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

Bioorg Med Chem Lett. 2016 Apr 1;26(7):1671-4. doi: 10.1016/j.bmcl.2016.02.063.

Zhao Yang ¹, Zheng Fang ², Wei He ³, Zhixiang Wang ¹, Haifeng Gan ³, Qitao Tian ³, Kai Guo ³

Affiliations

1 School of Pharmaceutical Engineering, China Pharmaceutical University, No. 639 Longmian Avenue, Nanjing 211816, China.
2 School of Pharmaceutical Science, Nanjing Technology University, No. 30 Puzhu South Road, Nanjing 211816, China.
3 College of Biotechnology and Pharmaceutical Engineering, Nanjing Technology University, No. 30 Puzhu South Road, Nanjing 211816, China.

PMID: 26920800 DOI: 10.1016/j.bmcl.2016.02.063

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.

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