Development of 11β-HSD1 inhibitors for the treatment of type 2 diabetes

被引：31
|
作者：
Hale, Clarence [1 ]
Wang, Minghan [1 ]
机构：
[1] Amgen Inc, Dept Metab Disorders, Thousand Oaks, CA 91320 USA
来源：
MINI-REVIEWS IN MEDICINAL CHEMISTRY | 2008年 / 8卷 / 07期
关键词：
11 beta-hydroxysteroid dehydrogenase; glucocorticoid receptor; cortisol; ex vivo activity; insulin resistance; Cushing's syndrome;
D O I：
10.2174/138955708784567421
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Glucocorticoid action is linked to the development of obesity and insulin resistance. Inhibition of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) has been proposed as a strategy to suppress glucocorticoid action in a tissue-specific manner. A large variety of 11 beta-HSD1 inhibitor classes are under investigation by the pharmaceutical industry to treat type 2 diabetes and obesity.
引用
收藏
页码：702 / 710
页数：9
相关论文
共 50 条
  • [1] 11β-HSD1 Inhibitors for the Treatment of Type 2 Diabetes and Cardiovascular Disease
    Anna Anderson
    Brian R. Walker
    Drugs, 2013, 73 : 1385 - 1393
  • [2] Inhibitors of 11β-HSD1: A Potential Treatment for the Metabolic Syndrome
    Jean, David J. St., Jr.
    Wang, Minghan
    Fotsch, Christopher
    CURRENT TOPICS IN MEDICINAL CHEMISTRY, 2008, 8 (17) : 1508 - 1523
  • [3] Discovery of Adamantyl Ethanone Derivatives as Potent 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors
    Su, Xiangdong
    Pradaux-Caggiano, Fabienne
    Thomas, Mark P.
    Szeto, Michelle W. Y.
    Halem, Heather A.
    Culler, Michael D.
    Vicker, Nigel
    Potter, Barry V. L.
    CHEMMEDCHEM, 2010, 5 (07) : 1026 - 1044
  • [4] Structure Based Design of 11β-HSD1 Inhibitors
    Singh, Suresh B.
    Tice, Colin M.
    CURRENT PHARMACEUTICAL BIOTECHNOLOGY, 2010, 11 (07) : 779 - 791
  • [5] Synthesis of selective 11β-HSD1 inhibitors based on dammarane scaffold
    Shao, Li-Dong
    Bao, Ying
    Shen, Yu
    Su, Jia
    Leng, Ying
    Zhao, Qin-Shi
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2017, 135 : 324 - 338
  • [6] Interplay between H6PDH and 11β-HSD1 implicated in the pathogenesis of type 2 diabetes
    Yao, Fan
    Chen, Li
    Fan, Zheng
    Teng, Fei
    Zhao, Yali
    Guan, Fengying
    Zhang, Ming
    Liu, Yanjun
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2017, 27 (17) : 4107 - 4113
  • [7] The discovery of azepane sulfonamides as potent 11β-HSD1 inhibitors
    Neelamkavil, Santhosh F.
    Boyle, Craig D.
    Chackalamannil, Samuel
    Greenlee, William J.
    Zhang, Lili
    Terracina, Giuseppe
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (16) : 4563 - 4565
  • [8] Identification and optimisation of 3,3-dimethylazetidin-2-ones as potent and selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1)
    McCoull, William
    Augustin, Martin
    Blake, Caroline
    Ertan, Anne
    Kilgour, Elaine
    Krapp, Stephan
    Moore, Jane E.
    Newcombe, Nicholas J.
    Packer, Martin J.
    Rees, Amanda
    Revill, John
    Scott, James S.
    Selmi, Nidhal
    Gerhardt, Stefan
    Ogg, Derek J.
    Steinbacher, Stefan
    Whittamore, Paul R. O.
    MEDCHEMCOMM, 2014, 5 (01) : 57 - 63
  • [9] Antidiabetic effects of 11β-HSD1 inhibition in a mouse model of combined diabetes, dyslipidaemia and atherosclerosis
    Lloyd, D. J.
    Helmering, J.
    Cordover, D.
    Bowsman, M.
    Chen, M.
    Hale, C.
    Fordstrom, P.
    Zhou, M.
    Wang, M.
    Kaufman, S. A.
    Veniant, M. M.
    DIABETES OBESITY & METABOLISM, 2009, 11 (07) : 688 - 699
  • [10] Inhibition of 11β-HSD1 by LG13 improves glucose metabolism in type 2 diabetic mice
    Zhao, Leping
    Pan, Yong
    Peng, Kesong
    Wang, Zhe
    Li, Jieli
    Li, Dan
    Tong, Chao
    Wang, Yi
    Liang, Guang
    JOURNAL OF MOLECULAR ENDOCRINOLOGY, 2015, 55 (02) : 119 - 131
12345