Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Stefan D. Gross"'
Autor:
Stefan D Gross, Christopher A. Eide, Michael R Burkard, Anna Reister Schultz, Monette A Aujay, Samuel Kintz, Brian J. Druker, Joseph P Lyssikatos
Publikováno v:
Blood. 140:3095-3096
Autor:
Monette Aujay, Amanda J. Broad, Stefan D. Gross, Li Ren, Joseph P. Lyssikatos, Samuel Kintz, Qi Wang, Helen Collins
Publikováno v:
Cancer Research. 83:4019-4019
Mutation or amplification of the human epidermal growth factor receptor 2 (HER2) gene has been identified in numerous solid tumor types, including non-small cell lung cancer (NSCLC), breast, and colorectal cancer. These genetic alterations are believ
Publikováno v:
Journal of Clinical Investigation. 125:1780-1789
Kinase inhibitors have played an increasingly prominent role in the treatment of cancer and other diseases. Currently, more than 25 oncology drugs that target kinases have been approved, and numerous additional therapeutics are in various stages of c
Autor:
Nicholas J. Skelton, Hartmut Koeppen, Heidi Savage, Jeffrey Wallin, Tyler Risom, Jason Oeh, Bianca M. Liederer, Lori Friedman, Kui Lin, Stefan D. Gross, Michael Degtyarev, Robert Kassees, Rebecca Hong, Marcia Belvin, Zhengyu Guan, Deepak Sampath, Michelle Nannini, Leslie Lee, Elizabeth Punnoose, Brian Lee, Jie Lin
Publikováno v:
Clinical Cancer Research. 19:1760-1772
Purpose: We describe the preclinical pharmacology and antitumor activity of GDC-0068, a novel highly selective ATP-competitive pan-Akt inhibitor currently in clinical trials for the treatment of human cancers. Experimental Design: The effect of GDC-0
Autor:
Eli M. Wallace, Francis X. Sullivan, Yvan Le Huerou, Stefan D. Gross, Jennifer Garrus, P LouAnn Cable, Richard Woessner, Kurtis D. Davies, Ira von Carlowitz
Publikováno v:
Cancer Biology & Therapy. 12:788-796
Inhibition of the checkpoint kinase Chk1, both as a monotherapy and in combination with DNA damaging cytotoxics, is a promising therapeutic approach for the treatment of a wide array of human cancers. However, much remains to be elucidated in regard
Autor:
Josef R. Bencsik, Barbara J. Brandhuber, Banka Anna L, Guy Vigers, Nicholas J. Skelton, Stefan D. Gross, Wen-I Wu, Matthew Martinson, Ian S. Mitchell, Susan L. Gloor, Rui Xu, Keith Lee Spencer, Tyler Risom, James F. Blake, Nicholas C. Kallan, Eli M. Wallace, Tony Morales
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2335-2340
We describe the design and synthesis of novel bicyclic spiro sulfonamides as potent Akt inhibitors. Through structure-based rational design, we have successfully improved PKA selectivity of previously disclosed spirochromanes. Representative compound
Autor:
Nicholas J. Skelton, Matthew Martinson, Ian S. Mitchell, Josef R. Bencsik, Susan L. Gloor, Tony Morales, Rui Xu, Keith Lee Spencer, Tyler Risom, Barbara J. Brandhuber, Guy Vigers, Nicholas C. Kallan, Justin W. Heizer, James F. Blake, Wen-I Wu, Stefan D. Gross
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2410-2414
A novel series of spirochromane pan-Akt inhibitors is reported. SAR optimization furnished compounds with improved enzyme potencies and excellent selectivity over the related AGC kinase PKA. Attempted replacement of the phenol hinge binder provided c
Autor:
Keith Lee Spencer, Tyler Risom, Guy Vigers, Nicholas J. Skelton, Stefan D. Gross, Nicholas C. Kallan, Josef R. Bencsik, James F. Blake, Matthew Martinson, Ian S. Mitchell, Rui Xu, Richard Woessner, Tony Morales, Susan L. Gloor, Dengming Xiao, Barbara J. Brandhuber
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5607-5612
The discovery and optimization of a series of pyrrolopyrimidine based protein kinase B (Pkb/Akt) inhibitors discovered via HTS and structure based drug design is reported. The compounds demonstrate potent inhibition of all three Akt isoforms and knoc
Autor:
Richard A. Anderson, Stefan D. Gross
Publikováno v:
Cellular Signalling. 10:699-711
The casein kinase I family of serine/threonine protein kinases is highly conserved from yeast to humans. Until only recently, both the function and regulation of these enzymes remained poorly uncharacterised in that they appeared to be constitutively
Autor:
Mark Joseph Chicarelli, Francis X. Sullivan, Stefan D. Gross, Eli M. Wallace, Lyon Michael, Michael J. Humphries, Gunawardana Indrani W, Mohr Peter, Yvan Le Huerou, James F. Blake, Kurtis D. Davies, Bin Wang, Ira von Carlowitz
Publikováno v:
Oncology research. 19(7)
Chk1 is a serine/threonine kinase that plays several important roles in the cellular response to genotoxic stress. Since many current standard-of-care therapies for human cancer directly damage DNA or inhibit DNA synthesis, there is interest in using