Zobrazeno 1 - 10
of 50
pro vyhledávání: '"Anthony M Giannetti"'
Autor:
Christopher E Heise, Jeremy Murray, Katherine E Augustyn, Brandon Bravo, Preeti Chugha, Frederick Cohen, Anthony M Giannetti, Paul Gibbons, Rami N Hannoush, Brian R Hearn, Priyadarshini Jaishankar, Cuong Q Ly, Kinjalkumar Shah, Karen Stanger, Micah Steffek, Yinyan Tang, Xianrui Zhao, Joseph W Lewcock, Adam R Renslo, John Flygare, Michelle R Arkin
Publikováno v:
PLoS ONE, Vol 7, Iss 12, p e50864 (2012)
Inhibition of caspase-6 is a potential therapeutic strategy for some neurodegenerative diseases, but it has been difficult to develop selective inhibitors against caspases. We report the discovery and characterization of a potent inhibitor of caspase
Externí odkaz:
https://doaj.org/article/86e58beea90d4df59b4e81e29a6f24b6
Publikováno v:
PLoS Biology, Vol 1, Iss 3, p E51 (2003)
Transferrin receptor 1 (TfR) plays a critical role in cellular iron import for most higher organisms. Cell surface TfR binds to circulating iron-loaded transferrin (Fe-Tf) and transports it to acidic endosomes, where low pH promotes iron to dissociat
Externí odkaz:
https://doaj.org/article/d478c513ce8e49d1967cc210ab48f9fd
Autor:
Michael L Doyle, Preston Hensley, Anthony M. Giannetti, Aaron P. Yamniuk, John A Newitt, Fred P Schwarz, Edward Eisenstein, James A. Thomson, David G Myszka, Fumio Arisaka
Publikováno v:
Journal of Biomolecular Techniques : JBT. 26:125-141
A significant challenge in the molecular interaction field is to accurately determine the stoichiometry and stepwise binding affinity constants for macromolecules having >1 binding site. The mission of the Molecular Interactions Research Group (MIRG)
Autor:
Wendy Sandoval, Barbara J. Brandhuber, Brandon J. Bravo, Wilson Phung, Sarah G. Hymowitz, Steve Sideris, Darin Smith, Alexandre Masselot, Jacob R. Haling, Tony Morales, Shiva Malek, Ivana Yen, Ariana Peck, Anthony M. Giannetti, Jawahar Sudhamsu
Publikováno v:
Cancer Cell. 26(3):402-413
Numerous oncogenic mutations occur within the BRAF kinase domain (BRAF(KD)). Here we show that stable BRAF-MEK1 complexes are enriched in BRAF(WT) and KRAS mutant (MT) cells but not in BRAF(MT) cells. The crystal structure of the BRAF(KD) in a comple
Autor:
Peter S. Dragovich, Benjamin P. Fauber, Jason Boggs, Jinhua Chen, Laura B. Corson, Charles Z. Ding, Charles Eigenbrot, HongXiu Ge, Anthony M. Giannetti, Thomas Hunsaker, Sharada Labadie, Chiho Li, Yichin Liu, Yingchun Liu, Shuguang Ma, Shiva Malek, David Peterson, Keith E. Pitts, Hans E. Purkey, Kirk Robarge, Laurent Salphati, Steve Sideris, Mark Ultsch, Erica VanderPorten, Jing Wang, BinQing Wei, Qing Xu, Ivana Yen, Qin Yue, Huihui Zhang, Xuying Zhang, Aihe Zhou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:3764-3771
A novel class of 3-hydroxy-2-mercaptocyclohex-2-enone-containing inhibitors of human lactate dehydrogenase (LDH) was identified through a high-throughput screening approach. Biochemical and surface plasmon resonance experiments performed with a scree
Autor:
Erin McNamara, Chudi Ndubaku, Ping Wu, Steven Magnuson, Lesley J. Murray, Anthony M. Giannetti, Kristina West, Weilan Ye, Stanley Mark S, Seth F. Harris, Jason Boggs, Brandon J. Bravo, Tanya Smyczek, Jim Nonomiya, Kelly J. Delatorre, Stephen E. Gould, Philip Vitorino, Stephen Schmidt, Huifen Chen, Lan Wang, Terry Crawford, Amy Sambrone
Publikováno v:
Journal of Medicinal Chemistry. 57:3484-3493
Mitogen-activated protein kinase kinase kinase kinase 4 (MAP4K4) is a serine/threonine kinase implicated in the regulation of many biological processes. A fragment-based lead discovery approach was used to generate potent and selective MAP4K4 inhibit
Autor:
Thomas O'Brien, Peter S. Dragovich, Brandon J. Bravo, Xiaozhang Zheng, Chengcheng Wang, Weiru Wang, Nicholas J. Skelton, Qiang Zhao, Yunli Wang, Mark Zak, Angela Oh, Guangkun Li, Yen-Ching Ho, Anthony M. Giannetti, Guiling Zhao, Yuen Po-Wai, Xiaolei Ma, Yang Xiao, Rongbao Hua, Xiaorong Liang, Timm Baumeister
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:954-962
The fragment-based identification of two novel and potent biochemical inhibitors of the nicotinamide phosphoribosyltransferase (NAMPT) enzyme is described. These compounds (51 and 63) incorporate an amide moiety derived from 3-aminopyridine, and are
Autor:
Micah Steffek, Frederick Cohen, Christine Pozniak, Preeti Chugha, Joe Lewcock, Brandon J. Bravo, Yinyan Tang, Adam R. Renslo, Xianrui Zhao, Brian R. Hearn, Jeremy Murray, Michelle R. Arkin, John A. Flygare, Priyadarshini Jaishankar, Christine Tam, Cuong Ly, Paul Gibbons, Anthony M. Giannetti
Publikováno v:
ChemMedChem. 9:73-77
Although they represent attractive therapeutic targets, caspases have so far proven recalcitrant to the development of drugs targeting the active site. Allosteric modulation of caspase activity is an alternate strategy that potentially avoids the nee
Autor:
Binqing Wei, Erica VanderPorten, Peter S. Dragovich, Benjamin Fauber, Qin Yue, Jinhua Chen, Shiva Malek, Wang Jing, Charles Z. Ding, Anthony M. Giannetti, Liu Yingchun, Yichin Liu, Ivana Yen, Keith Pitts, Laura Corson, Charles Eigenbrot, Steve Sideris, Mark Ultsch, Sharada Labadie, David Peterson, Thomas Hunsaker
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:5533-5539
A 2-amino-5-aryl-pyrazine was identified as an inhibitor of human lactate dehydrogenase A (LDHA) via a biochemical screening campaign. Biochemical and biophysical experiments demonstrated that the compound specifically interacted with human LDHA. Str
Autor:
Erica VanderPorten, Binqing Wei, Keith Pitts, Shiva Malek, Benjamin Fauber, Sharada Labadie, Mark Ultsch, Anthony M. Giannetti, Steve Sideris, Huihui Zhang, Qin Yue, Thomas Hunsaker, Charles Z. Ding, Laura Corson, David Peterson, Xuying Zhang, Borlan Pan, Charles Eigenbrot, Yichin Liu, Hans E. Purkey, Peter S. Dragovich, HongXiu Ge, Ivana Yen, Qing Xu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:3186-3194
A novel 2-thio-6-oxo-1,6-dihydropyrimidine-containing inhibitor of human lactate dehydrogenase (LDH) was identified by high-throughput screening (IC50=8.1 μM). Biochemical, surface plasmon resonance, and saturation transfer difference NMR experiment