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人类免疫缺陷病毒具有一种天冬氨酸型蛋白酶,它可被胃蛋白酶抑制剂A抑制。

Human immunodeficiency virus has an aspartic-type protease that can be inhibited by pepstatin A.

作者信息

Seelmeier S, Schmidt H, Turk V, von der Helm K

机构信息

Max von Pettenkofer Institute, University of Munich, Federal Republic of Germany.

出版信息

Proc Natl Acad Sci U S A. 1988 Sep;85(18):6612-6. doi: 10.1073/pnas.85.18.6612.

DOI:10.1073/pnas.85.18.6612
PMID:3045820
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC282027/
Abstract

The protease encoded by the human immunodeficiency virus (HIV) processes the viral gag and gag-pol protein precursor by posttranslational cleavage. In this study we have demonstrated by site-specific mutagenesis (Asp----Thr) and by pepstatin A inhibition that the recombinant HIV protease is an aspartic-type protease. Furthermore, incubation of HIV-infected H9 cells with pepstatin A inhibited part of the intracellular processing of the HIV gag protein yet had no apparent toxicity on HIV-infected cells during 48 hr of incubation.

摘要

人类免疫缺陷病毒(HIV)编码的蛋白酶通过翻译后切割处理病毒的gag和gag-pol蛋白前体。在本研究中,我们通过位点特异性诱变(天冬氨酸→苏氨酸)和胃蛋白酶抑制剂A抑制实验证明,重组HIV蛋白酶是一种天冬氨酸型蛋白酶。此外,用胃蛋白酶抑制剂A孵育HIV感染的H9细胞,可抑制HIV gag蛋白的部分细胞内加工过程,但在48小时的孵育期间对HIV感染的细胞没有明显毒性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a565/282027/671dcc39ffe7/pnas00297-0047-b.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a565/282027/d0710c787379/pnas00297-0045-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a565/282027/e403a662a6df/pnas00297-0045-b.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a565/282027/2eb2c5233dbb/pnas00297-0045-c.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a565/282027/6c77094524ff/pnas00297-0046-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a565/282027/a4e2fecc0c11/pnas00297-0047-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a565/282027/671dcc39ffe7/pnas00297-0047-b.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a565/282027/d0710c787379/pnas00297-0045-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a565/282027/e403a662a6df/pnas00297-0045-b.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a565/282027/2eb2c5233dbb/pnas00297-0045-c.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a565/282027/6c77094524ff/pnas00297-0046-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a565/282027/a4e2fecc0c11/pnas00297-0047-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a565/282027/671dcc39ffe7/pnas00297-0047-b.jpg

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本文引用的文献

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High throughput and targeted screens for prepilin peptidase inhibitors do not identify common inhibitors of eukaryotic gamma-secretase.高通量和靶向筛选前导肽酶抑制剂不能鉴定真核γ-分泌酶的常见抑制剂。
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Comprehending the Structure, Dynamics, and Mechanism of Action of Drug-Resistant HIV Protease.理解耐药性HIV蛋白酶的结构、动力学及作用机制。
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