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作为血管生成抑制剂的 probestin 的固相合成及生物学评价。

Solid phase synthesis and biological evaluation of probestin as an angiogenesis inhibitor.

机构信息

Department of Pharmaceutical Sciences, College of Pharmacy, The University of Oklahoma Health Sciences Center, 1110 N. Stonewall Avenue, Room 301, Oklahoma City, OK 73117, USA.

出版信息

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3561-4. doi: 10.1016/j.bmcl.2013.04.031. Epub 2013 Apr 23.

Abstract

Probestin is a potent aminopeptidase N (APN) inhibitor originally isolated from the bacterial culture broth. Here, we report probestin synthesis by solid phase peptide synthesis (SPPS) method and evaluated its activity to inhibit angiogenesis using a chicken embryo chorioallantoic membrane (CAM) assay and a CAM tumor xenograft model. Results from these studies demonstrate that probestin inhibits the angiogenic activity and tumor growth.

摘要

Probestin 是一种从细菌培养液中分离得到的强效氨肽酶 N(APN)抑制剂。本文采用固相多肽合成(SPPS)法合成了 Probestin,并通过鸡胚尿囊膜(CAM)试验和 CAM 肿瘤异种移植模型评价其抑制血管生成的活性。这些研究结果表明,Probestin 可抑制血管生成活性和肿瘤生长。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f817/7172075/694156d03193/fx1.jpg

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