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费耶尔凝集素,一种源自[生物名称]皮肤的凝集素样肽,通过靶向糖蛋白41抑制HIV-1进入。

Fejerlectin, a Lectin-like Peptide from the Skin of , Inhibits HIV-1 Entry by Targeting Gp41.

作者信息

Xiong Weichen, Zhou Chenliang, Yin Shuwen, Chai Jinwei, Zeng Baishuang, Wu Jiena, Li Yibin, Li Lin, Xu Xueqing

机构信息

Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Shatai Nan Road, No. 1023-1063, Guangzhou 510515, China.

Department of Pharmacy, Sun Yat-sen University Cancer Center, State Key Laboratory of Oncology in South China, Collaborative Innovation Center for Cancer Medicine, Guangzhou 510060, China.

出版信息

ACS Omega. 2021 Feb 24;6(9):6414-6423. doi: 10.1021/acsomega.1c00033. eCollection 2021 Mar 9.

Abstract

Human immunodeficiency virus type 1 (HIV-1) is mainly transmitted by sexual intercourse, and effective microbicides preventing HIV-1 transmission are still required. Amphibian skin is a rich source of defense peptides with antiviral activity. Here, we characterized a lectin-like peptide, fejerlectin (RLCYMVLPCP), isolated from the skin of the frog . Fejerlectin showed significant hemagglutination and d-(+)-galacturonic acid-binding activities. Furthermore, fejerlectin suppressed the early entry of HIV-1 into target cells by binding to the N-terminal heptad repeat of HIV-1 gp41 and preventing 6-HB formation and Env-mediated membrane fusion. Fejerlectin is the smallest lectin-like peptide identified to date and represents a new and promising platform for anti-HIV-1 drug development.

摘要

1型人类免疫缺陷病毒(HIV-1)主要通过性行为传播,因此仍需要有效的预防HIV-1传播的杀菌剂。两栖动物皮肤是具有抗病毒活性的防御肽的丰富来源。在这里,我们鉴定了一种从青蛙皮肤中分离出来的类凝集素肽,费耶凝集素(RLCYMVLPCP)。费耶凝集素表现出显著的血凝和d-(+)-半乳糖醛酸结合活性。此外,费耶凝集素通过与HIV-1 gp41的N端七肽重复序列结合,抑制HIV-1早期进入靶细胞,并阻止六螺旋束(6-HB)的形成和Env介导的膜融合。费耶凝集素是迄今为止鉴定出的最小的类凝集素肽,代表了抗HIV-1药物开发的一个新的、有前景的平台。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7906/7948434/f4f8acb0e4ee/ao1c00033_0002.jpg

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