• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

通过整合素激活实现细胞毒性药物的分子递送。

Molecular Delivery of Cytotoxic Agents via Integrin Activation.

作者信息

Cirillo Martina, Giacomini Daria

机构信息

Department of Chemistry "Giacomo Ciamician", Alma Mater Studiorum University of Bologna, Via Selmi 2, 40126 Bologna, Italy.

出版信息

Cancers (Basel). 2021 Jan 15;13(2):299. doi: 10.3390/cancers13020299.

DOI:10.3390/cancers13020299
PMID:33467465
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7830197/
Abstract

Integrins are cell adhesion receptors overexpressed in tumor cells. A direct inhibition of integrins was investigated, but the best inhibitors performed poorly in clinical trials. A gained attention towards these receptors arouse because they could be target for a selective transport of cytotoxic agents. Several active-targeting systems have been developed to use integrins as a selective cell entrance for some antitumor agents. The aim of this review paper is to report on the most recent results on covalent conjugates between integrin ligands and antitumor drugs. Cytotoxic drugs thus conjugated through specific linker to integrin ligands, mainly RGD peptides, demonstrated that the covalent conjugates were more selective against tumor cells and hopefully with fewer side effects than the free drugs.

摘要

整合素是在肿瘤细胞中过度表达的细胞粘附受体。人们研究了对整合素的直接抑制作用，但最佳抑制剂在临床试验中的表现不佳。由于整合素可能成为细胞毒性药物选择性转运的靶点，因此受到了更多关注。已经开发了几种主动靶向系统，将整合素用作某些抗肿瘤药物的选择性细胞入口。这篇综述文章的目的是报告整合素配体与抗肿瘤药物之间共价缀合物的最新研究结果。通过特定连接子与整合素配体（主要是RGD肽）缀合的细胞毒性药物表明，共价缀合物对肿瘤细胞的选择性更高，有望比游离药物产生更少的副作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/6dc10ff1e7ac/cancers-13-00299-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/2dc93ab8f09a/cancers-13-00299-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/07085b8e7abb/cancers-13-00299-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/8f10bd3511ab/cancers-13-00299-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/a383f2f34c48/cancers-13-00299-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/97bc091452a4/cancers-13-00299-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/bef5f61ca1bd/cancers-13-00299-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/7e3379213e4a/cancers-13-00299-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/74d1426388e2/cancers-13-00299-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/c0d92c51bc1f/cancers-13-00299-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/0f71e959fe6e/cancers-13-00299-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/96c4a8a186a1/cancers-13-00299-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/bbf3e8c57cf7/cancers-13-00299-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/6dc10ff1e7ac/cancers-13-00299-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/2dc93ab8f09a/cancers-13-00299-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/07085b8e7abb/cancers-13-00299-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/8f10bd3511ab/cancers-13-00299-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/a383f2f34c48/cancers-13-00299-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/97bc091452a4/cancers-13-00299-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/bef5f61ca1bd/cancers-13-00299-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/7e3379213e4a/cancers-13-00299-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/74d1426388e2/cancers-13-00299-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/c0d92c51bc1f/cancers-13-00299-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/0f71e959fe6e/cancers-13-00299-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/96c4a8a186a1/cancers-13-00299-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/bbf3e8c57cf7/cancers-13-00299-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f49/7830197/6dc10ff1e7ac/cancers-13-00299-g013.jpg

相似文献

1
Molecular Delivery of Cytotoxic Agents via Integrin Activation.通过整合素激活实现细胞毒性药物的分子递送。
Cancers (Basel). 2021 Jan 15;13(2):299. doi: 10.3390/cancers13020299.
2
Integrin-Targeted Peptide- and Peptidomimetic-Drug Conjugates for the Treatment of Tumors.用于治疗肿瘤的整合素靶向肽和拟肽药物偶联物
Recent Pat Anticancer Drug Discov. 2017;12(2):148-168. doi: 10.2174/1574892812666170203151930.
3
Integrin-targeted delivery into cancer cells of a Pt(IV) pro-drug through conjugation to RGD-containing peptides.通过与含RGD肽偶联将铂（IV）前药靶向递送至癌细胞。
Dalton Trans. 2015 Jan 7;44(1):202-12. doi: 10.1039/c4dt02710h.
4
The organometallic ferrocene exhibits amplified anti-tumor activity by targeted delivery via highly selective ligands to αvβ3, αvβ6, or α5β1 integrins.有机金属配合物二茂铁通过与 αvβ3、αvβ6 或 α5β1 整合素的高选择性配体进行靶向递送，表现出增强的抗肿瘤活性。
Biomaterials. 2021 Apr;271:120754. doi: 10.1016/j.biomaterials.2021.120754. Epub 2021 Mar 12.
5
RGD-mediated delivery of small-molecule drugs.RGD介导的小分子药物递送。
Future Med Chem. 2017 Apr;9(6):579-604. doi: 10.4155/fmc-2017-0008. Epub 2017 Apr 10.
6
VivoTag-S680–conjugated 3-aminomethyl αβ antagonist derivative for fluorescence molecular tomography of tumors用于肿瘤荧光分子断层成像的VivoTag-S680共轭3-氨基甲基αβ拮抗剂衍生物
7
Delivery of Theranostic Nanoparticles to Various Cancers by Means of Integrin-Binding Peptides.通过整合素结合肽将治疗性纳米颗粒递送至各种癌症。
Int J Mol Sci. 2022 Nov 8;23(22):13735. doi: 10.3390/ijms232213735.
8
Integrin-Targeting Peptides for the Design of Functional Cell-Responsive Biomaterials.用于设计功能性细胞响应生物材料的整合素靶向肽
Biomedicines. 2020 Aug 25;8(9):307. doi: 10.3390/biomedicines8090307.
9
I-Labeled arginine-arginine-leucine (RRL)-containing cyclic peptide (YCGGRRLGGC) for imaging prostate carcinoma用于前列腺癌成像的含I标记精氨酸-精氨酸-亮氨酸（RRL）的环肽（YCGGRRLGGC）
10
Tumor Targeting via Integrin Ligands.通过整合素配体实现肿瘤靶向
Front Oncol. 2013 Aug 30;3:222. doi: 10.3389/fonc.2013.00222.

