Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Paul Robert Fleming"'
Autor:
Rachel Fearns, Qin Yu, Michael Foley, Paul Robert Fleming, Jeremy R. Duvall, Barbara Ludeke, Christina Scherer, Carol A. Mulrooney, Michelle Palmer, Maurice D. Lee, Karthick Vishwanathan, Sarah M. McLeod, Lynn VerPlank, Sebastian T. Le Quement
Publikováno v:
Antiviral Research. 131:19-25
Respiratory syncytial virus (RSV) infections affect millions of children and adults every year. Despite the significant disease burden, there are currently no safe and effective vaccines or therapeutics. We employed a replicon-based high throughput s
Autor:
Jonathan A. Rose, Paul Robert Fleming, Adam B. Shapiro, David C. McKinney, Stewart L. Fisher, Rob Albert, Marshall Morningstar, Sushmita D. Lahiri
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:3301-3306
With increasing emergence of multi-drug resistant infections, there is a dire need for new classes of compounds that act through unique mechanisms. In this work, we describe the discovery and optimization of a novel series of inhibitors of bacterial
Autor:
Helen Plant, Robert E. McLaughlin, Melinda A. Foulk, Boudewijn L. M. de Jonge, Robert Albert, Scott D. Mills, Shubha Sriram, Paul Robert Fleming, Marian Preston, Jun Fan, Kathy MacCormack
Publikováno v:
Antimicrobial Agents and Chemotherapy. 58:7264-7272
Bacterial biosensor strains can be useful tools for the discovery and characterization of antibacterial compounds. A plasmid-based reporter vector containing a transcriptional fusion between the recA promoter and green fluorescence protein gene was i
Autor:
Ed T. Buurman, Melinda A. Foulk, Demetri T. Moustakas, David C. McKinney, Adam B. Shapiro, Jonathan A. Rose, Ning Gao, Paul Robert Fleming, Valerie A. Laganas
Publikováno v:
Journal of Bacteriology. 194:5504-5512
A series of inhibitors with a squaramide core was synthesized following its discovery in a high-throughput screen for novel inhibitors of a transcription-coupled translation assay using Escherichia coli S30 extracts. The inhibitors were inactive when
Autor:
Vadim Molodtsov, David C. McKinney, Paul Robert Fleming, Andrew D. Ferguson, Craig E. Masse, Charles J. Eyermann, Ed T. Buurman, Katsuhiko S. Murakami, Melinda A. Foulk
Squaramides constitute a novel class of RNA polymerase inhibitors of which genetic evidence and computational modeling previously have suggested an inhibitory mechanism mediated by binding to the RNA polymerase switch region. An iterative chemistry p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2deaa42b28ed498ea60e8a5991c5254
https://europepmc.org/articles/PMC4658208/
https://europepmc.org/articles/PMC4658208/
Autor:
Makiko Mori, Paul Robert Fleming, James D. Whiteaker, Robert E. McLaughlin, Alita A. Miller, Sarah M. McLeod, Shin-ichiro Narita, Hajime Tokuda, Kathleen MacCormack
In Gram-negative bacteria, lipoproteins are transported to the outer membrane by the Lol system. In this process, lipoproteins are released from the inner membrane by the ABC transporter LolCDE and passed to LolA, a diffusible periplasmic molecular c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bd52fc4d780dd0ee33dcce9bf2b69e87
https://europepmc.org/articles/PMC4336340/
https://europepmc.org/articles/PMC4336340/
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:775-778
Novel phenol bis-Mannich adducts were identified as IL-2 expression inhibitors in a T cell proliferation screening assay. Analogues of the lead compound were prepared through parallel synthesis and a highly selective IL-2 inhibitor was discovered tha
Autor:
Claire Sadler, Shubha Sriram, Naina Vinay Mudugal, Boudewijn L. M. de Jonge, Gajanan Shanbhag, David C. McKinney, Praveena Manjrekar, Paul Robert Fleming, Beena Paul, Charles J. Eyermann, Vasan K. Sambandamurthy, Anisha Ambady, Sudha Ravishankar, Parvinder Kaur, Murugan Chinnapattu, Anandkumar Raichurkar, Shahul Hameed P, Chaitanyakumar Kedari, Supreeth Guptha, Manoranjan Panda, Vaishali Humnabadkar
Publikováno v:
ACS chemical biology. 9(10)
The bacterial peptidoglycan biosynthesis pathway provides multiple targets for antibacterials, as proven by the clinical success of β-lactam and glycopeptide classes of antibiotics. The Mur ligases play an essential role in the biosynthesis of the p
Autor:
Douglas Ferguson, Hui Xiong, Qin Yu, Demetri T. Moustakas, Melinda A. Foulk, Dean G. Brown, Paul Robert Fleming, Dedong Wu, Jun Fan, Lisa Aschenbrenner, Minli Zhang, Kenneth D. Johnson, Choi-Lai Tiong-Yip
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(24)
Targeting viral polymerases has been a proven and attractive strategy for antiviral drug discovery. Herein we describe our effort in improving the antiviral activity and physical properties of a series of benzothienoazepine compounds as respiratory s
Autor:
John I. Manchester, Jonathan A. Rose, Shanta Bist, Kenneth Gregory Hull, Daemian Dussault, Paul Robert Fleming, Georgine Ioannidis, Maria Uria-Nickelsen, P. Ann Boriack-Sjodin
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(15)
We present the discovery and optimization of a novel series of bacterial topoisomerase inhibitors. Starting from a virtual screening hit, activity was optimized through a combination of structure-based design and physical property optimization. Synth