An in vitro assay for evaluation of small-molecule inhibitors of cholesterol absorption

被引：36
作者：
Kværno, L
Ritter, T
Werder, M
Hauser, H
Carreira, EM
机构：
[1] ETH Honggerberg, Organ Chem Lab, CH-8093 Zurich, Switzerland
[2] ETH Honggerberg, Inst Biochem, CH-8093 Zurich, Switzerland
来源：
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2004年 / 43卷 / 35期
关键词：
cholesterol; inhibitors; medicinal chemistry; membranes;
D O I：
10.1002/anie.200460348
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
Giving cholesterol the brush off: An intestinal brush border membrane vesicle assay has been devised for the convenient in vitro testing of small molecules for inhibition of cholesterol absorption. The assay was used to identify new nonhydrolyzable glycosides as potent cholesterol-absorption inhibitors and an oxazolidinone as an effective replacement of the β-lactam scaffold of ezetimibe (1).
引用
收藏
页码：4653 / 4656
页数：4
相关论文
共 50 条
  • [41] New Small-molecule Analgesics
    Laev, S. Sergey
    Salakhutdinov, F. Nariman
    CURRENT MEDICINAL CHEMISTRY, 2021, 28 (30) : 6234 - 6273
  • [42] Psoromic Acid Derivatives: A New Family of Small-Molecule Pre-mRNA Splicing Inhibitors Discovered by a Stage-Specific High-Throughput in Vitro Splicing Assay
    Samatov, Timur R.
    Wolf, Alexander
    Odenwaelder, Peter
    Bessonov, Sergey
    Deraeve, Celine
    Bon, Robin S.
    Waldmann, Herbert
    Luehrmann, Reinhard
    CHEMBIOCHEM, 2012, 13 (05) : 640 - 644
  • [43] Pyrrole-Based Macrocyclic Small-Molecule Inhibitors That Target Oocyte Maturation
    Gunasekaran, Pethaiah
    Lee, So-Rim
    Jeong, Seung-Min
    Kwon, Jeong-Woo
    Takei, Toshiki
    Asahina, Yuya
    Bang, Geul
    Kim, Seongnyeon
    Ahn, Mija
    Ryu, Eun Kyung
    Kim, Hak Nam
    Nam, Ki-Yub
    Shin, Song Yub
    Hojo, Hironobu
    Namgoong, Suk
    Kim, Nam-Hyung
    Bang, Jeong Kyu
    CHEMMEDCHEM, 2017, 12 (08) : 580 - 589
  • [44] Small-molecule inhibitors targeting apoptosis signal-regulated kinase 1
    Wang, Tiantian
    Pang, Lidan
    He, Mengni
    Wang, Zengtao
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023, 262
  • [45] Synthesis and Biological Assay of Small-Molecule Quorum Sensing Inhibitors: A Three-Week Course-Based Undergraduate Research Experience
    Dorn, Stanna K.
    Newman, Jane D.
    van Kessel, Julia C.
    Brown, Laura C.
    JOURNAL OF CHEMICAL EDUCATION, 2021, 98 (11) : 3533 - 3541
  • [46] Recent progress of small-molecule of RET inhibitors against Non-small cell lung cancer
    Jiayi Shen
    Liping Chen
    Yulan Song
    Sheng Chen
    Wei Guo
    Yongdong Li
    AAPS Open, 10 (1)
  • [47] Substrate Activity Screening with Kinases: Discovery of Small-Molecule Substrate-Competitive c-Src Inhibitors
    Breen, Meghan E.
    Steffey, Michael E.
    Lachacz, Eric J.
    Kwarcinski, Frank E.
    Fox, Christel C.
    Soellner, Matthew B.
    ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2014, 53 (27) : 7010 - 7013
  • [48] Discovery of Small-Molecule Inhibitors of the TLR1/TLR2 Complex
    Cheng, Kui
    Wang, Xiaohui
    Zhang, Shuting
    Yin, Hang
    ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2012, 51 (49) : 12246 - 12249
  • [49] Small-molecule HIV-1 integrase inhibitors: the 2001-2002 update
    Dayam, R
    Neamati, N
    CURRENT PHARMACEUTICAL DESIGN, 2003, 9 (22) : 1789 - 1802
  • [50] Small-molecule inhibitors as potential therapeutics and as tools to understand the role of phospholipases A2
    Nikolaou, Aikaterini
    Kokotou, Maroula G.
    Vasilakaki, Sofia
    Kokotos, George
    BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS, 2019, 1864 (06): : 941 - 956
12345