引用本文的文献

1
Interpreting the function of cell penetrating peptide (RGD) in drug transport to the cell membrane: a computational approach.解析细胞穿透肽（RGD）在药物向细胞膜转运中的功能：一种计算方法。
Sci Rep. 2024 Nov 29;14(1):29668. doi: 10.1038/s41598-024-80060-7.
2
Targeting Cytotoxic Agents through EGFR-Mediated Covalent Binding and Release.通过 EGFR 介导的共价结合和释放靶向细胞毒性剂。
J Med Chem. 2023 Sep 14;66(17):12324-12341. doi: 10.1021/acs.jmedchem.3c00845. Epub 2023 Aug 30.
3
Fabrication of curcumin-loaded magnetic PEGylated-PLGA nanocarriers tagged with GRGDS peptide for improving anticancer activity.

本文引用的文献

1
RGD-modified dihydrolipoamide dehydrogenase conjugated to titanium dioxide nanoparticles - integrin-targeted photodynamic treatment of melanoma cells.RGD修饰的二氢硫辛酰胺脱氢酶与二氧化钛纳米颗粒偶联——整合素靶向光动力治疗黑色素瘤细胞
RSC Adv. 2018 Mar 1;8(17):9112-9119. doi: 10.1039/c7ra13777j. eCollection 2018 Feb 28.
2
Surface receptor-mediated targeted drug delivery systems for enhanced cancer treatment: A state-of-the-art review.用于增强癌症治疗的表面受体介导的靶向给药系统：最新综述
Drug Dev Res. 2021 May;82(3):309-340. doi: 10.1002/ddr.21758. Epub 2020 Nov 10.
3
fabrication of MS@MnO hybrid as nanozymes for enhancing ROS-mediated breast cancer therapy.
负载姜黄素的磁性聚乙二醇化聚乳酸-羟基乙酸共聚物纳米载体的制备及其与GRGDS肽结合以提高抗癌活性
MethodsX. 2023 May 23;10:102229. doi: 10.1016/j.mex.2023.102229. eCollection 2023.
4
Targeting Integrins for Cancer Therapy - Disappointments and Opportunities.靶向整合素用于癌症治疗——失望与机遇
Front Cell Dev Biol. 2022 Mar 9;10:863850. doi: 10.3389/fcell.2022.863850. eCollection 2022.
5
Selective Integrin Ligands Promote Cell Internalization of the Antineoplastic Agent Fluorouracil.选择性整合素配体促进抗肿瘤药物氟尿嘧啶的细胞内化。
ACS Pharmacol Transl Sci. 2021 Sep 2;4(5):1528-1542. doi: 10.1021/acsptsci.1c00094. eCollection 2021 Oct 8.
将 MS@MnO 杂化作为纳米酶用于增强 ROS 介导的乳腺癌治疗的制备。
Nanoscale. 2020 Nov 12;12(43):22317-22329. doi: 10.1039/d0nr03931d.
4
Biological Relevance of RGD-Integrin Subtype-Specific Ligands in Cancer.RGD 整联蛋白亚型特异性配体在癌症中的生物学相关性。
Chembiochem. 2021 Apr 6;22(7):1151-1160. doi: 10.1002/cbic.202000626. Epub 2020 Nov 27.
5
New insights into the activities and toxicities of the old anticancer drug doxorubicin.对老抗癌药物阿霉素的活性和毒性的新认识。
FEBS J. 2021 Nov;288(21):6095-6111. doi: 10.1111/febs.15583. Epub 2020 Oct 19.
6
Integrin-Targeting Peptides for the Design of Functional Cell-Responsive Biomaterials.用于设计功能性细胞响应生物材料的整合素靶向肽
Biomedicines. 2020 Aug 25;8(9):307. doi: 10.3390/biomedicines8090307.
7
Cancer therapy: Attempt cure or manage drug resistance?癌症治疗：尝试治愈还是应对耐药性？
Evol Appl. 2020 Aug 6;13(7):1660-1672. doi: 10.1111/eva.12994. eCollection 2020 Aug.
8
Dihydrolipoamide dehydrogenase moonlighting activity as a DNA chelating agent.二氢硫辛酰胺脱氢酶作为DNA螯合剂的兼职活性。
Proteins. 2020 Aug 6. doi: 10.1002/prot.25991.
9
Dual Targeting of Norepinephrine Transporter (NET) Function and Thyrointegrin αvβ3 Receptors in the Treatment of Neuroblastoma.靶向去甲肾上腺素转运体（NET）功能和甲状腺球蛋白αvβ3 受体治疗神经母细胞瘤。
J Med Chem. 2020 Jul 23;63(14):7653-7662. doi: 10.1021/acs.jmedchem.0c00537. Epub 2020 Jul 7.
10
5-Fluorouracil resistance mechanisms in colorectal cancer: From classical pathways to promising processes.结直肠癌中5-氟尿嘧啶的耐药机制：从经典途径到有前景的过程
Cancer Sci. 2020 Sep;111(9):3142-3154. doi: 10.1111/cas.14532. Epub 2020 Aug 13.