ArticleAnalytical biochemistry2011
Application of a high-throughput fluorescent acetyltransferase assay to identify inhibitors of homocitrate synthase.
Article in Analytical biochemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
What it found
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
7 citing papers in PubMed, 10 citations in OpenAlex.
- Chemoproteomics Yields a Selective Molecular Host for Acetyl-CoA.Journal of the American Chemical Society · 2023Article
- New Therapeutic Candidates for the Treatment of Malassezia pachydermatis -Associated Infections.Scientific reports · 2020Article
- In Vitro Activity Assays for MYST Histone Acetyltransferases and Adaptation for High-Throughput Inhibitor Screening.Methods in enzymology · 2016Article
- PAINS in the assay: chemical mechanisms of assay interference and promiscuous enzymatic inhibition observed during a sulfhydryl-scavenging HTS.Journal of medicinal chemistry · 2015Article
- Comparative studies of thiol-sensitive fluorogenic probes for HAT assays.Analytical and bioanalytical chemistry · 2013Article
- A cell-free fluorometric high-throughput screen for inhibitors of Rtt109-catalyzed histone acetylation.PloS one · 2013Article
- A continuous fluorescent enzyme assay for early steps of lipid A biosynthesis.Analytical biochemistry · 2012Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Homocitrate synthase (HCS) catalyzes the first step of l-lysine biosynthesis in fungi by condensing acetyl-coenzyme A and 2-oxoglutarate to form 3R-homocitrate and coenzyme A. Due to its conservation in pathogenic fungi, HCS has been proposed as a candidate for antifungal drug design. Here we report the development and validation of a robust fluorescent assay for HCS that is amenable to high-throughput screening for inhibitors in vitro. Using this assay, Schizosaccharomyces pombe HCS was screened against a diverse library of approximately 41,000 small molecules. Following confirmation, counter screens, and dose-response analysis, we prioritized more than 100 compounds for further in vitro and in vivo analysis. This assay can be readily adapted to screen for small molecule modulators of other acyl-CoA-dependent acyltransferases or enzymes that generate a product with a free sulfhydryl group, including histone acetyltransferases, aminoglycoside N-acetyltransferases, thioesterases, and enzymes involved in lipid metabolism.
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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.