ArticleProceedings of the National Academy of Sciences of the United States of America2010
Recombinant yeast screen for new inhibitors of human acetyl-CoA carboxylase 2 identifies potential drugs to treat obesity.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 31 citations in OpenAlex.
- Expression of Yarrowia lipolytica acetyl-CoA carboxylase in Saccharomyces cerevisiae and its effect on in-vivo accumulation of Malonyl-CoA.Computational and structural biotechnology journal · 2022Article
- Cross-Species Complementation of Nonessential Yeast Genes Establishes Platforms for Testing Inhibitors of Human Proteins.Genetics · 2020Article
- Yeast as a tool to identify anti-aging compounds.FEMS yeast research · 2018Review
- Distinct role of nuclear receptor corepressor 1 regulated de novo fatty acids synthesis in liver regeneration and hepatocarcinogenesis in mice.Hepatology (Baltimore, Md.) · 2018Article
- Analysis of Arabidopsis Accessions Hypersensitive to a Loss of Chloroplast Translation.Plant physiology · 2016Article
- A novel approach to the discovery of anti-tumor pharmaceuticals: searching for activators of liponecrosis.Oncotarget · 2016Review
- Identification of an aminothiazole with antifungal activity against intracellular Histoplasma capsulatum.Antimicrobial agents and chemotherapy · 2013Article
- The effects of statins on the mevalonic acid pathway in recombinant yeast strains expressing human HMG-CoA reductase.BMC biotechnology · 2013Article
- Structure and function of biotin-dependent carboxylases.Cellular and molecular life sciences : CMLS · 2013Review
- Yeast-based automated high-throughput screens to identify anti-parasitic lead compounds.Open biology · 2013Article
- Yeast toxicogenomics: genome-wide responses to chemical stresses with impact in environmental health, pharmacology, and biotechnology.Frontiers in genetics · 2012Article
- Functional expression of parasite drug targets and their human orthologs in yeast.PLoS neglected tropical diseases · 2011Article
Corrections and comments
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Authors and funding
12 authors at 2 institutions in 1 country.
Funding
Abstract
Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism with multiple isozymes often expressed in different eukaryotic cellular compartments. ACC-made malonyl-CoA serves as a precursor for fatty acids; it also regulates fatty acid oxidation and feeding behavior in animals. ACC provides an important target for new drugs to treat human diseases. We have developed an inexpensive nonradioactive high-throughput screening system to identify new ACC inhibitors. The screen uses yeast gene-replacement strains depending for growth on cloned human ACC1 and ACC2. In "proof of concept" experiments, growth of such strains was inhibited by compounds known to target human ACCs. The screen is sensitive and robust. Medium-size chemical libraries yielded new specific inhibitors of human ACC2. The target of the best of these inhibitors was confirmed with in vitro enzymatic assays. This compound is a new drug chemotype inhibiting human ACC2 with 2.8 muM IC(50) and having no effect on human ACC1 at 100 muM.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.