文献检索文档翻译深度研究
Suppr Zotero 插件Zotero 插件
邀请有礼套餐&价格历史记录

新学期，新优惠

限时优惠:9月1日-9月22日

30天高级会员仅需29元

1天体验卡首发特惠仅需5.99元

了解详情
不再提醒
插件&应用
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
高级版
套餐订阅购买积分包
AI 工具
文献检索文档翻译深度研究
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 @ 2025

靶向树枝状抗癌前药：一种甲氨蝶呤-叶酸-聚（酰胺胺）共轭物及一种新型、快速的“一锅法”合成方法。

Targeted dendrimeric anticancer prodrug: a methotrexate-folic acid-poly(amidoamine) conjugate and a novel, rapid, "one pot" synthetic approach.

作者信息

Zhang Yuehua, Thomas Thommey P, Desai Ankur, Zong Hong, Leroueil Pascale R, Majoros Istvan J, Baker James R

机构信息

Michigan Nanotechnology Institute for Medicine and Biological Sciences, Department of Internal Medicine, University of Michigan, Ann Arbor, Michigan 48109.

出版信息

Bioconjug Chem. 2010 Mar 17;21(3):489-95. doi: 10.1021/bc9003958. Epub 2010 Feb 3.

DOI:10.1021/bc9003958
PMID:20128612
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2892195/
Abstract

A targeted dendrimeric anticancer prodrug, a conjugate of generation 5 (G5) polyamidoamine (PAMAM) dendrimer, folic acid (FA), and methotrexate (MTX), has been successfully synthesized by using a novel "one pot" approach which is simple, reproducible, and feasible for large-scale synthesis. All dendrimer products have been characterized by (1)H NMR, MALDI-TOF, GPC, and HPLC. With this new method, the ratio of FA versus MTX attached to the dendrimer can be easily tuned to achieve the desired therapeutic effect. A new analytical approach for calculating the numbers of FA and MTX attached to the dendrimer has been established. In vitro studies performed on FA receptor-expressing KB cells show that the new conjugate has a similar affinity and cytotoxic potency to G5-FA-MTX synthesized using the traditional multiple-step approach.

摘要

一种靶向树枝状抗癌前药，即第5代（G5）聚酰胺-胺（PAMAM）树枝状大分子、叶酸（FA）和甲氨蝶呤（MTX）的共轭物，已通过一种新颖的“一锅法”成功合成，该方法简单、可重复且适用于大规模合成。所有树枝状大分子产物均已通过¹H NMR、基质辅助激光解吸电离飞行时间质谱（MALDI-TOF）、凝胶渗透色谱（GPC）和高效液相色谱（HPLC）进行了表征。采用这种新方法，可以轻松调节连接到树枝状大分子上的FA与MTX的比例，以实现所需的治疗效果。已建立了一种计算连接到树枝状大分子上的FA和MTX数量的新分析方法。在表达FA受体的KB细胞上进行的体外研究表明，这种新的共轭物与使用传统多步方法合成的G5-FA-MTX具有相似的亲和力和细胞毒性效力。

相似文献

[1]
Targeted dendrimeric anticancer prodrug: a methotrexate-folic acid-poly(amidoamine) conjugate and a novel, rapid, "one pot" synthetic approach.

Bioconjug Chem. 2010-3-17

[2]
Bifunctional PAMAM dendrimer conjugates of folic acid and methotrexate with defined ratio.

Biomacromolecules. 2012-3-30

[3]
Targeting and inhibition of cell growth by an engineered dendritic nanodevice.

J Med Chem. 2005-6-2

[4]
Preclinical antitumor efficacy evaluation of dendrimer-based methotrexate conjugates.

Anticancer Drugs. 2008-2

[5]
Design considerations for PAMAM dendrimer therapeutics.

Bioorg Med Chem Lett. 2013-4-1

[6]
Dendrimeric anticancer prodrugs for targeted delivery of ursolic acid to folate receptor-expressing cancer cells: synthesis and biological evaluation.

Eur J Pharm Sci. 2015-4-5

[7]
PAMAM dendrimer-based multifunctional conjugate for cancer therapy: synthesis, characterization, and functionality.

Biomacromolecules. 2006-2

[8]
Folate Receptor-Targeted Dendrimer-Methotrexate Conjugate for Inflammatory Arthritis.

J Biomed Nanotechnol. 2015-8

[9]
Polyvalent dendrimer-methotrexate as a folate receptor-targeted cancer therapeutic.

Mol Pharm. 2012-8-7

[10]
Polyvalent saccharide-functionalized generation 3 poly(amidoamine) dendrimer-methotrexate conjugate as a potential anticancer agent.

Bioorg Med Chem. 2011-3-12

引用本文的文献

[1]
Dendrimer-Coated Gold Nanoparticles for Efficient Folate-Targeted mRNA Delivery In Vitro.

Pharmaceutics. 2021-6-17

[2]
Targeting Groups Employed in Selective Dendrons and Dendrimers.

Pharmaceutics. 2018-11-8

[3]
Dendrimer Prodrugs.

Molecules. 2016-5-31

[4]
Design and in vitro validation of multivalent dendrimer methotrexates as a folate-targeting anticancer therapeutic.

Curr Pharm Des. 2013

[5]
Polyvalent dendrimer-methotrexate as a folate receptor-targeted cancer therapeutic.

Mol Pharm. 2012-8-7

[6]
Folate-targeted nanoparticles show efficacy in the treatment of inflammatory arthritis.

Arthritis Rheum. 2011-9

[7]
Polyvalent saccharide-functionalized generation 3 poly(amidoamine) dendrimer-methotrexate conjugate as a potential anticancer agent.

Bioorg Med Chem. 2011-3-12

本文引用的文献

[1]
Amphiphilic multi-arm-block copolymer conjugated with doxorubicin via pH-sensitive hydrazone bond for tumor-targeted drug delivery.

Biomaterials. 2009-10

[2]
Nanocarriers as an emerging platform for cancer therapy.

Nat Nanotechnol. 2007-12

[3]
Antitumoral activity of PEG-gemcitabine prodrugs targeted by folic acid.

J Control Release. 2008-5-8

[4]
Discovery and development of folic-acid-based receptor targeting for imaging and therapy of cancer and inflammatory diseases.

Acc Chem Res. 2008-1

[5]
The binding avidity of a nanoparticle-based multivalent targeted drug delivery platform.

Chem Biol. 2007-1

[6]
HPLC analysis of functionalized poly(amidoamine) dendrimers and the interaction between a folate-dendrimer conjugate and folate binding protein.

Analyst. 2006-7

[7]
PAMAM dendrimer-based multifunctional conjugate for cancer therapy: synthesis, characterization, and functionality.

Biomacromolecules. 2006-2

[8]
Poly(amidoamine) dendrimer-based multifunctional engineered nanodevice for cancer therapy.

J Med Chem. 2005-9-22

[9]
Folate receptor-mediated drug targeting: from therapeutics to diagnostics.

J Pharm Sci. 2005-10

[10]
Nanoparticle targeting of anticancer drug improves therapeutic response in animal model of human epithelial cancer.

Cancer Res. 2005-6-15

文献AI研究员

20分钟写一篇综述，助力文献阅读效率提升50倍

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

推荐工具

医学文档翻译智能文献检索