Lipogenesis inhibitors: therapeutic opportunities and challenges

B Batchuluun, SL Pinkosky, GR Steinberg - Nature Reviews Drug …, 2022 - nature.com
Fatty acids are essential for survival, acting as bioenergetic substrates, structural
components and signalling molecules. Given their vital role, cells have evolved mechanisms …

Animal fatty acid synthase: a chemical nanofactory

P Paiva, FE Medina, M Viegas, P Ferreira… - Chemical …, 2021 - ACS Publications
Fatty acids are crucial molecules for most living beings, very well spread and conserved
across species. These molecules play a role in energy storage, cell membrane architecture …

Fatty acid biosynthesis: chain‐length regulation and control

CS Heil, SS Wehrheim, KS Paithankar… - …, 2019 - Wiley Online Library
De novo biosynthesis of fatty acids is an iterative process requiring strict regulation of the
lengths of the produced fatty acids. In this review, we focus on the factors determining chain …

Activity-based proteome profiling of potential cellular targets of orlistat− an FDA-approved drug with anti-tumor activities

PY Yang, K Liu, MH Ngai, MJ Lear… - Journal of the …, 2010 - ACS Publications
Orlistat, or tetrahydrolipstatin (THL), is an FDA-approved antiobesity drug with potential
antitumor activities. Cellular off-targets and potential side effects of Orlistat in cancer …

The lipogenesis pathway as a cancer target

HN Abramson - Journal of medicinal chemistry, 2011 - ACS Publications
Lipids constitute some of nature's most abundant molecules, being found in virtually all
forms of life. They are derived by condensation reactions involving acetate units and may be …

Recent advances in targeting the fatty acid biosynthetic pathway using fatty acid synthase inhibitors

TS Angeles, RL Hudkins - Expert opinion on drug discovery, 2016 - Taylor & Francis
Introduction: Elevated lipogenesis has been associated with a variety of diseases including
obesity, cancer and nonalcoholic fatty liver disease (NAFLD). Fatty acid synthase (FASN) …

[HTML][HTML] Biochemistry, molecular biology, and pharmacology of fatty acid synthase, an emerging therapeutic target and diagnosis/prognosis marker

H Liu, JY Liu, X Wu, JT Zhang - International journal of biochemistry …, 2010 - ncbi.nlm.nih.gov
Human fatty acid synthase (FASN) is a 270-kDa cytosolic dimeric enzyme that is responsible
for palmitate synthesis. FASN is slowly emerging and rediscovered as a marker for …

Peptides from purified soybean β‐conglycinin inhibit fatty acid synthase by interaction with the thioesterase catalytic domain

C Martinez‐Villaluenga, SG Rupasinghe… - The FEBS …, 2010 - Wiley Online Library
Fatty acid synthase (FAS) is uniquely expressed at high levels in cancer cells and adipose
tissue. The objectives of this study were to identify, purify and validate soy FAS inhibitory …

Type I fatty acid synthase trapped in the octanoyl‐bound state

A Rittner, KS Paithankar, A Himmler… - Protein science, 2020 - Wiley Online Library
De novo fatty acid biosynthesis in humans is accomplished by a multidomain protein, the
Type I fatty acid synthase (FAS). Although ubiquitously expressed in all tissues, fatty acid …

Targeting lipid esterases in mycobacteria grown under different physiological conditions using activity-based profiling with tetrahydrolipstatin (THL)

MS Ravindran, SPS Rao, X Cheng, A Shukla… - Molecular & cellular …, 2014 - ASBMB
Tetrahydrolipstatin (THL) is bactericidal but its precise target spectrum is poorly
characterized. Here, we used a THL analog and activity-based protein profiling to identify …