Literature DB >> 32048880

Recent development in acetyl-CoA carboxylase inhibitors and their potential as novel drugs.

Xin Wu1, Tonghui Huang1.   

Abstract

Acetyl-CoA carboxylase (ACC), a critical enzyme in the regulation of fatty acid synthesis and metabolism, has emerged as an attractive target for a plethora of emerging diseases, such as diabetes mellitus, nonalcoholic fatty liver disease, cancer, bacterial infections and so on. With decades of efforts in medicinal chemistry, significant progress has been made toward the design and discovery of a considerable number of inhibitors of this enzyme. In this review, we not only clarify the role of ACC in emerging diseases, but also summarize recent developments of potent ACC inhibitors and discuss their molecular mechanisms of action and potentials as novel drugs as well as future perspectives toward the design and discovery of novel ACC inhibitors.

Entities:  

Keywords:  acetyl-CoA carboxylase; bacterial infections; cancer; crystal structure; fatty acid; metabolic diseases

Mesh:

Substances:

Year:  2020        PMID: 32048880     DOI: 10.4155/fmc-2019-0312

Source DB:  PubMed          Journal:  Future Med Chem        ISSN: 1756-8919            Impact factor:   3.808


  5 in total

1.  Mechanism and therapeutic strategy of hepatic TM6SF2-deficient non-alcoholic fatty liver diseases via in vivo and in vitro experiments.

Authors:  Zu-Yin Li; Gang Wu; Chen Qiu; Zhi-Jie Zhou; Yu-Peng Wang; Guo-He Song; Chao Xiao; Xin Zhang; Gui-Long Deng; Rui-Tao Wang; Yu-Long Yang; Xiao-Liang Wang
Journal:  World J Gastroenterol       Date:  2022-07-07       Impact factor: 5.374

2.  Synthesis and biological evaluation of 4-phenoxy-phenyl isoxazoles as novel acetyl-CoA carboxylase inhibitors.

Authors:  Xin Wu; Yongbo Yu; Tonghui Huang
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

3.  Inhibition of fatty acid synthase with FT-4101 safely reduces hepatic de novo lipogenesis and steatosis in obese subjects with non-alcoholic fatty liver disease: Results from two early-phase randomized trials.

Authors:  Carine Beysen; Patricia Schroeder; Eric Wu; Julie Brevard; Maria Ribadeneira; Wei Lu; Kiran Dole; Terry O'Reilly; Linda Morrow; Marcus Hompesch; Marc K Hellerstein; Kelvin Li; Lars Johansson; Patrick F Kelly
Journal:  Diabetes Obes Metab       Date:  2020-12-21       Impact factor: 6.577

4.  Acetyl-CoA Carboxylase Inhibitor CP640.186 Increases Tubulin Acetylation and Impairs Thrombin-Induced Platelet Aggregation.

Authors:  Marie Octave; Laurence Pirotton; Audrey Ginion; Valentine Robaux; Sophie Lepropre; Jérôme Ambroise; Caroline Bouzin; Bruno Guigas; Martin Giera; Marc Foretz; Luc Bertrand; Christophe Beauloye; Sandrine Horman
Journal:  Int J Mol Sci       Date:  2021-12-04       Impact factor: 5.923

5.  Fatty Acid Synthase Inhibitor Platensimycin Intervenes the Development of Nonalcoholic Fatty Liver Disease in a Mouse Model.

Authors:  Meng Su; Danfeng Cao; Zhe Wang; Yanwen Duan; Yong Huang
Journal:  Biomedicines       Date:  2021-12-21
  5 in total

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