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.
authors.affiliation: School of Pharmaceutical Engineering, China Pharmaceutical University, No. 639 Longmian Avenue, Nanjing 211816, China.
authors.forename: Zhao
authors.initials: Z
authors.lastname: Yang
authors.affiliation: School of Pharmaceutical Science, Nanjing Technology University, No. 30 Puzhu South Road, Nanjing 211816, China.
authors.forename: Zheng
authors.initials: Z
authors.lastname: Fang
authors.affiliation: College of Biotechnology and Pharmaceutical Engineering, Nanjing Technology University, No. 30 Puzhu South Road, Nanjing 211816, China.
authors.forename: Wei
authors.initials: W
authors.lastname: He
authors.affiliation: School of Pharmaceutical Engineering, China Pharmaceutical University, No. 639 Longmian Avenue, Nanjing 211816, China.
authors.forename: Zhixiang
authors.initials: Z
authors.lastname: Wang
authors.affiliation: College of Biotechnology and Pharmaceutical Engineering, Nanjing Technology University, No. 30 Puzhu South Road, Nanjing 211816, China.
authors.forename: Haifeng
authors.initials: H
authors.lastname: Gan
authors.affiliation: College of Biotechnology and Pharmaceutical Engineering, Nanjing Technology University, No. 30 Puzhu South Road, Nanjing 211816, China.
authors.forename: Qitao
authors.initials: Q
authors.lastname: Tian
authors.affiliation: College of Biotechnology and Pharmaceutical Engineering, Nanjing Technology University, No. 30 Puzhu South Road, Nanjing 211816, China.
authors.forename: Kai
authors.initials: K
authors.lastname: Guo
mesh_terms: D020533:Angiogenesis Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D020650:Combinatorial Chemistry Techniques / Q000379:methods; D055808:Drug Discovery; D006801:Humans; D009369:Neoplasms / Q000098:blood supply / Q000188:drug therapy; D009389:Neovascularization, Pathologic / Q000188:drug therapy; D054852:Small Molecule Libraries / Q000737:chemistry* / Q000494:pharmacology*; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D054852:Small Molecule Libraries; D040301:Vascular Endothelial Growth Factor Receptor-2
keywords: Drug discovery; Dynamic combinatorial chemistry; Enzyme inhibitors; Imine formation; Ligand separation