title: Identification of polyoxometalates as inhibitors of basic fibroblast growth factor.
abstract: Angiogenesis is the process of new blood vessel formation from pre-existing ones. Angiogenic factors contribute to neovascularization that takes place in angiogenesis-dependent diseases, including cancer. Inhibiting the activity of the angiogenic factors to block the angiogenesis pathways is the current strategy of cancer therapy. Basic fibroblast growth factor (bFGF) is regarded as one of the most important angiogenic factors. Herein, we selected polyoxometalates (POMs) with different structures to study the interactions between bFGF and POMs. The results show that POMs could bind to the protein with high affinity, causing detectable changes in conformation and biophysical properties of protein. In addition, POMs could effectively inhibit the cell proliferation induced by bFGF. Significantly, we found that the structure, size and composition of POMs play a key role in the interactions between bFGF and POMs. This study will be meaningful for future screening and design of polyoxometalate-based anticancer drugs.
authors.affiliation: State Key Laboratory of Rare Earth Resources Utilization and Laboratory of Chemical Biology, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, 130022, China.
authors.forename: Fang
authors.initials: F
authors.lastname: Pu
authors.forename: Enbo
authors.initials: E
authors.lastname: Wang
authors.forename: Hongyu
authors.initials: H
authors.lastname: Jiang
authors.forename: Jinsong
authors.initials: J
authors.lastname: Ren
mesh_terms: D000704:Analysis of Variance; D001665:Binding Sites; D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D002942:Circular Dichroism; D016222:Fibroblast Growth Factor 2 / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000187:drug effects / Q000378:metabolism; D061307:Human Umbilical Vein Endothelial Cells / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D010446:Peptide Fragments / Q000737:chemistry / Q000378:metabolism; D011489:Protein Denaturation; D013050:Spectrometry, Fluorescence; D014357:Trypsin / Q000737:chemistry / Q000378:metabolism; D017973:Tungsten Compounds / Q000737:chemistry / Q000494:pharmacology*; D000099294:Polyoxometalates
chemical_list: D016222:Fibroblast Growth Factor 2; D010446:Peptide Fragments; D014357:Trypsin; D017973:Tungsten Compounds; C102296:polyoxometalate I; D000099294:Polyoxometalates