C-terminal constrained phenylalanine as a pharmacophoric unit in peptide-based proteasome inhibitors.

Baldisserotto A; Marastoni M; Lazzari I; Trapella C; Gavioli R; Tomatis R

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C-terminal constrained phenylalanine as a pharmacophoric unit in peptide-based proteasome inhibitors.

机译：C末端约束苯丙氨酸作为基于肽的蛋白酶体抑制剂中的药效学单元。

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Here we report the synthesis and biological properties of peptide-based molecules bearing constrained analogues of phenylalanine at the C-terminal. Compounds were tested as proteasome subunits' inhibitors. Dehydro-peptides showed good inhibition, in particular against trypsin-like (T-L) proteasome activity while some C-terminal Tic-derivatives inhibit only caspase-like activity in enzymatic beta1 subunits with a certain degree of efficacy. The best analogues of the series demonstrated good resistance to proteolysis and a capacity to permeate the cell membrane.

机译：在这里，我们报告了在C端带有受约束的苯丙氨酸类似物的肽基分子的合成和生物学特性。测试化合物作为蛋白酶体亚基的抑制剂。脱氢肽显示出良好的抑制作用，尤其是对胰蛋白酶样（T-L）蛋白酶体活性的抑制作用，而某些C末端Tic衍生物仅在酶促β1亚基中抑制胱天蛋白酶样活性，具有一定的功效。该系列中最好的类似物表现出良好的抗蛋白水解性和渗透细胞膜的能力。

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来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2008年第7期|共9页
作者
Baldisserotto A; Marastoni M; Lazzari I; Trapella C; Gavioli R; Tomatis R;
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正文语种 eng
中图分类医药、卫生;劳动卫生;
关键词
Carbon ion; multicatalytic endopeptidase complex; Peptides; inhibitors; Phenylalanine; 肽类; 苯丙氨酸;

机译：碳离子;多催化内肽酶复合物;肽;抑制剂;苯丙氨酸;肽类;苯丙氨酸;

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专利

1. C-terminal constrained phenylalanine as a pharmacophoric unit in peptide-based proteasome inhibitors. [J] . Baldisserotto A, Marastoni M, Lazzari I, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2008,第7期

机译：C末端约束苯丙氨酸作为基于肽的蛋白酶体抑制剂中的药效学单元。
2. A C-terminal cysteine residue is required for peptide-based inhibition of the NGF/TrkA interaction at nM concentrations: implications for peptide-based analgesics [J] . Andrew J. Poole, Laura Frigotto, Matthew E. Smith, Scientific reports. . 2019,第1期

机译：C端半胱氨酸残基对于nM浓度下基于肽的NGF / TrkA相互作用的抑制是必需的：对基于肽的镇痛药的影响
3. Mucin 1 C-terminal subunit oncoprotein is a target for small-molecule inhibitors. [J] . Zhou Y, Rajabi H, Kufe D Molecular pharmacology. . 2011,第5期

机译：Mucin 1 C末端亚基癌蛋白是小分子抑制剂的靶标。
4. An Asymmetric Synthesis of (R)- and (5)-o-cyano-phenylalanine Leading to Chiral Constrained Phenylalanine Dipeptide Mimetics [C] . Karolien Van Rompaey, Isabelle Van den Eynde, Steven Ballet American Peptide Symposium . 2006

机译：（R） - 和（5）-O-氰基 - 苯丙氨酸的不对称合成，导致手性约束苯丙氨酸二肽模拟物
5. STAT3 activation by the ErbB2 receptor and development of peptide-based STAT3 inhibitors. [D] . Ren, Zhiyong. 2005

机译：ErbB2受体激活STAT3，并开发出基于肽的STAT3抑制剂。
6. Phosphorylation of the C-terminal tail of proteasome subunit α7 is required for binding of the proteasome quality control factor Ecm29 [O] . Prashant S. Wani, Anjana Suppahia, Xavier Capalla, -1

机译：蛋白酶体质量控制因子Ecm29的结合需要蛋白酶体亚基α7的C末端尾部磷酸化
7. Phosphorylation of the C-terminal tail of proteasome subunit ?7 is required for binding of the proteasome quality control factor Ecm29 [O] . Wani Prashant S., Suppahia Anjana, Capalla Xavier, 2016

机译：蛋白酶体质量控制因子Ecm29的结合需要蛋白酶体亚基α7的C末端尾部磷酸化。

C-terminal constrained phenylalanine as a pharmacophoric unit in peptide-based proteasome inhibitors.

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