Cell Biology . 2002,第2期

机译：果蝇蛋白酪氨酸磷酸酶和胰岛素受体激酶的磷酸酶和激酶结构域的比较模型，以及它们相互相互作用的计算研究
3. The insulin receptor tyrosine kinase domain in a chimaeric epidermal growth factor-insulin receptor generates Ca2+ signals through the PLC-gamma1 pathway. [J] . Telting D, Willems PH, van der Zon GC, Biochimica et biophysica acta: international journal of biochemistry and biophysics . 1999,第2期

机译：嵌合表皮生长因子胰岛素受体中的胰岛素受体酪氨酸激酶结构域通过PLC-gamma1途径产生Ca2 +信号。
4. Function of the Membrane-Bound Isoform Ligands of the Receptor Tyrosine Kinase Subclass III in Inducing Inducing Self-Renewal of Early Hematopoietic Progenitor Cells [C] . Jutta Friel, Christoph Heberlein, Maren Geldmacher, NATO Advanced Research Workshop on Stem Cells and their Potential for Clinical Application . 2008

机译：受体酪氨酸激酶亚类III膜结合同种型配体的作用在诱导早期造血祖细胞的诱导自我更新中
5. Single chain antibody targeting of the ligand binding domain of the tyrosine kinase receptor anaplastic lymphoma kinase. [D] . Stylianou, Dora C. 2006

机译：单链抗体靶向酪氨酸激酶受体间变性淋巴瘤激酶的配体结合结构域。
6. In situ autoradiography and ligand-dependent tyrosine kinase activity reveal insulin receptors and insulin-like growth factor I receptors in prepancreatic chicken embryos. [O] . M Girbau, L Bassas, J Alemany, 1989

机译：原位放射自显影和依赖配体的酪氨酸激酶活性揭示了胰腺前鸡胚中的胰岛素受体和胰岛素样生长因子I受体。
7. Tyrosine Kinase Activity of a Chimeric Insulin-Like-Growth-Factor-l Receptor Containing the Insulin Receptor C-Terminal Domain. Comparison with the Tyrosine Kinase Activities of the Insulin and Msulin-Like-Growth-Factor-1 Receptors Using a Cell-Free System [O] . Isabelle Mothe, Sophie Tartare, Aline Kowalski-Chauvel, 1995

机译：含有胰岛素受体C-末端结构域的嵌合胰岛素样生长因子-1受体的酪氨酸激酶活性。使用无细胞系统比较胰岛素和Msulin样生长因子-1受体的酪氨酸激酶活性

Submonomer synthesis of azapeptide ligands of the Insulin Receptor Tyrosine Kinase domain

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