The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors.

Rosner KE; Guo Z; Orth

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The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors.

机译：基于酒石酸盐的新型TNF-α转化酶（TACE）抑制剂的发现。

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A novel series of TNF-alpha convertase (TACE) inhibitors which are non-hydroxamate have been discovered. These compounds are bis-amides of L-tartaric acid (tartrate) and coordinate to the active site zinc in a tridentate manner. They are selective for TACE over other MMP's. We report the first X-ray crystal structure for a tartrate-based TACE inhibitor.

机译：已经发现了非异羟肟酸酯的一系列新的TNF-α转化酶（TACE）抑制剂。这些化合物是L-酒石酸（酒石酸盐）的双酰胺，并以三齿方式与活性位点锌配位。与其他MMP相比，它们对TACE具有选择性。我们报告了基于酒石酸盐的TACE抑制剂的第一个X射线晶体结构。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第3期|共5页
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Rosner KE; Guo Z; Orth;
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1. The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors. [J] . Rosner KE, Guo Z, Orth Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：基于酒石酸盐的新型TNF-α转化酶（TACE）抑制剂的发现。
2. Synthesis and activity of tryptophan sulfonamide derivatives as novel non-hydroxamate TNF-alpha converting enzyme (TACE) inhibitors. [J] . Park K, Gopalsamy A, Aplasca A Bioorganic and medicinal chemistry . 2009,第11期

机译：色氨酸磺酰胺衍生物作为新型非异羟肟酸酯TNF-α转化酶（TACE）抑制剂的合成和活性。
3. Synthesis and biological activity of selective pipecolic acid-based TNF-alpha converting enzyme (TACE) inhibitors. [J] . Letavic MA, Axt MZ, Barberia JT, Bioorganic and Medicinal Chemistry Letters . 2002,第10期

机译：选择性基于胡椒酸的TNF-α转化酶（TACE）抑制剂的合成和生物学活性。
4. Synthesis of the first highly potent inhibitor of the three vasopeptidases:endothelin converting enzyme (ECE),angiotensin converting enzyme (ACE) and neprilysin (NEP) [C] . Nicolas Inguimbert, Herve Poras, Pascale Coric, European Peptide Symposium . 2002

机译：三种血管肽酶的第一高效抑制剂的合成：内皮素转化酶（ECE），血管紧张素转化酶（ACE）和Neplysin（NEP）
5. Role of oligopeptide transporters rat PEPT1 and PEPT2 in the transport of angiotensin converting enzyme inhibitors. [D] . Zhu, Tong. 2000

机译：寡肽转运蛋白大鼠PEPT1和PEPT2在血管紧张素转化酶抑制剂的转运中的作用。
6. Strain-induced Differentiation of Fetal Type II Epithelial Cells Is Mediated via the Integrin α6β1-ADAM17/Tumor Necrosis Factor-α-converting Enzyme (TACE) Signaling Pathway [O] . Yulian Wang, Zheping Huang, Pritha S. Nayak, 2013

机译：整合素α6β1-ADAM17/肿瘤坏死因子-α转化酶（TACE）信号传导通路介导胎儿II型上皮细胞的应变诱导分化。
7. Stabilization of the autoproteolysis of TNF-alpha converting enzyme (TACE) results in a novel crystal form suitable for structure-based drug design studies [O] . Richard N. Ingram, Peter Orth, Corey L. Strickland, 2006

机译：TNF-α转换酶（TACE）的自蛋白酶稳定化导致一种适用于基于结构的药物设计研究的新型晶体形式
8. Soluble Dextran Complexes of Kallikrein, Bradykinin and Enzyme Inhibitors. [R] . Odya, C. E., Levin, Y., Erdoes, E. G., 1977

机译：激肽释放酶，缓激肽和酶抑制剂的可溶性葡聚糖复合物。

The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors.

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