Synthesis and antiangiogenic properties of 2-methoxestradiol-RGD peptide conjugates

Min Hang Xin; Hua Xiang; Wen Bo Si; Wei Zhao; Hong Xiao; Qi Dong You

Synthesis and antiangiogenic properties of 2-methoxestradiol-RGD peptide conjugates

Min Hang Xin
, Hua Xiang
, Wen Bo Si
, Wei Zhao
, Hong Xiao
, Qi Dong You

China Pharmaceutical University
Nanjing Medical University

Research output: Contribution to journal › Article › peer-review

2 Scopus citations

Abstract

A series of 2-methoxyestradiol (2-MeO-E₂) RGD peptide conjugates with coupling RGD peptides to 3- position or 17-position of 2-MeO-E₂ through space linker were synthesized. Their antiangiogenic properties were preliminarily evaluated by cell migration scratch assays against HUVECs. Compound 26c binding RGDV peptide showed the best inhibitory effect. In addition, all 2-MeO-E₂ RGD peptide conjugates exhibited obvious activity. These results demonstrate that conjugates with RGD peptides represent a promising means for targeting angiogenesis in cancer therapy.

Original language	English
Pages (from-to)	198-205
Number of pages	8
Journal	Journal of China Pharmaceutical University
Volume	42
Issue number	3
State	Published - Jun 2011
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

2-Methoxyestradiol
Antiangiogenic properties
Cell migration scratch assays
RGD peptide conjugates

Cite this

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title = "Synthesis and antiangiogenic properties of 2-methoxestradiol-RGD peptide conjugates",

abstract = "A series of 2-methoxyestradiol (2-MeO-E2) RGD peptide conjugates with coupling RGD peptides to 3- position or 17-position of 2-MeO-E2 through space linker were synthesized. Their antiangiogenic properties were preliminarily evaluated by cell migration scratch assays against HUVECs. Compound 26c binding RGDV peptide showed the best inhibitory effect. In addition, all 2-MeO-E2 RGD peptide conjugates exhibited obvious activity. These results demonstrate that conjugates with RGD peptides represent a promising means for targeting angiogenesis in cancer therapy.",

keywords = "2-Methoxyestradiol, Antiangiogenic properties, Cell migration scratch assays, RGD peptide conjugates",

author = "Xin, \{Min Hang\} and Hua Xiang and Si, \{Wen Bo\} and Wei Zhao and Hong Xiao and You, \{Qi Dong\}",

year = "2011",

month = jun,

language = "英语",

volume = "42",

pages = "198--205",

journal = "Journal of China Pharmaceutical University",

issn = "1000-5048",

publisher = "China Pharmaceutical University",

number = "3",

}

TY - JOUR

T1 - Synthesis and antiangiogenic properties of 2-methoxestradiol-RGD peptide conjugates

AU - Xin, Min Hang

AU - Xiang, Hua

AU - Si, Wen Bo

AU - Zhao, Wei

AU - Xiao, Hong

AU - You, Qi Dong

PY - 2011/6

Y1 - 2011/6

N2 - A series of 2-methoxyestradiol (2-MeO-E2) RGD peptide conjugates with coupling RGD peptides to 3- position or 17-position of 2-MeO-E2 through space linker were synthesized. Their antiangiogenic properties were preliminarily evaluated by cell migration scratch assays against HUVECs. Compound 26c binding RGDV peptide showed the best inhibitory effect. In addition, all 2-MeO-E2 RGD peptide conjugates exhibited obvious activity. These results demonstrate that conjugates with RGD peptides represent a promising means for targeting angiogenesis in cancer therapy.

AB - A series of 2-methoxyestradiol (2-MeO-E2) RGD peptide conjugates with coupling RGD peptides to 3- position or 17-position of 2-MeO-E2 through space linker were synthesized. Their antiangiogenic properties were preliminarily evaluated by cell migration scratch assays against HUVECs. Compound 26c binding RGDV peptide showed the best inhibitory effect. In addition, all 2-MeO-E2 RGD peptide conjugates exhibited obvious activity. These results demonstrate that conjugates with RGD peptides represent a promising means for targeting angiogenesis in cancer therapy.

KW - 2-Methoxyestradiol

KW - Antiangiogenic properties

KW - Cell migration scratch assays

KW - RGD peptide conjugates

UR - https://www.scopus.com/pages/publications/79960417674

M3 - 文章

AN - SCOPUS:79960417674

SN - 1000-5048

VL - 42

SP - 198

EP - 205

JO - Journal of China Pharmaceutical University

JF - Journal of China Pharmaceutical University

IS - 3

ER -

Synthesis and antiangiogenic properties of 2-methoxestradiol-RGD peptide conjugates

Abstract

UN SDGs

Keywords

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