First-in-class small molecule inhibitors of the single-strand DNA cytosine deaminase APOBEC3G.
- Ming Li, S. Shandilya, R. Harris
- Biology, ChemistryACS Chemical Biology
- 16 March 2012
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
- Mike S. Lee, D. Hook, E. Kerns, K. Volk, I. E. Rosenberg
- Chemistry
- 1993
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.
- D. Hook, C. More, J. J. Yacobucci, G. Dubay, S. O'Connor
- ChemistryJournal of Chromatography A
- 9 January 1987
Identification of Novel Non-Hydroxamate Anthrax Toxin Lethal Factor Inhibitors by Topomeric Searching, Docking and Scoring, and in Vitro Screening
- Ting-Lan Chiu, J. Solberg, Elizabeth A. Amin
- Biology, ChemistryJournal of Chemical Information and Modeling
- 20 November 2009
It is found that micromolar-level LF inhibition can be attained by compounds with non-hydroxamate zinc-binding groups that exhibit monodentate zinc chelation as long as key hydrophobic interactions with at least two LF subsites are retained.
Approaches to Automating the Dereplication of Bioactive Natural Products—The Key Step in High Throughput Screening of Bioactive Materials From Natural Sources
- D. Hook, E. Pack, J. J. Yacobucci, J. Guss
- Biology, Chemistry
- 1 April 1997
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
- Jayme L. Dahlin, Rondedrick Sinville, Zhiguo Zhang
- Biology, ChemistryPLoS ONE
- 18 November 2013
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
- D. Hook
- Medicine, Biology
- 1 April 2008
If you know are looking for the book enPDFd functional protein microarrays in drug discovery as the choice of reading, you can find here.
The Fungal Sexual Pheromone Sirenin Activates the Human CatSper Channel Complex
- S. S. Syeda, Erick J Carlson, G. Georg
- BiologyACS Chemical Biology
- 16 December 2015
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.
- K. Shimada, D. Hook, G. Warner, H. Floss
- Chemistry, BiologyBiochemistry
- 25 July 1978
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
- Yujian Zhang, Defeng Tian, J. Hawkinson
- BiologyJournal of biomolecular screening
- 8 January 2016
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.
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