Peptide inhibitors of human HMG-CoA reductase as potential hypocholesterolemia agents

被引：20

作者：

Lin, Shih-Hung ^{[1
,2
]}

Chang, Ding-Kwo ^{[3
]}

Chou, Mei-Ju ^{[3
]}

Huang, Kao-Jean ^{[1
,2
]}

Shiuan, David ^{[1
,2
]}

机构：

[1] Natl Dong Hwa Univ, Dept Life Sci, Hualien 974, Taiwan

[2] Natl Dong Hwa Univ, Inst Biotechnol, Hualien 974, Taiwan

[3] Acad Sinica, Inst Chem, Taipei 112, Taiwan

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 2015年 / 456卷 / 01期

关键词：

HMG-CoA reductase; Phage display; Molecule docking; PROTEIN; LIBRARIES; MECHANISM;

D O I：

10.1016/j.bbrc.2014.11.042

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 mu M), could be a lead compound to develop hypocholesterolemic agents. (C) 2014 Elsevier Inc. All rights reserved.

引用

页码：104 / 109

页数：6

共 50 条

[11] HMG-COA REDUCTASE INHIBITORS, A NOVEL CLASS OF HYPOLIPIDEMIC AGENTS
SMITH, RL
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1987, 194 : 91 - MEDI
[12] Various HMG-CoA reductase inhibitors
Thiery, J
Seidel, D
[J]. INTERNIST, 1999, 40 (01): : 113 - 114
[13] HMG-CoA reductase inhibitors and the kidney
Vito M. Campese
Bassel Hadaya
Josephine Chiu
[J]. Current Hypertension Reports, 2005, 7 : 337 - 342
[14] HMG-CoA reductase inhibitors and apoptosis
Senatore, M
Buemi, M
[J]. NEPHRON, 1999, 81 (04): : 439 - 440
[15] HMG-CoA reductase inhibitors and myotoxicity
Ucar, M
Mjörndal, T
Dahlqvist, R
[J]. DRUG SAFETY, 2000, 22 (06) : 441 - 457
[16] Rhabdomyolysis and HMG-CoA reductase inhibitors
Omar, MA
Wilson, JP
Cox, TS
[J]. ANNALS OF PHARMACOTHERAPY, 2001, 35 (09) : 1096 - 1107
[17] HMG-CoA Reductase Inhibitors and Myotoxicity
Memduh Ucar
Tom Mjörndal
Rune Dahlqvist
[J]. Drug Safety, 2000, 22 : 441 - 457
[18] Syntheses of HMG-CoA reductase inhibitors
Nissan Chemical Industries, Ltd, Chiba, Japan
[J]. Yuki Gosei Kagaku Kyokaishi, 3 (186-196):
[19] SYNTHESES OF HMG-COA REDUCTASE INHIBITORS
MIYACHI, N
SUZUKI, M
OHARA, Y
HIYAMA, T
[J]. JOURNAL OF SYNTHETIC ORGANIC CHEMISTRY JAPAN, 1995, 53 (03) : 186 - 196
[20] IMIDAZOLES AS HMG-COA REDUCTASE INHIBITORS
WAREING, JR
LEGINUS, JM
SCALLEN, TJ
LINDER, J
LEE, GT
STABLER, R
MARTIN, M
WIDLER, L
MYERS, SW
[J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1988, 196 : 106 - MEDI

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