Lipogenesis inhibitors: therapeutic opportunities and challenges Journal Articles

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 entered clinical-stage development and may become the foundation for a new class of therapeutics.

authors

• Batchuluun, Battsetseg
• Pinkosky, Stephen L
• Steinberg, Gregory

status

• published 

publication date

• April 2022

has subject area

• 06 Biological Sciences (FoR)
• 11 Medical and Health Sciences (FoR)
• ATP Citrate (pro-S)-Lyase (MeSH)
• Acetyl-CoA Carboxylase (MeSH)
• Fatty Acids (MeSH)
• Humans (MeSH)
• Lipogenesis (MeSH)
• Pharmacology & Pharmacy (Science Metrix)
• Signal Transduction (MeSH)

published in

• Nature Reviews Drug Discovery  Journal

keywords

• ATP Citrate (pro-S)-Lyase
• Acetyl-CoA Carboxylase
• Fatty Acids
• Humans
• Lipogenesis
• Signal Transduction

Digital Object Identifier (DOI)

• 10.1038/s41573-021-00367-2

start page

• 283

end page

• 305

volume

• 21

issue

• 4