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多胺-药物偶联物:它们能增强药物活性吗?

Polyamine-Drug Conjugates: Do They Boost Drug Activity?

机构信息

Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.

出版信息

Molecules. 2023 Jun 2;28(11):4518. doi: 10.3390/molecules28114518.

DOI:10.3390/molecules28114518
PMID:37298993
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10254200/
Abstract

Over the past two decades, the strategy of conjugating polyamine tails with bioactive molecules such as anticancer and antimicrobial agents, as well as antioxidant and neuroprotective scaffolds, has been widely exploited to enhance their pharmacological profile. Polyamine transport is elevated in many pathological conditions, suggesting that the polyamine portion could improve cellular and subcellular uptake of the conjugate via the polyamine transporter system. In this review, we have presented a glimpse on the polyamine conjugate scenario, classified by therapeutic area, of the last decade with the aim of highlighting achievements and fostering future developments.

摘要

在过去的二十年中,人们广泛地利用将多胺尾巴与生物活性分子(如抗癌和抗菌剂以及抗氧化剂和神经保护支架)缀合的策略来增强它们的药理学特性。在许多病理条件下,多胺的转运都会增加,这表明多胺部分可以通过多胺转运系统改善缀合物的细胞和亚细胞摄取。在这篇综述中,我们按治疗领域分类介绍了过去十年中多胺缀合物的情况,旨在突出成就并促进未来的发展。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af4e/10254200/0468407ca9ce/molecules-28-04518-g021.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af4e/10254200/ca6b12527726/molecules-28-04518-g002.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af4e/10254200/ec09d4c13d7c/molecules-28-04518-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af4e/10254200/9c5a11c51309/molecules-28-04518-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af4e/10254200/2ee7a4d558b0/molecules-28-04518-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af4e/10254200/fd75bd833d49/molecules-28-04518-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af4e/10254200/3af62d5af408/molecules-28-04518-g012.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af4e/10254200/108d88a0bb99/molecules-28-04518-g014.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af4e/10254200/52cae124b9f1/molecules-28-04518-g016.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af4e/10254200/87fa023cdb6b/molecules-28-04518-g017.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af4e/10254200/3c659d6c0fe0/molecules-28-04518-g018.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af4e/10254200/9d837a62e560/molecules-28-04518-g019.jpg
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