Zobrazeno 1 - 10
of 45
pro vyhledávání: '"Cristina Lewis"'
Autor:
Lori S. Friedman, Marcia Belvin, Deepak Sampath, Mark R. Lackner, Leanne Ross, Robert Kassees, Letitia Lensun, Sonal Patel, Jill M. Spoerke, Carol O'Brien, Daniel P. Sutherlin, Alan G. Olivero, Laurent Salphati, Jodie Pang, Jim Nonomiya, Cristina Lewis, John D. Lesnick, Leslie Lee, Wei Wei Prior, Megan Berry, Jane Guan, Kyle A. Edgar, Jeffrey J. Wallin
PDF file - 894K
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::136e199abb6bc063918f64da058aa806
https://doi.org/10.1158/1535-7163.22496520
https://doi.org/10.1158/1535-7163.22496520
Autor:
Lori S. Friedman, Marcia Belvin, Deepak Sampath, Mark R. Lackner, Leanne Ross, Robert Kassees, Letitia Lensun, Sonal Patel, Jill M. Spoerke, Carol O'Brien, Daniel P. Sutherlin, Alan G. Olivero, Laurent Salphati, Jodie Pang, Jim Nonomiya, Cristina Lewis, John D. Lesnick, Leslie Lee, Wei Wei Prior, Megan Berry, Jane Guan, Kyle A. Edgar, Jeffrey J. Wallin
Alterations of the phosphoinositide-3 kinase (PI3K)/Akt signaling pathway occur broadly in cancer via multiple mechanisms including mutation of the PIK3CA gene, loss or mutation of phosphatase and tensin homolog (PTEN), and deregulation of mammalian
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::344448ff3a06fe2f5d7081d2a898c2c2
https://doi.org/10.1158/1535-7163.c.6535305
https://doi.org/10.1158/1535-7163.c.6535305
Autor:
Jim Nonomiya, Laurent Salphati, Martin Augistin, Philip Stephen Jackson, Mario Mörtl, Steven Do, Steve Price, Robert Heald, Chudi Ndubaku, Binqing Wei, Timothy P. Heffron, Aleksander Kolesnikov, John Lesnick, Alan G. Olivero, Leslie Lee, Charles Eigenbrot, Graham Jones, Vickie Tsui, Wei Wei Prior, Neville James Mclean, Kyle A. Edgar, Emanuela Gancia, Deepak Sampath, Jodie Pang, Steven T. Staben, Stefan Steinbacher, Cristina Lewis, Jeffrey Wallin, Steve Sideris, Lori Friedman
Publikováno v:
Journal of Medicinal Chemistry. 59:985-1002
Inhibitors of the class I phosphoinositide 3-kinase (PI3K) isoform PI3Kα have received substantial attention for their potential use in cancer therapy. Despite the particular attraction of targeting PI3Kα, achieving selectivity for the inhibition o
Autor:
Bryan K. Chan, Cristina Lewis, Steve Price, Brian Safina, Robert Heald, Zachary Kevin Sweeney, Jodie Pang, Karin Reif, Georgette Castanedo, Jun Li, Daniel P. Sutherlin, Michael Flagella, Eileen Mary Seward, Jeremy Murray, Jim Nonomiya, Laurent Salphati, Angelina Bisconte, Binqing Wei, Diane E. Carrera
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23(17):4953-4959
In an effort to identify potent and isoform selective inhibitors of PI3Kδ, GNE-293 (34) was identified. Inhibitor 2 was found to induce micronuclei formation in both the MNT and HCA in vitro assays. Compounds testing negative for genotoxicity were s
Autor:
Richard A. Goldsmith, Cristina Lewis, Binqing Wei, Jeffery J. Wallin, Erin K. Bradley, Nicole Blaquiere, Leslie Lee, Steven T. Staben, Jim Nonomiya, Steven Do, Deepak Sampath, Laurent Salphati, Timothy P. Heffron, Jodie Pang, Chudi Ndubaku, Kyle A. Edgar, Danette Dudley, Robert Heald, Richard James Bull, Matthew Baumgardner, Steve Price, Wei Wei Prior, Steve Sideris, Jennafer Dotson, Lan Wang, Michelle Nannini, Aleksandr Kolesnikov, Lori Friedman, Olivero Alan G
Publikováno v:
Journal of Medicinal Chemistry. 56:4597-4610
Dysfunctional signaling through the phosphoinositide 3-kinase (PI3K)/AKT/mTOR pathway leads to uncontrolled tumor proliferation. In the course of the discovery of novel benzoxepin PI3K inhibitors, we observed a strong dependency of in vivo antitumor
