法尼醇X受体及其激动剂与肝脏疾病

被引：8

作者：

贾锶琦

窦晓光

机构：

[1] 中国医科大学附属盛京医院感染科

来源：

肝脏 | 2021年 / 26卷 / 11期

关键词：

法尼醇X受体; FXR激动剂; 肝脏代谢性疾病;

D O I：

10.14000/j.cnki.issn.1008-1704.2021.11.028

中图分类号：

R575 [肝及胆疾病];

学科分类号：

100201 [内科学];

摘要：

法尼醇X受体(farnesoid X receptor,FXR)又名胆汁酸受体,是一种配体激活转录因子。FXR激动剂作用于FXR后,激活一系列复杂的下游通路,其代谢产物参与调节胆汁酸、糖类、脂质的稳态,进而在肝脏组织炎症、纤维化、再生及癌变过程中起到重要的调节作用,影响肝脏代谢性疾病的发生发展。寻找治疗靶点更精确且高效低毒的FXR激动剂,治疗肝脏代谢性疾病是当前的研究热点。本文将主要围绕FXR对代谢的调节及其与肝脏疾病的关系及其激动剂的研究进展进行讨论。

引用

页码：1293 / 1297

页数：5

共 18 条

[1]

Liver Injury in Patients With Cholestatic Liver Disease Treated With Obeticholic Acid [J].

Eaton, John E. ;

Vuppalanchi, Raj ;

Reddy, Rajender ;

Sathapathy, Sanjaya ;

Ali, Bilal ;

Kamath, Patrick S. .

HEPATOLOGY, 2020, 71 (04) :1511-1514

[2]

Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel Non-Bile Acid FXR Agonist Tropifexor (LJN452) in Healthy Volunteers [J].

Badman, Michael K. ;

Chen, Jin ;

Desai, Sachin ;

Vaidya, Soniya ;

Neelakantham, Srikanth ;

Zhang, Jie ;

Gan, Lu ;

Danis, Kate ;

Laffitte, Bryan ;

Klickstein, Lloyd B. .

CLINICAL PHARMACOLOGY IN DRUG DEVELOPMENT, 2020, 9 (03) :395-410

[3]

Cilofexor, a NonsteroidalFXRAgonist, in Patients With Noncirrhotic NASH: A Phase 2 Randomized Controlled Trial [J].

Patel, Keyur ;

Harrison, Stephen A. ;

Elkhashab, Magdy ;

Trotter, James F. ;

Herring, Robert ;

Rojter, Sergio E. ;

Kayali, Zeid ;

Wong, Vincent Wai-Sun ;

Greenbloom, Susan ;

Jayakumar, Saumya ;

Shiffman, Mitchell L. ;

Freilich, Bradley ;

Lawitz, Eric J. ;

Gane, Edward J. ;

Harting, Eliza ;

Xu, Jun ;

Billin, Andrew N. ;

Chung, Chuhan ;

Djedjos, C. Stephen ;

Subramanian, G. Mani ;

Myers, Robert P. ;

Middleton, Michael S. ;

Rinella, Mary ;

Noureddin, Mazen .

HEPATOLOGY, 2020, 72 (01) :58-71

[4]

Bile Acid-Activated Receptors: A Review on FXR and Other Nuclear Receptors..[J].Shin Dong-Ju;Wang Li.Handbook of experimental pharmacology.2019,

[5]

Improvements in Histologic Features and Diagnosis Associated With Improvement in Fibrosis in Nonalcoholic Steatohepatitis: Results From the Nonalcoholic Steatohepatitis Clinical Research Network Treatment Trials [J].

Brunt, Elizabeth M. ;

Kleiner, David E. ;

Wilson, Laura A. ;

Sanyal, Arun J. ;

Neuschwander-Tetri, Brent A. .

HEPATOLOGY, 2019, 70 (02) :522-531

[6]

Bile Acids Activated Receptors Regulate innate immunity [J].

Fiorucci, Stefano ;

Biagioli, Michele ;

Zampella, Angela ;

Distrutti, Eleonora .

FRONTIERS IN IMMUNOLOGY, 2018, 9

[7]

Glucagon Receptor Signaling Regulates Energy Metabolism via Hepatic Farnesoid X Receptor and Fibroblast Growth Factor 21 [J].

Kim, Teayoun ;

Nason, Shelly ;

Holleman, Cassie ;

Pepin, Mark ;

Wilson, Landon ;

Berryhill, Taylor F. ;

Wende, Adam R. ;

Steele, Chad ;

Young, Martin E. ;

Barnes, Stephen ;

Drucker, Daniel J. ;

Finan, Brian ;

DiMarchi, Richard ;

Perez-Tilve, Diego ;

Tschoep, Matthias ;

Habegger, Kirk M. .

DIABETES, 2018, 67 (09) :1773-1782

[8]

Current Prevention and Treatment Options for NAFLD..[J].Wong Vincent Wai-Sun.Advances in experimental medicine and biology.2018,

[9]

Disruption of TFGβ-SMAD3 pathway by the nuclear receptor SHP mediates the antifibrotic activities of BAR704; a novel highly selective FXR ligand.[J].Adriana Carino;Michele Biagioli;Silvia Marchianò;Paolo Scarpelli;Angela Zampella;Vittorio Limongelli;Stefano Fiorucci.Pharmacological Research.2018,

[10]

Allosteric modulation of the farnesoid X receptor by a small molecule [J].

Gabler, Matthias ;

Kramer, Jan ;

Schmidt, Jurema ;

Pollinger, Julius ;

Weber, Julia ;

Kaiser, Astrid ;

Loehr, Frank ;

Proschak, Ewgenij ;

Schubert-Zsilavecz, Manfred ;

Merk, Daniel .

SCIENTIFIC REPORTS, 2018, 8

← 1 2 →