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First-in-class small molecule inhibitors of the single-strand DNA cytosine deaminase APOBEC3G.
A structural model is presented in which the mechanism of inhibition is both specific and competitive, by binding a pocket adjacent to the APOBEC3G active site, reacting with C321, and blocking access to substrate DNA cytosines.
Rapid screening of fermentation broths for flavones using tandem mass spectrometry
Fermentation broth extracts were rapidly screened for the presence of daidzein and genistein with an approach utilizing the desorption chemical ionization (DCI) and thermospray (TS) ionization modes
Integrated biological-physicochemical system for the identification of antitumor compounds in fermentation broths.
A rapid, integrated biological-physicochemical system for the identification of six major classes of antitumor compounds in fermentation broths is described. The system relies upon preliminary
Approaches to Automating the Dereplication of Bioactive Natural Products—The Key Step in High Throughput Screening of Bioactive Materials From Natural Sources
The effective use of automated procedures and databases in the isolation, identification and biological profiling of bioactive compounds will be described and the potential of new technologies to enhance this process will be discussed as well as the possible reintroduction of TLC as a parallel dereplication method.
A Cell-Free Fluorometric High-Throughput Screen for Inhibitors of Rtt109-Catalyzed Histone Acetylation
The development and optimization of a cell-free fluorometric high-throughput screen (HTS) for small-molecule inhibitors of Rtt109-catalyzed histone acetylation and its applications could serve as chemical probes or leads for a new class of antifungals targeting an epigenetic enzyme.
Functional Protein Microarrays in Drug Discovery
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The Fungal Sexual Pheromone Sirenin Activates the Human CatSper Channel Complex
Based on this proficient synthetic route and confirmed activation of CatSper, analogues of sirenin can be designed as blockers of the CatSar channel that could provide male contraceptive agents.
Biosynthesis of the antibiotic 2,5-dihydrophenylalanine by Streptomyces arenae.
By preparing and feeding 5,6-dihydro[4-3H]prephenate it was shown that this compound is not an intermediate in the biosynthesis of DHPA and a reaction sequence is proposed for the conversion of prephenate to DHPA, involving an allylic rearrangement and a combined decarboxylation/dehydration.
Human Adenine Nucleotide Translocase (ANT) Modulators Identified by High-Throughput Screening of Transgenic Yeast
A novel yeast-based high-throughput screening (HTS) strategy to identify compounds inhibiting the function of ANT, finding closantel and CD437 were identified as broad-spectrum ANT inhibitors, whereas leelamine was found to be a modulator of AnT function.
Stimulation of the conversion of penicillin N to cephalosporin by ascorbic acid, alpha-ketoglutarate, and ferrous ions in cell-free extracts of strains of Cephalosporium acremonium.
It is shown that the activity was lost upon boiling, indicating the reaction is enzymatic in nature, and the production of the cephalosporin-like material was stimulated by the addition of ascorbic acid and ferrous ions, components which are co-factors in monooxygenase and dioxygenase reactions.