Publications by authors named "Brent Appleton"

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GABARAP sequesters the FLCN-FNIP tumor suppressor complex to couple autophagy with lysosomal biogenesis.
Jonathan M Goodwin, Ward G Walkup, Kirsty Hooper, Taoyingnan Li, Chieko Kishi-Itakura, Brent A Appleton

Sci Adv· October 2021

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Design and Discovery of -(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic.
Savithri Ramurthy, Benjamin R Taft, Robert J Aversa, Paul A Barsanti, Matthew T Burger, Brent A Appleton

J Med Chem· March 2020

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Design and synthesis of potent RSK inhibitors.
Rama Jain, Michelle Mathur, Jiong Lan, Abran Costales, Gordana Atallah, Brent A Appleton

Bioorg Med Chem Lett· October 2018

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Mathematical and Structural Characterization of Strong Nonadditive Structure-Activity Relationship Caused by Protein Conformational Changes.
Laurent Gomez, Rui Xu, William Sinko, Brandon Selfridge, William Vernier, Brent Appleton

J Med Chem· September 2018

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Fragment-Based Drug Discovery of Inhibitors of Phosphopantetheine Adenylyltransferase from Gram-Negative Bacteria.
Robert J Moreau, Colin K Skepper, Brent A Appleton, Anke Blechschmidt, Carl J Balibar

J Med Chem· April 2018

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Discovery and Optimization of Phosphopantetheine Adenylyltransferase Inhibitors with Gram-Negative Antibacterial Activity.
Colin K Skepper, Robert J Moreau, Brent A Appleton, Bret M Benton, Joseph E Drumm

J Med Chem· April 2018

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Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.
Aaron Smith, Zhi-Jie Ni, Daniel Poon, Zilin Huang, Zheng Chen, Brent A Appleton

Bioorg Med Chem Lett· December 2017

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Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers.
Gisele A Nishiguchi, Alice Rico, Huw Tanner, Robert J Aversa, Benjamin R Taft, Brent A Appleton

J Med Chem· June 2017

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Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug Design.
Wooseok Han, Yu Ding, Yongjin Xu, Keith Pfister, Shejin Zhu, Brent Appleton

J Med Chem· April 2016

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Discovery of Potent and Selective RSK Inhibitors as Biological Probes.
Rama Jain, Michelle Mathur, Jiong Lan, Abran Costales, Gordana Atallah, Brent A Appleton

J Med Chem· September 2015

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Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.
Teresa E Williams, Sharadha Subramanian, Joelle Verhagen, Christopher M McBride, Abran Costales, Brent A Appleton

ACS Med Chem Lett· September 2015

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Discovery of the 1,7-diazacarbazole class of inhibitors of checkpoint kinase 1.
Lewis Gazzard, Brent Appleton, Kerry Chapman, Huifen Chen, Kevin Clark

Bioorg Med Chem Lett· December 2014

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A structural portrait of the PDZ domain family.
Andreas Ernst, Brent A Appleton, Ylva Ivarsson, Yingnan Zhang, David Gfeller

J Mol Biol· October 2014

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Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers.
Ida Aronchik, Brent A Appleton, Stephen E Basham, Kenneth Crawford, Mercedita Del Rosario

Mol Cancer Res· May 2014

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2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors.
Abran Costales, Michelle Mathur, Savithri Ramurthy, Jiong Lan, Sharadha Subramanian, Brent A Appleton

Bioorg Med Chem Lett· March 2014

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A drug resistance screen using a selective MET inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patients.
Ralph Tiedt, Elisa Degenkolbe, Pascal Furet, Brent A Appleton, Sabrina Wagner

Cancer Res· August 2011

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Structure of IL-33 and its interaction with the ST2 and IL-1RAcP receptors--insight into heterotrimeric IL-1 signaling complexes.
Andreas Lingel, Thomas M Weiss, Marc Niebuhr, Borlan Pan, Brent A Appleton

Structure· October 2009

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Inhibition of Wnt signaling by Dishevelled PDZ peptides.
Yingnan Zhang, Brent A Appleton, Christian Wiesmann, Ted Lau, Mike Costa

Nat Chem Biol· April 2009

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Variants of the antibody herceptin that interact with HER2 and VEGF at the antigen binding site.
Jenny Bostrom, Shang-Fan Yu, David Kan, Brent A Appleton, Chingwei V Lee

Science· March 2009

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Anakinra in the treatment of polyarticular-course juvenile rheumatoid arthritis: safety and preliminary efficacy results of a randomized multicenter study.
Norman Ilowite, Oscar Porras, Andreas Reiff, Sue Rudge, Marilynn Punaro, Brent Appleton

Clin Rheumatol· February 2009

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A specificity map for the PDZ domain family.
Raffi Tonikian, Yingnan Zhang, Stephen L Sazinsky, Bridget Currell, Jung-Hua Yeh, Brent A Appleton

PLoS Biol· September 2008

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Effect of anakinra on functional status in patients with active rheumatoid arthritis receiving concomitant therapy with traditional disease modifying antirheumatic drugs: evidence from the OMEGA Trial.
Xavier Le Loët, Dan Nordström, Manuel Rodriguez, Andrea Rubbert, Piercarlo Sarzi-Puttini, Brent Appleton

J Rheumatol· August 2008

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Comprehensive analysis of the factors contributing to the stability and solubility of autonomous human VH domains.
Pierre A Barthelemy, Helga Raab, Brent A Appleton, Christopher J Bond, Ping Wu

J Biol Chem· February 2008

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Structural and functional analysis of the PDZ domains of human HtrA1 and HtrA3.
Steven T Runyon, Yingnan Zhang, Brent A Appleton, Stephen L Sazinsky, Ping Wu

Protein Sci· November 2007

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Structural studies of neuropilin/antibody complexes provide insights into semaphorin and VEGF binding.
Brent A Appleton, Ping Wu, Janice Maloney, JianPing Yin, Wei-Ching Liang

EMBO J· November 2007

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