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作为氨肽酶抑制剂的 bestatin 类似物的开发进展。

Progress in the development of bestatin analogues as aminopeptidases inhibitors.

机构信息

Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong 250012, China.

出版信息

Curr Med Chem. 2011;18(7):964-76. doi: 10.2174/092986711794940879.

DOI:10.2174/092986711794940879
PMID:21254977
Abstract

Aminopeptidases play essential roles in protein maturation, activation, and stability as well as in the degradation and regulation of hormonal and nonhormonal peptides that can serve as important enzyme targets for drug design. This review will focus on an effective inhibitor of aminopeptidases, bestatin, including work to find better inhibitors in the past three decades that has sought to optimize bestatin and prospective developments in bestatin optimization in the future.

摘要

氨肽酶在蛋白质成熟、激活和稳定性以及激素和非激素肽的降解和调节中发挥着重要作用,这些肽可以作为药物设计的重要酶靶标。这篇综述将集中讨论氨肽酶的一种有效抑制剂——亮抑酶肽,包括过去三十年寻找更好抑制剂的工作,旨在优化亮抑酶肽,并对未来亮抑酶肽的优化进行展望。

相似文献

1
Progress in the development of bestatin analogues as aminopeptidases inhibitors.作为氨肽酶抑制剂的 bestatin 类似物的开发进展。
Curr Med Chem. 2011;18(7):964-76. doi: 10.2174/092986711794940879.
2
Synthesis of sulfur-containing analogues of bestatin. Inhibition of aminopeptidases by alpha-thiolbestatin analogues.贝他定含硫类似物的合成。α-硫醇贝他定类似物对氨肽酶的抑制作用。
J Med Chem. 1988 Nov;31(11):2193-9. doi: 10.1021/jm00119a022.
3
alpha-Keto amide inhibitors of aminopeptidases.
J Med Chem. 1992 Feb 7;35(3):451-6. doi: 10.1021/jm00081a005.
4
Bestatin-based chemical biology strategy reveals distinct roles for malaria M1- and M17-family aminopeptidases.基于贝司他汀的化学生物学策略揭示了疟原虫 M1-和 M17-家族氨肽酶的不同作用。
Proc Natl Acad Sci U S A. 2011 Aug 23;108(34):E526-34. doi: 10.1073/pnas.1105601108. Epub 2011 Aug 15.
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Bestatin as an experimental tool in mammals.贝司他汀作为哺乳动物的一种实验工具。
Curr Drug Metab. 2001 Mar;2(1):67-85. doi: 10.2174/1389200013338748.
6
Hypoalgesic action of bestatin analogues that inhibit central aminopeptidases, but not neutral endopeptidase.抑制中枢氨肽酶而非中性内肽酶的贝司他汀类似物的镇痛作用。
Neuropeptides. 1993 Sep;25(3):175-82. doi: 10.1016/0143-4179(93)90100-o.
7
Augmentation of death ligand-induced apoptosis by aminopeptidase inhibitors in human solid tumor cell lines.氨肽酶抑制剂增强死亡配体诱导的人实体瘤细胞系凋亡
Int J Cancer. 2001 Nov;94(4):485-91. doi: 10.1002/ijc.1492.
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Inhibition of tumor invasion and extracellular matrix degradation by ubenimex (bestatin).乌苯美司(抑氨肽酶B)对肿瘤侵袭和细胞外基质降解的抑制作用
Clin Exp Metastasis. 1992 Jan;10(1):49-59. doi: 10.1007/BF00163576.
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Aminopeptidase inhibitors bestatin and actinonin inhibit cell proliferation of myeloma cells predominantly by intracellular interactions.氨肽酶抑制剂抑氨肽酶素和放线菌素主要通过细胞内相互作用抑制骨髓瘤细胞的增殖。
Cancer Lett. 2002 Aug 28;182(2):113-9. doi: 10.1016/s0304-3835(02)00086-1.
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In vivo actions of bestatin-related compounds in relation to their actions in vitro.
Biochem Int. 1984 Nov;9(5):643-50.

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