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Targeting the AAA ATPase p97 as an Approach to Treat Cancer through Disruption of Protein Homeostasis

Cancer cell, 2015-11, Vol.28 (5), p.653-665

2015

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Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth

Molecular cancer therapeutics, 2011-12, Vol.10 (12), p.2298-2308

2011

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The p97 Inhibitor CB-5083 Is a Unique Disrupter of Protein Homeostasis in Models of Multiple Myeloma

Molecular cancer therapeutics, 2017-11, Vol.16 (11), p.2375-2386

2017

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Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083)

Journal of medicinal chemistry, 2015-12, Vol.58 (24), p.9480-9497

2015

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Inhibition of Tumor Cell Growth, Invasion, and Metastasis by EXEL-2880 (XL880, GSK1363089), a Novel Inhibitor of HGF and VEGF Receptor Tyrosine Kinases

Cancer research (Chicago, Ill.), 2009-10, Vol.69 (20), p.8009-8016

2009

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Loss of PTEN MMAC1 TEP in EGF receptor-expressing tumor cells counteracts the antitumor action of EGFR tyrosine kinase inhibitors

Oncogene, 2003-05, Vol.22 (18), p.2812-2822

2003

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In vitro and in vivo activity of cabozantinib (XL184), an inhibitor of RET, MET, and VEGFR2, in a model of medullary thyroid cancer

Thyroid (New York, N.Y.), 2013-12, Vol.23 (12), p.1569

2013

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Mitochondrial DNA Damage is More Extensive and Persists Longer than Nuclear DNA Damage in Human Cells Following Oxidative Stress

Proceedings of the National Academy of Sciences - PNAS, 1997-01, Vol.94 (2), p.514-519

1997

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The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models

Molecular cancer therapeutics, 2015-04, Vol.14 (4), p.931-940

2015

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The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors

Bioorganic & medicinal chemistry letters, 2012-08, Vol.22 (15), p.4979-4985

2012

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Hydrogen Peroxide– and Peroxynitrite-Induced Mitochondrial DNA Damage and Dysfunction in Vascular Endothelial and Smooth Muscle Cells

Circulation research, 2000-05, Vol.86 (9), p.960-966

2000

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Inhibition of the T790M Gatekeeper Mutant of the Epidermal Growth Factor Receptor by EXEL-7647

Clinical cancer research, 2007-06, Vol.13 (12), p.3713-3723

2007

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Herceptin-induced inhibition of phosphatidylinositol-3 kinase and Akt is required for antibody-mediated effects on p27, cyclin D1, and antitumor action

Cancer research (Chicago, Ill.), 2002-07, Vol.62 (14), p.4132-4141

2002

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PKB/Akt mediates cell-cycle progression by phosphorylation of p27(Kip1) at threonine 157 and modulation of its cellular localization

Nature medicine, 2002-10, Vol.8 (10), p.1145-1152

2002

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Characterization of the activity of the PI3K/mTOR inhibitor XL765 (SAR245409) in tumor models with diverse genetic alterations affecting the PI3K pathway

Molecular cancer therapeutics, 2014-05, Vol.13 (5), p.1078-1091

2014

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Mutations Associated with Base Excision Repair Deficiency and Methylation-Induced Genotoxic Stress

Proceedings of the National Academy of Sciences - PNAS, 2002-05, Vol.99 (10), p.6860-6865

2002

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Pharmacological Abrogation of S-Phase Checkpoint Enhances the Anti-Tumor Activity of Gemcitabine In Vivo

Cell cycle (Georgetown, Tex.), 2007-01, Vol.6 (1), p.104-110

2007

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Discovery of a Novel Series of Potent and Orally Bioavailable Phosphoinositide 3-Kinase γ Inhibitors

Journal of medicinal chemistry, 2012-06, Vol.55 (11), p.5467-5482

2012

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HER (erbB) tyrosine kinase inhibitors in the treatment of breast cancer

Seminars in oncology, 2002, Vol.29 (3), p.4-10

2002

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Epidermal growth factor receptor (HER1) tyrosine kinase inhibitor ZD1839 (Iressa) inhibits HER2/neu (erbB2)-overexpressing breast cancer cells in vitro and in vivo

