title: Peptide inhibitors of human HMG-CoA reductase as potential hypocholesterolemia agents.
abstract: Hypercholesterolemia may lead to obesity and cardiovascular diseases. To prevent hypercholesterolemia, many drugs have been developed while searching for better drugs to treat hypercholesterolemia has never been ended. Other than small molecule drugs, peptide drugs are gaining more visibilities in many therapeutic areas. In the present study, we employed phage-display techniques to screen peptide inhibitors against human HMG-CoA reductase. The results indicate that the tetrapeptide PMAS inhibits hHMGR effectively (IC50=68 μM), could be a lead compound to develop hypocholesterolemic agents.
authors.affiliation: Department of Life Science and Institute of Biotechnology, National Dong Hwa University, Hualien 974, Taiwan, ROC.
authors.forename: Shih-Hung
authors.initials: SH
authors.lastname: Lin
authors.affiliation: Institute of Chemistry, Academia Sinica, Taipei 112, Taiwan, ROC.
authors.forename: Ding-Kwo
authors.initials: DK
authors.lastname: Chang
authors.affiliation: Institute of Chemistry, Academia Sinica, Taipei 112, Taiwan, ROC.
authors.forename: Mei-Ju
authors.initials: MJ
authors.lastname: Chou
authors.affiliation: Department of Life Science and Institute of Biotechnology, National Dong Hwa University, Hualien 974, Taiwan, ROC.
authors.forename: Kao-Jean
authors.initials: KJ
authors.lastname: Huang
authors.affiliation: Department of Life Science and Institute of Biotechnology, National Dong Hwa University, Hualien 974, Taiwan, ROC. Electronic address: shiuan@mail.ndhu.edu.tw.
authors.forename: David
authors.initials: D
authors.lastname: Shiuan
mesh_terms: D000924:Anticholesteremic Agents / Q000737:chemistry*; D003001:Cloning, Molecular; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D050171:Dyslipidemias / Q000188:drug therapy*; D004791:Enzyme Inhibitors / Q000737:chemistry*; D004797:Enzyme-Linked Immunosorbent Assay; D004926:Escherichia coli / Q000378:metabolism; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D062105:Molecular Docking Simulation; D019151:Peptide Library; D011485:Protein Binding; D011487:Protein Conformation; D011994:Recombinant Proteins / Q000378:metabolism
chemical_list: D000924:Anticholesteremic Agents; D004791:Enzyme Inhibitors; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D019151:Peptide Library; D011994:Recombinant Proteins
keywords: HMG-CoA reductase; Molecule docking; Phage display