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Characterization of a novel mitogen-activated protein kinase kinase 1/2 inhibitor with a unique mechanism of action for cancer therapy.
The mitogen-activated protein kinase (MAPK) signal transduction pathway plays a central role in regulating tumor cell growth, survival, differentiatio…
Authors: Sherif Daouti, Huisheng Wang, Wen-hui Li, Brian Higgins, Kenneth Kolinsky, Kathryn Packman, Anthony Specian, Norman Kong, Nicholas Huby, Yang Wen,…
Source: Cancer research. 2009 Mar 1
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Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties.
Notch signaling is an area of great interest in oncology. RO4929097 is a potent and selective inhibitor of gamma-secretase, producing inhibitory activ…
Authors: Leopoldo Luistro, Wei He, Melissa Smith, Kathryn Packman, Maria Vilenchik, Daisy Carvajal, John Roberts, James Cai, Windy Berkofsky-Fessler, Holly Hilton,…
Source: Cancer research. 2009 Oct 1
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A selective phosphatase of regenerating liver phosphatase inhibitor suppresses tumor cell anchorage-independent growth by a novel mechanism involving p130Cas cleavage.
The phosphatase of regenerating liver (PRL) family, a unique class of oncogenic phosphatases, consists of three members: PRL-1, PRL-2, and PRL-3. Aber…
Authors: Sherif Daouti, Wen-hui Li, Hong Qian, Kuo-Sen Huang, Janna Holmgren, Wayne Levin, Linda Reik, Debra Lucas McGady, Paul Gillespie, Agostino Perrotta,…
Source: Cancer research. 2008 Feb 15
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Preclinical in vivo evaluation of efficacy, pharmacokinetics, and pharmacodynamics of a novel MEK1/2 kinase inhibitor RO5068760 in multiple tumor models.
Targeting the Ras/Raf/mitogen-activated protein kinase kinase (MEK)/extracellular signal-regulated kinase (ERK) pathway represents a promising antican…
Authors: Sherif Daouti, Brian Higgins, Kenneth Kolinsky, Kathryn Packman, Huisheng Wang, Christine Rizzo, John Moliterni, Nicholas Huby, Nader Fotouhi, Mei Liu,…
Source: Molecular cancer therapeutics. 2010 Jan
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In vivo activity of novel capecitabine regimens alone and with bevacizumab and oxaliplatin in colorectal cancer xenograft models.
Modifying the capecitabine dosing schedule from 14 days on, 7 days off (14/7) to 7 days on, 7 days off (7/7) may enable higher doses and improved anti…
Authors: Kenneth Kolinsky, Ben-Quan Shen, Yu-E Zhang, Joseph Kohles, Ute Dugan, Thomas F Zioncheck, David Heimbrook, Kathryn Packman, Brian Higgins
Source: Molecular cancer therapeutics. 2009 Jan
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Novel regimens of capecitabine alone and combined with irinotecan and bevacizumab in colorectal cancer xenografts.
BACKGROUND: Xenograft and mathematical models have shown that the antitumor activity of capecitabine can be increased by modifying the schedule from 1…
Authors: Kenneth Kolinsky, Yu-E Zhang, Ute Dugan, David Heimbrook, Kathryn Packman, Brian Higgins
Source: Anticancer research. 2009 Jan
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A novel orally bioavailable inhibitor of kinase insert domain-containing receptor induces antiangiogenic effects and prevents tumor growth in vivo.
A strategy for antagonizing vascular endothelial growth factor (VEGF) -induced angiogenesis is to inhibit the kinase activity of its receptor, kinase …
Authors: Laura Sepp-Lorenzino, Elaine Rands, Xianzhi Mao, Brett Connolly, Jennifer Shipman, Joanne Antanavage, Susan Hill, Lenora Davis, Stephen Beck, Keith Rickert,…
Source: Cancer research. 2004 Jan 15
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Antitumor activity of capecitabine and bevacizumab combination in a human estrogen receptor-negative breast adenocarcinoma xenograft model.
BACKGROUND: Capecitabine and bevacizumab have each been shown to inhibit tumor growth. Their combination failed to improve survival in a phase III tri…
Authors: Brian Higgins, Kenneth Kolinsky, Michael Linn, Violeta Adames, Yu-E Zhang, Carlos Moisa, Ute Dugan, David Heimbrook, Kathryn Packman
Source: Anticancer research. 2007 Jul-Aug
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In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials.
The cyclin-dependent protein kinases are key regulators of cell cycle progression. Aberrant expression or altered activity of distinct cyclin-dependen…
Authors: Wanda DePinto, Xin-Jie Chu, Xuefeng Yin, Melissa Smith, Kathryn Packman, Petra Goelzer, Allen Lovey, Yingsi Chen, Hong Qian, Rachid Hamid,…
Source: Molecular cancer therapeutics. 2006 Nov
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