Lipogenesis inhibitors: therapeutic opportunities and challenges
McMaster University · Esperion Therapeutics (United States) · +1 more institution
Abstract
Fatty acids are essential for survival, acting as bioenergetic substrates, structural components and signalling molecules. Given their vital role, cells have evolved mechanisms to generate fatty acids from alternative carbon sources, through a process known as de novo lipogenesis (DNL). Despite the importance of DNL, aberrant upregulation is associated with a wide variety of pathologies. Inhibiting core enzymes of DNL, including citrate/isocitrate carrier (CIC), ATP-citrate lyase (ACLY), acetyl-CoA carboxylase (ACC) and fatty acid synthase (FAS), represents an attractive therapeutic strategy. Despite challenges related to efficacy, selectivity and safety, several new classes of synthetic DNL inhibitors have…
Citation impact
- FWCI
- 33.13
- Percentile
- 100%
- References
- 304
Authors
3Topics & keywords
- Lipogenesis
- ATP citrate lyase
- Fatty acid synthase
- Fatty acid synthesis
- Lyase
- Biochemistry
- Acetyl-CoA carboxylase
- Small molecule
- Clean water and sanitation