High Throughput Screening Laboratory Scholarly Works

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Recent Submissions

  • Discovery of small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase 

    Kaur, Supreet; Nieto, Nicholas S.; McDonald, Peter; Beck, Josh R.; Honzatko, Richard B.; Roy, Anuradha; Nelson, Scott W. (Taylor & Francis Open Access, 2022-05-05)
    Malaria is caused by infection with protozoan parasites of the Plasmodium genus, which is part of the phylum Apicomplexa. Most organisms in this phylum contain a relic plastid called the apicoplast. The apicoplast genome ...

  • Overcoming Wnt–β-catenin dependent anticancer therapy resistance in leukaemia stem cells 

    Perry, John M.; Tao, Fang; Roy, Anuradha; Lin, Tara; He, Xi C.; Chen, Shiyuan; Lu, Xiuling; Nemechek, Jacqelyn; Ruan, Linhao; Yu, Xiazhen; Dukes, Debra; Moran, Andrea; Pace, Jennifer; Schroeder, Kealan; Zhao, Meng; Venkatraman, Aparna; Qian, Pengxu; Li, Zhenrui; Hembree, Mark; Paulson, Ariel; He, Zhiquan; Xu, Dong; Tran, Thanh-Huyen; Deshmukh, Prashant; Nguyen, Chi Thanh; Kasi, Rajeswari M.; Ryan, Robin; Broward, Melinda; Ding, Sheng; Guest, Erin; August, Keith; Gamis, Alan S.; Godwin, Andrew; Sittampalam, G. Sitta; Weir, Scott J.; Li, Linheng (Nature Research, 2020-04-20)
    Leukaemia stem cells (LSCs) underlie cancer therapy resistance but targeting these cells remains difficult. The Wnt–β-catenin and PI3K–Akt pathways cooperate to promote tumorigenesis and resistance to therapy. In a mouse ...

  • YM155 Inhibits NleB and SseK Arginine Glycosyltransferase Activity 

    Zhu, Congrui; El Qaidi, Samir; McDonald, Peter; Roy, Anuradha; Hardwidge, Philip R. (MDPI, 2021-02-23)
    The type III secretion system effector proteins NleB and SseK are glycosyltransferases that glycosylate protein substrates on arginine residues. We conducted high-throughput screening assays on 42,498 compounds to identify ...

  • Repurposing p97 inhibitors for chemical modulation of the bacterial ClpB–DnaK bichaperone system 

    Glaza, Przemyslaw; Ranaweera, Chathurange B.; Shiva, Sunitha; Roy, Anuradha; Geisbrecht, Brian V.; Schoenen, Frank J.; Zolkiewski, Michal (Elsevier, 2020-11-13)
    The ClpB–DnaK bichaperone system reactivates aggregated cellular proteins and is essential for survival of bacteria, fungi, protozoa, and plants under stress. AAA+ ATPase ClpB is a promising target for the development of ...

  • High-Throughput Screening for Bacterial Glycosyltransferase Inhibitors 

    El Qaidi, Samir; Zhu, Congrui; McDonald, Peter; Roy, Anuradha; Maity, Pradip Kumar; Rane, Digamber; Perera, Chamani; Hardwidge, Philip R. (Frontiers Media, 2018-12-18)
    The enteropathogenic and enterohemorrhagic Escherichia coli NleB proteins as well as the Salmonella enterica SseK proteins are type III secretion system effectors that function as glycosyltransferase enzymes to ...

  • Identification and Validation of an Aspergillus nidulans Secondary Metabolite Derivative as an Inhibitor of the Musashi-RNA Interaction 

    Lan, Lan; Liu, Jiajun; Xing, Minli; Smith, Amber R.; Wang, Jinan; Wu, Xiaoqing; Appelman, Carl; Li, Ke; Roy, Anuradha; Gowthaman, Ragul; Karanicolas, John; Somoza, Amber D.; Wang, Clay C. C.; Miao, Yinglong; Guzman, Roberto De; Oakley, Berl R.; Neufeld, Kristi L.; Xu, Liang (Wiley, 2020-08-08)
    RNA-binding protein Musashi-1 (MSI1) is a key regulator of several stem cell populations. MSI1 is involved in tumor proliferation and maintenance, and it regulates target mRNAs at the translational level. The known mRNA ...

