Identification of inhibitors for vascular endothelial growth factor receptor by using dynamic combinatorial chemistry

Zhao Yang; Zheng Fang; Wei He; Zhixiang Wang; Haifeng Gan; Qitao Tian; Kai Guo

doi:10.1016/j.bmcl.2016.02.063

Identification of inhibitors for vascular endothelial growth factor receptor by using dynamic combinatorial chemistry

Zhao Yang, Zheng Fang, Wei He, Zhixiang Wang, Haifeng Gan, Qitao Tian, Kai Guo

COLLEGE OF BIOTECHNOLOGY AND PHARMACEUTICAL ENGINEERING

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

7 Scopus citations

Abstract

The novel analysis method consisting of size-exclusion chromatography (SEC) and HRMS analysis was firstly applied in the discovery of potential inhibitors towards cancer drug targets. With vascular endothelial growth factor receptor (VEGFR-2) as a target, dynamic combinatorial libraries (DCLs) were prepared by reacting aldehydes with amines. Four sensitive binders targeted VEGFR-2 were directly isolated from the library. Antitumor activity test in vitro and inhibition experiments toward angiogenesis were also carried out.

Original language	English
Pages (from-to)	1671-1674
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	26
Issue number	7
DOIs	https://doi.org/10.1016/j.bmcl.2016.02.063
State	Published - 2016

Keywords

Drug discovery
Dynamic combinatorial chemistry
Enzyme inhibitors
Imine formation
Ligand separation

UN SDGs

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

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10.1016/j.bmcl.2016.02.063

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title = "Identification of inhibitors for vascular endothelial growth factor receptor by using dynamic combinatorial chemistry",

abstract = "The novel analysis method consisting of size-exclusion chromatography (SEC) and HRMS analysis was firstly applied in the discovery of potential inhibitors towards cancer drug targets. With vascular endothelial growth factor receptor (VEGFR-2) as a target, dynamic combinatorial libraries (DCLs) were prepared by reacting aldehydes with amines. Four sensitive binders targeted VEGFR-2 were directly isolated from the library. Antitumor activity test in vitro and inhibition experiments toward angiogenesis were also carried out.",

keywords = "Drug discovery, Dynamic combinatorial chemistry, Enzyme inhibitors, Imine formation, Ligand separation",

author = "Zhao Yang and Zheng Fang and Wei He and Zhixiang Wang and Haifeng Gan and Qitao Tian and Kai Guo",

note = "Publisher Copyright: {\textcopyright} 2016 Elsevier Ltd",

year = "2016",

doi = "10.1016/j.bmcl.2016.02.063",

language = "英语",

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pages = "1671--1674",

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T1 - Identification of inhibitors for vascular endothelial growth factor receptor by using dynamic combinatorial chemistry

AU - Yang, Zhao

AU - Fang, Zheng

AU - He, Wei

AU - Wang, Zhixiang

AU - Gan, Haifeng

AU - Tian, Qitao

AU - Guo, Kai

PY - 2016

Y1 - 2016

N2 - The novel analysis method consisting of size-exclusion chromatography (SEC) and HRMS analysis was firstly applied in the discovery of potential inhibitors towards cancer drug targets. With vascular endothelial growth factor receptor (VEGFR-2) as a target, dynamic combinatorial libraries (DCLs) were prepared by reacting aldehydes with amines. Four sensitive binders targeted VEGFR-2 were directly isolated from the library. Antitumor activity test in vitro and inhibition experiments toward angiogenesis were also carried out.

AB - The novel analysis method consisting of size-exclusion chromatography (SEC) and HRMS analysis was firstly applied in the discovery of potential inhibitors towards cancer drug targets. With vascular endothelial growth factor receptor (VEGFR-2) as a target, dynamic combinatorial libraries (DCLs) were prepared by reacting aldehydes with amines. Four sensitive binders targeted VEGFR-2 were directly isolated from the library. Antitumor activity test in vitro and inhibition experiments toward angiogenesis were also carried out.

KW - Drug discovery

KW - Dynamic combinatorial chemistry

KW - Enzyme inhibitors

KW - Imine formation

KW - Ligand separation

UR - http://www.scopus.com/inward/record.url?scp=84982972424&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2016.02.063

DO - 10.1016/j.bmcl.2016.02.063

M3 - 文章

C2 - 26920800

AN - SCOPUS:84982972424

SN - 0960-894X

VL - 26

SP - 1671

EP - 1674

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 7

ER -

Identification of inhibitors for vascular endothelial growth factor receptor by using dynamic combinatorial chemistry

Abstract

Keywords

UN SDGs

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