Autor:
Laurent Salphati, Nicole Blaquiere, Cristina Lewis, Steven Do, Binqing Wei, Steven T. Staben, Aleksandr Kolesnikov, Alan G. Olivero, Erin K. Bradley, Jim Nonomiya, Lionel Rouge, Jenna Dotson, Jodie Pang, Vickie Tsui, John Lesnick, Richard Goldsmith, Timothy P. Heffron, Ping Wu, Jeremy Murray, Christian Wiesmann
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:897-901
Substructural class effects surrounding replacement of a 'cis' N-methyl aniline amide within potent and selective thienobenzoxepin PI3-kinase inhibitors are disclosed. While a simple aryl to alkyl switch was not tolerated due to differences in prefer
Autor:
Timothy P, Heffron, Robert A, Heald, Chudi, Ndubaku, BinQing, Wei, Martin, Augistin, Steven, Do, Kyle, Edgar, Charles, Eigenbrot, Lori, Friedman, Emanuela, Gancia, Philip S, Jackson, Graham, Jones, Aleksander, Kolesnikov, Leslie B, Lee, John D, Lesnick, Cristina, Lewis, Neville, McLean, Mario, Mörtl, Jim, Nonomiya, Jodie, Pang, Steve, Price, Wei Wei, Prior, Laurent, Salphati, Steve, Sideris, Steven T, Staben, Stefan, Steinbacher, Vickie, Tsui, Jeffrey, Wallin, Deepak, Sampath, Alan G, Olivero
Publikováno v:
Journal of medicinal chemistry. 59(3)
Inhibitors of the class I phosphoinositide 3-kinase (PI3K) isoform PI3Kα have received substantial attention for their potential use in cancer therapy. Despite the particular attraction of targeting PI3Kα, achieving selectivity for the inhibition o
Autor:
Jeffrey Wallin, Jodie Pang, Laurent Salphati, Stephen E. Gould, Leslie Lee, Jonathan Cheong, Cristina Lewis, Timothy P. Heffron, Xiaolin Zhang, Steve Sideris, Chudi Ndubaku, Jim Nonomiya, Joy Drobnick, Emile Plise, Lan Wang, Bruno Alicke, Alan G. Olivero, Kyle A. Edgar, John Lesnick
Publikováno v:
ACS medicinal chemistry letters. 7(4)
Inhibition of phosphoinositide 3-kinase (PI3K) signaling is an appealing approach to treat brain tumors, especially glioblastoma multiforme (GBM). We previously disclosed our successful approach to prospectively design potent and blood–brain barrie
Autor:
Laurent Salphati, Stewart J. Baker, Steve Price, Jim Nonomiya, Matthew C. Lucas, Timothy Hancox, David Knowles, Bohdan Waszkowycz, Neil Anthony Pegg, David Chantry, Bryan K. Chan, Paul Blaney, Anthony Brown, Steven T. Staben, Jodie Pang, Paul Depledge, Rama K. Kondru, Mark Ultsch, Paul Goldsmith, Karin Reif, Angelina Bisconte, Cristina Lewis, Eileen Mary Seward, Jeremy Murray, Brian Safina, Daniel P. Sutherlin, Zachary Kevin Sweeney, Georgette Castanedo, David Michael Goldstein, Jasmit Kaur, Sukhjit Sohal, Binqing Wei, John Lesnick, Stephen J. Shuttleworth, Alan Nadin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4296-4302
A potent inhibitor of PI3Kδ that is ⩾200 fold selective for the remaining three Class I PI3K isoforms and additional kinases is described. The hypothesis for selectivity is illustrated through structure activity relationships and crystal structure
Autor:
Amy Gustafson, Maureen Beresini, Linda O. Elliott, Robert Mintzer, Kevin R Clark, Christopher E. Heise, Cristina Lewis, Kinjalkumar Shah, Marya Liimatta, Yichin Liu, Adam R. Johnson, Stephen Schmidt
Publikováno v:
SLAS Discovery. 17:225-236
Identifying chemical lead matter by high-throughput screening (HTS) has been a common practice in early stage drug discovery. Evolution of small-molecule library composition to include more drug-like molecules with desirable physical chemical propert