  • Cooperative p16 and p21 action protects female astrocytes from transformation 

    Kfoury, Najla; Sun, Tao; Yu, Kwanha; Rockwell, Nathan; Tinkum, Kelsey L.; Qi, Zongtai; Warrington, Nicole M.; McDonald, Peter R.; Roy, Anuradha; Weir, Scott J.; Mohila, Carrie A.; Deneen, Benjamin; Rubin, Joshua B. (BioMed Central, 2018-02-20)
    Mechanisms underlying sex differences in cancer incidence are not defined but likely involve dimorphism (s) in tumor suppressor function at the cellular and organismal levels. As an example, sexual dimorphism in retinoblastoma ...

  • Early Probe and Drug Discovery in Academia: A Minireview 

    Roy, Anuradha (MDPI, 2018-02-09)
    Drug discovery encompasses processes ranging from target selection and validation to the selection of a development candidate. While comprehensive drug discovery work flows are implemented predominantly in the big pharma ...

  • Comparative oncology approach to drug repurposing in osteosarcoma 

    Parrales, Alejandro; McDonald, Peter R.; Ottomeyer, Megan; Roy, Anuradha; Shoenen, Frank J.; Broward, Melinda; Bruns, Tyce; Thamm, Douglas H.; Weir, Scott J.; Neville, Kathleen A.; Iwakuma, Tomoo; Fulbright, Joy M. (Public Library of Science, 2018-03-26)
    BACKGROUND: Osteosarcoma is an orphan disease for which little improvement in survival has been made since the late 1980s. New drug discovery for orphan diseases is limited by the cost and time it takes to develop new ...

  • Development of High-Throughput Screening Assay for Antihantaviral Therapeutics 

    Roy, Anuradha; Mir, Mohammad A. (SAGE Publications, 2017-07)
    Humans acquire hantavirus infection by the inhalation of aerosolized excreta of infected rodent hosts. There is no treatment for hantavirus diseases at present. Therapeutic intervention during early stages of viral infection ...

  • Measuring and statistically testing the size of the effect of a chemical compound on a continuous in-vitro pharmacological response through a new statistical model of response detection limit 

    Diaz, Francisco J.; McDonald, Peter R.; Pinter, Abraham; Chaguturu, Rathnam (Taylor & Francis, 2015)
    Biomolecular screening research frequently searches for the chemical compounds that are most likely to make a biochemical or cell-based assay system produce a strong continuous response. Several doses are tested with each ...

  • Drug Repurposing for Gastrointestinal Stromal Tumor 

    Pessetto, Ziyan Y.; Weir, Scott J.; Sethi, Geetika; Broward, Melinda; Godwin, Andrew K. (American Association for Cancer Research, 2013-07)
    Despite significant treatment advances over the past decade, metastatic gastrointestinal stromal tumor (GIST) remains largely incurable. Rare diseases, such as GIST, individually affect small groups of patients but ...

  • Open Access High Throughput Drug Discovery in the Public Domain: A Mount Everest in the Making 

    Roy, Anuradha; McDonald, Peter R.; Sittampalam, Sitta; Chaguturu, Rathnam (Bentham Science Publishers, 2010-11-11)
    High throughput screening (HTS) facilitates screening large numbers of compounds against a biochemical target of interest using validated biological or biophysical assays. In recent years, a significant number of drugs in ...

  • Targeting Epithelial-Mesenchymal Transition for Identification of Inhibitors for Pancreatic Cancer Cell Invasion and Tumor Spheres Formation 

    Polireddy, Kishore; Dong, Ruochen; McDonald, Peter R.; Wang, Tao; Luke, Brendan; Chen, Ping; Broward, Melinda; Roy, Anuradha; Chen, Qi (Public Library of Science, 2016-10-20)
    Background Pancreatic cancer has an enrichment of stem-like cancer cells (CSCs) that contribute to chemoresistant tumors prone to metastasis and recurrence. Drug screening assays based on cytotoxicity cannot identify ...