Zobrazeno 1 - 10
of 55
pro vyhledávání: '"Deborah DeFeo"'
Autor:
Qing-Bai She, Sarat Chandarlapaty, Qing Ye, Jose Lobo, Kathleen M Haskell, Karen R Leander, Deborah DeFeo-Jones, Hans E Huber, Neal Rosen
Publikováno v:
PLoS ONE, Vol 3, Iss 8, p e3065 (2008)
Dysregulated PI3K/Akt signaling occurs commonly in breast cancers and is due to HER2 amplification, PI3K mutation or PTEN inactivation. The objective of this study was to determine the role of Akt activation in breast cancer as a function of mechanis
Externí odkaz:
https://doaj.org/article/b5b859fcec964286a6785e18f0e5d4e2
Autor:
Martin G. Sanda, Karen R. Leander, Deborah Defeo-Jones, Mohamed S. Arredouani, Clara Hwang, Brent K. Hollenbeck, Stephanie Tseng-Rogenski, June Escara-Wilke
Publikováno v:
The Prostate. 70:1002-1011
BACKGROUND In recent years, there has been an increasing interest in targeting human prostate tumor-associated antigens (TAAs) for prostate cancer immunotherapy as an alternative to other therapeutic modalities. However, immunologic tolerance to TAA
Autor:
Stanley F. Barnett, Tony Siu, Jeannie M. Arruda, Deborah Defeo-Jones, Jun Liang, Raymond E. Jones, Ronald G. Robinson, Yiwei Li
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4186-4190
This paper describes the improvement of cell potency in a class of allosteric Akt 1 and 2 inhibitors. Key discoveries include identifying the solvent exposed region of the molecule and appending basic amines to enhance the physiochemical properties o
Autor:
Peter C. Chua, Yiwei Li, Jun Liang, Johnny Y. Nagasawa, Raymond E. Jones, Stanley F. Barnett, Lida R. Tehrani, Ronald G. Robinson, Deborah Defeo-Jones, Tony Siu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4191-4194
This letter details the attenuation of hERG in a class of Akt inhibitors through heteroatom insertions into aromatic rings. The development of a cell-active dual Akt 1 and 2 inhibitors devoid of hERG activity is discussed using structure-activity rel
Autor:
Ronald G. Robinson, Mark T. Bilodeau, Stanley F. Barnett, Lou Anne Neilson, Astrid M. Kral, Raymond E. Jones, George D. Hartman, Hans E. Huber, John C. Hartnett, Zhicai Wu, Deborah Defeo-Jones, Sheng Fu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1274-1279
This communication reports a new synthetic route of pyridopyrimidines to facilitate their structural optimization in a library fashion and describes the development of pyridopyrimidines that have excellent enzymatic and cell potency against Akt1 and
Autor:
Charles W. Ross, Deborah Defeo-Jones, Stanley F. Barnett, Craig W. Lindsley, Ray T. McClain, Michael J. Bogusky, George D. Hartman, William H. Leister, Ronald G. Robinson
Publikováno v:
Tetrahedron Letters. 46:2779-2782
Employing a ‘one-pot’ microwave-assisted protocol, unnatural canthine alkaloids with biological activities beyond the natural products have been prepared. This report describes unnatural canthine alkaloid analogs as selective, allosteric Akt kina
Autor:
Stanley F. Barnett, Zhijian Zhao, Joel R. Huff, Deborah Defeo-Jones, Raymond E. Jones, Craig W. Lindsley, Mark E. Duggan, William H. Leister, Ronald G. Robinson, Hans E. Huber, George D. Hartman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:761-764
This letter describes the development of two series of potent and selective allosteric Akt kinase inhibitors that display an unprecedented level of selectivity for either Akt1, Akt2 or both Akt1/Akt2. An iterative analog library synthesis approach qu
Autor:
Deborah DeFeo-Jones, Stanley F. Barnett, Sheng Fu, Paula J. Hancock, Kathleen M. Haskell, Karen R. Leander, Elizabeth McAvoy, Ronald G. Robinson, Mark E. Duggan, Craig W. Lindsley, Zhijian Zhao, Hans E. Huber, Raymond E. Jones
Publikováno v:
Molecular Cancer Therapeutics. 4:271-279
Recent studies indicate that dysregulation of the Akt/PKB family of serine/threonine kinases is a prominent feature of many human cancers. The Akt/PKB family is composed of three members termed Akt1/PKBα, Akt2/PKBβ, and Akt3/PKBγ. It is currently
Autor:
Stanley F. Barnett, Nicholas D. P. Cosford, Deborah Defeo-Jones, Michael A. Rossi, Jun Liang, Hans E. Huber, Ronald G. Robinson, Raymond E. Jones, Hu Essa H, Yiwei Li, Sachin Mittal, Karen R. Leander, Tony Siu, Peppi Prasit
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:834-836
A series of [1,2,4]triazolo[3,4-f][1,6]naphthyridine allosteric dual inhibitors of Akt1 and 2 have been developed. These compounds have been shown to have potent dual Akt1 and 2 cell potency. The representative compound 13 provided potent inhibitory