Literature DB >> 2211682

NB-598: a potent competitive inhibitor of squalene epoxidase.

M Horie1, Y Tsuchiya, M Hayashi, Y Iida, Y Iwasawa, Y Nagata, Y Sawasaki, H Fukuzumi, K Kitani, T Kamei.   

Abstract

NB-598, (E)N-ethyl-N-(6,6-dimethyl-2-hepten-4-ynyl)-3-[(3,3'-bith iophen-5-yl)methoxy]benzene-methanamine, was found to inhibit human microsomal squalene epoxidase (from Hep G2 cells) in a competitive manner. NB-598 inhibited cholesterol synthesis from [14C]acetate dose dependently in Hep G2 cells and increased the intracellular radioactivity of squalene. A single oral administration of NB-598 inhibited cholesterol synthesis from [14C]acetate in rats. Moreover, multiple oral administration of NB-598 to dogs decreased serum total and low density lipoprotein cholesterol levels and increased serum squalene levels. After termination of treatment, the reduced serum cholesterol and increased squalene levels returned to their control values.

Entities:  

Mesh：

Substances：

Year:  1990        PMID： 2211682

Source DB:  PubMed          Journal:  J Biol Chem        ISSN： 0021-9258            Impact factor:   5.157


  20 in total

Review 1.  Antifungal agents: chemotherapeutic targets and immunologic strategies.

Authors:  N H Georgopapadakou; T J Walsh
Journal:  Antimicrob Agents Chemother       Date:  1996-02       Impact factor: 5.191

2.  Experimental model of escape phenomenon in hamsters and the effectiveness of YM-53601 in the model.

Authors:  Tohru Ugawa; Hirotoshi Kakuta; Hiroshi Moritani; Hisataka Shikama
Journal:  Br J Pharmacol       Date:  2002-03       Impact factor: 8.739

3.  Cholesterol biosynthesis from lanosterol: development of a novel assay method and characterization of rat liver microsomal lanosterol delta 24-reductase.

Authors:  S H Bae; Y K Paik
Journal:  Biochem J       Date:  1997-09-01       Impact factor: 3.857

4.  Squalene and cholesterol in the balance at the ER membrane.

Authors:  James A Nathan
Journal:  Proc Natl Acad Sci U S A       Date:  2020-04-01       Impact factor: 11.205

5.  Lipid raft localization of EGFR alters the response of cancer cells to the EGFR tyrosine kinase inhibitor gefitinib.

Authors:  Mary E Irwin; Kelly L Mueller; Natacha Bohin; Yubin Ge; Julie L Boerner
Journal:  J Cell Physiol       Date:  2011-09       Impact factor: 6.384

6.  Transcriptional Regulation of Cytosolic Sulfotransferase 1C2 by Intermediates of the Cholesterol Biosynthetic Pathway in Primary Cultured Rat Hepatocytes.

Authors:  Elizabeth A Rondini; Asmita Pant; Thomas A Kocarek
Journal:  J Pharmacol Exp Ther       Date:  2015-10-01       Impact factor: 4.030

7.  RPR 101821, a new potent cholesterol-lowering agent: inhibition of squalene synthase and 7-dehydrocholesterol reductase.

Authors:  D Amin; R Z Rutledge; S J Needle; D J Hele; K Neuenswander; R C Bush; G E Bilder; M H Perrone
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1996-01       Impact factor: 3.000

8.  Dual roles for cholesterol in mammalian cells.

Authors:  Fang Xu; Scott D Rychnovsky; Jitendra D Belani; Helen H Hobbs; Jonathan C Cohen; Robert B Rawson
Journal:  Proc Natl Acad Sci U S A       Date:  2005-09-30       Impact factor: 11.205

9.  Mevalonate-mediated suppression of 3-hydroxy-3-methylglutaryl coenzyme A reductase function in alpha-toxin-perforated cells.

Authors:  M D Giron; C M Havel; J A Watson
Journal:  Proc Natl Acad Sci U S A       Date:  1994-07-05       Impact factor: 11.205

10.  Zaragozic acids: a family of fungal metabolites that are picomolar competitive inhibitors of squalene synthase.

Authors:  J D Bergstrom; M M Kurtz; D J Rew; A M Amend; J D Karkas; R G Bostedor; V S Bansal; C Dufresne; F L VanMiddlesworth; O D Hensens
Journal:  Proc Natl Acad Sci U S A       Date:  1993-01-01       Impact factor: 11.205
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.