Identification of nonabsorbable inhibitors of the scavenger receptor-BI (SR-BI) for tissue-specific administration

被引：5
|
作者：
Sparks, Steven M.
Zhou, Huiqiang
Generaux, Claudia
Harston, Lindsey
Moncol, David
Jayawickreme, Channa
Parham, Janet
Condreay, Patrick
Rimele, Thomas
机构：
[1] GlaxoSmithKline, Enteroendocrine Discovery Performance Unit, 5 Moore Dr, Res Triangle Pk, NC 27709 USA
[2] GlaxoSmithKline, Platform Technol & Sci, 5 Moore Dr, Res Triangle Pk, NC 27709 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 08期
关键词：
Scavenger receptor class B type I; SR-BI inhibitor; Nonabsorbed SR-BI inhibitor; Intestinal SR-BI; HIGHLY POTENT; CHOLESTEROL; DISCOVERY; ENTRY; ABSORPTION; TRANSPORT; LIPIDS; CD36;
D O I：
10.1016/j.bmcl.2016.03.025
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The identification of a low-permeability scavenger receptor BI (SR-BI) inhibitor starting from the ITX-5061 template is described. Structure-activity and structure-permeability relationships were assessed for analogs leading to the identification of compound 8 as a potent and nonabsorbable SR-BI inhibitor. (C) 2016 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1901 / 1904
页数：4
相关论文
共 50 条
  • [31] Oxidized LDL decreases macrophage expression of scavenger receptor B-I (SR-BI).
    Han, J
    Hajjar, DP
    Feng, J
    Scott, LD
    Zhou, X
    Gotto, AM
    Nicholson, AC
    FASEB JOURNAL, 2000, 14 (04): : A453 - A453
  • [32] Expression of the Scavenger Receptor Class B type I (SR-BI) family in Drosophila melanogaster
    Herboso, Leire
    Talamillo, Ana
    Perez, Coralia
    Barrio, Rosa
    INTERNATIONAL JOURNAL OF DEVELOPMENTAL BIOLOGY, 2011, 55 (06): : 603 - 611
  • [33] Statins increase expression of macrophage scavenger receptor class B type I (SR-BI)
    Nicholson, AC
    Han, JH
    Zhou, XY
    Parsons, M
    Gotto, AM
    Hajjar, DP
    FASEB JOURNAL, 2004, 18 (04): : A12 - A12
  • [34] Benzo-fused lactams from a diversity-oriented synthesis (DOS) library as inhibitors of scavenger receptor BI (SR-BI)-mediated lipid uptake
    Dockendorff, Chris
    Faloon, Patrick W.
    Pu, Jun
    Yu, Miao
    Johnston, Stephen
    Bennion, Melissa
    Penman, Marsha
    Nieland, Thomas J. F.
    Dandapani, Sivaraman
    Perez, Jose R.
    Munoz, Benito
    Palmer, Michelle A.
    Schreiber, Stuart L.
    Krieger, Monty
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2015, 25 (10) : 2100 - 2105
  • [35] Scavenger receptor class BI (SR-BI) mediates uptake of CPX-351 into K562 leukemia cells
    Di, Yunyun
    Wasan, Ellen K.
    Cawthray, Jacqueline
    Wasan, Kishor M.
    DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2019, 45 (01) : 21 - 26
  • [36] Functional role and regulation of hepatic scavenger receptor class B type I (SR-BI)
    Rigotti, A
    ATHEROSCLEROSIS SUPPLEMENTS, 2003, 4 (02) : 191 - 192
  • [37] Consequences of over-expression of rat Scavenger Receptor, SR-BI, in an adrenal cell model
    Eve Reaven
    Ann Nomoto
    Yuan Cortez
    Salman Azhar
    Nutrition & Metabolism, 3
  • [38] SR-BI (Scavenger Receptor BI), Not LDL (Low-Density Lipoprotein) Receptor, Mediates Adrenal Stress Response-Brief Report
    Ito, Misa
    Ye, Xiang
    Wang, Qian
    Guo, Ling
    Hao, Dan
    Howatt, Deborah
    Daugherty, Alan
    Cai, Lei
    Temel, Ryan
    Li, Xiang-An
    ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY, 2020, 40 (08) : 1830 - 1837
  • [39] Scavenger receptor class B type I (SR-BI) in Ruditapes philippinarum: A versatile receptor with multiple functions
    Yang, Dinglong
    Han, Yijing
    Chen, Lizhu
    Liu, Yongliang
    Cao, Ruiwen
    Wang, Qing
    Zhao, Jianmin
    FISH & SHELLFISH IMMUNOLOGY, 2019, 88 : 328 - 334
  • [40] Aspirin influences expression and function of scavenger receptor-BI in primary human macrophages
    Tancevski, I
    Wehinger, A
    Schgoer, W
    Eller, P
    Foeger, B
    Patsch, J
    Ritsch, A
    CIRCULATION, 2005, 112 (17) : U343 - U343
12345