Cancer research (Chicago, Ill.), 2001-12, Vol.61 (24), p.8887-8895

2001

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ErbB2/neu kinase modulates cellular p27(Kip1) and cyclin D1 through multiple signaling pathways

Cancer research (Chicago, Ill.), 2001-09, Vol.61 (17), p.6583-6591

2001

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Identification of a Novel Membrane Protein, HP59, with Therapeutic Potential as a Target of Tumor Angiogenesis

Clinical cancer research, 2001-12, Vol.7 (12), p.4182-4194

2001

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PKB/Akt mediates cell-cycle progression by phosphorylation of p27Kip1 at threonine 157 and modulation of its cellular localization

Nature medicine, 2002-10, Vol.8 (10), p.1145-1152

2002

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Pre-Clinical Activity of the Novel, First-in-Class p97 Inhibitor, CB-5083, in Multiple Myeloma

Blood, 2014-12, Vol.124 (21), p.4701-4701

2014

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Abstract 951: CB-5083 is a novel first in class p97 inhibitor that disrupts cellular protein homeostasis and demonstrates anti-tumor activity in solid and hematological models

Cancer research (Chicago, Ill.), 2014-10, Vol.74 (19_Supplement), p.951-951

2014

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Targeting the AAA ATPase p97 as an Approach to Treat Cancer through Disruption of Protein Homeostasis

Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth

The p97 Inhibitor CB-5083 Is a Unique Disrupter of Protein Homeostasis in Models of Multiple Myeloma

Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083)

Inhibition of Tumor Cell Growth, Invasion, and Metastasis by EXEL-2880 (XL880, GSK1363089), a Novel Inhibitor of HGF and VEGF Receptor Tyrosine Kinases

Loss of PTEN MMAC1 TEP in EGF receptor-expressing tumor cells counteracts the antitumor action of EGFR tyrosine kinase inhibitors

In vitro and in vivo activity of cabozantinib (XL184), an inhibitor of RET, MET, and VEGFR2, in a model of medullary thyroid cancer

Mitochondrial DNA Damage is More Extensive and Persists Longer than Nuclear DNA Damage in Human Cells Following Oxidative Stress

The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models

The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors

Hydrogen Peroxide– and Peroxynitrite-Induced Mitochondrial DNA Damage and Dysfunction in Vascular Endothelial and Smooth Muscle Cells

Inhibition of the T790M Gatekeeper Mutant of the Epidermal Growth Factor Receptor by EXEL-7647

Herceptin-induced inhibition of phosphatidylinositol-3 kinase and Akt is required for antibody-mediated effects on p27, cyclin D1, and antitumor action

PKB/Akt mediates cell-cycle progression by phosphorylation of p27(Kip1) at threonine 157 and modulation of its cellular localization

Characterization of the activity of the PI3K/mTOR inhibitor XL765 (SAR245409) in tumor models with diverse genetic alterations affecting the PI3K pathway

Mutations Associated with Base Excision Repair Deficiency and Methylation-Induced Genotoxic Stress

Pharmacological Abrogation of S-Phase Checkpoint Enhances the Anti-Tumor Activity of Gemcitabine In Vivo

Discovery of a Novel Series of Potent and Orally Bioavailable Phosphoinositide 3-Kinase γ Inhibitors

HER (erbB) tyrosine kinase inhibitors in the treatment of breast cancer

Epidermal growth factor receptor (HER1) tyrosine kinase inhibitor ZD1839 (Iressa) inhibits HER2/neu (erbB2)-overexpressing breast cancer cells in vitro and in vivo

ErbB2/neu kinase modulates cellular p27(Kip1) and cyclin D1 through multiple signaling pathways

Identification of a Novel Membrane Protein, HP59, with Therapeutic Potential as a Target of Tumor Angiogenesis

PKB/Akt mediates cell-cycle progression by phosphorylation of p27Kip1 at threonine 157 and modulation of its cellular localization

Pre-Clinical Activity of the Novel, First-in-Class p97 Inhibitor, CB-5083, in Multiple Myeloma

Abstract 951: CB-5083 is a novel first in class p97 inhibitor that disrupts cellular protein homeostasis and demonstrates anti-tumor activity in solid and hematological models

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