Research Topics
| D B MendelSummaryAffiliation: Preclinical Research and Exploratory Development Country: USA Publications
| Collaborators
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Detail Information
Publications
Development of SU5416, a selective small molecule inhibitor of VEGF receptor tyrosine kinase activity, as an anti-angiogenesis agentD B Mendel
SUGEN, Inc, South San Francisco, CA 94080, USA
Anticancer Drug Des 15:29-41. 2000..Its biochemical, biological and pharmacological properties are reviewed and clinical implications discussed...- The angiogenesis inhibitor SU5416 has long-lasting effects on vascular endothelial growth factor receptor phosphorylation and functionD B Mendel
SUGEN, Inc, South San Francisco, California 94080, USA
Clin Cancer Res 6:4848-58. 2000..The long-lasting inhibitory activity of SU5416 in vitro is consistent with the finding that SU5416 has demonstrated evidence of biological activity in clinical studies when administered twice a week despite a short plasma half-life... - In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationshipDirk B Mendel
Preclinical Research and Exploratory Development, SUGEN, Inc, South San Francisco, California 94080, USA
Clin Cancer Res 9:327-37. 2003..The pharmacokinetic/pharmacodynamic relationship established for SU11248 in these preclinical studies has aided in the design, selection, and evaluation of dosing regimens being tested in human trials... - High levels of HER-2 expression alter the ability of epidermal growth factor receptor (EGFR) family tyrosine kinase inhibitors to inhibit EGFR phosphorylation in vivoJ G Christensen
SUGEN, Inc, 230 East Grand Avenue, South San Francisco, CA 94080, USA
Clin Cancer Res 7:4230-8. 2001..The potential clinical implications of this observation are discussed... 
Conversion of 1-[((S)-2-hydroxy-2-oxo-1,4,2-dioxaphosphorinan-5-yl)methyl]cytosine to cidofovir by an intracellular cyclic CMP phosphodiesteraseD B Mendel
Gilead Sciences, Inc, Foster City, California 94404, USA
Antimicrob Agents Chemother 41:641-6. 1997..Importantly, hydrolysis of cHPMPC is not diminished in cells infected with HCMV...- CHIR-258 is efficacious in a newly developed fibroblast growth factor receptor 3-expressing orthotopic multiple myeloma model in miceXiaohua Xin
Translational Sciences, Chiron Corporation, Emeryville, California, USA
Clin Cancer Res 12:4908-15. 2006..CONCLUSIONS: Our data provide a relevant preclinical basis for clinical trials of CHIR-258 in FGFR3-positive MM patients... - SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activityShem Patyna
Pfizer Global Research and Development, 10777 Science Center Drive, San Diego, CA 92024, USA
Mol Cancer Ther 5:1774-82. 2006..These data support the ongoing phase I clinical evaluation of SU14813 in advanced malignancies... - Contribution of individual targets to the antitumor efficacy of the multitargeted receptor tyrosine kinase inhibitor SU11248Olga Potapova
Cureline, Inc, 393 East Grand Avenue, Suite I, South San Francisco, CA 94080, USA
Mol Cancer Ther 5:1280-9. 2006.... - A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivoJames G Christensen
Preclinical Research and Exploratory Development, SUGEN, Inc, South San Francisco, CA 94080, USA
Cancer Res 63:7345-55. 2003..Collectively, these results demonstrate the feasibility of selectively targeting c-Met with ATP-competitive small-molecules and suggest the therapeutic potential of targeting c-Met in human cancers... - Hair depigmentation is a biological readout for pharmacological inhibition of KIT in mice and humansKatherine G Moss
Department of Preclinical Research and Exploratory Development, SUGEN Inc, South San Francisco, CA, USA
J Pharmacol Exp Ther 307:476-80. 2003..These data demonstrate that hair pigmentation can serve as a dose-dependent, dynamic, biological readout for KIT inhibition in mice, and, apparently, in humans... - Phase I dose-escalating study of SU11654, a small molecule receptor tyrosine kinase inhibitor, in dogs with spontaneous malignanciesCheryl A London
School of Veterinary Medicine, University of California, Davis, Davis, California 95616, USA
Clin Cancer Res 9:2755-68. 2003..Given the similarities of canine and human cancers with regard to tumor biology and the presence of analogous RTK dysregulation, it is likely that such agents will demonstrate comparable antineoplastic activity in people... - Src family kinase activity is required for signal tranducer and activator of transcription 3 and focal adhesion kinase phosphorylation and vascular endothelial growth factor signaling in vivo and for anchorage-dependent and -independent growth of human tuA Douglas Laird
Preclinical Research and Exploratory Development, SUGEN, Inc, South San Francisco, California 94080, USA
Mol Cancer Ther 2:461-9. 2003..These data demonstrate that STAT3 (Y705) and FAK (Y861) phosphoepitopes are SFK-dependent in tumor cells and reveal a requirement for SFK function in tumor cell proliferation and vascular permeability... - Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitorsAlbert T Liao
Department of Surgical and Radiological Sciences, School of Veterinary Medicine, University of California at Davis, CA 95616, USA
Blood 100:585-93. 2002..Because the concentrations of drug necessary for receptor inhibition are readily achievable and nontoxic in vivo, these compounds may be useful in the treatment of spontaneous cancers expressing Kit mutations... - SU6668 inhibits Flk-1/KDR and PDGFRbeta in vivo, resulting in rapid apoptosis of tumor vasculature and tumor regression in miceA Douglas Laird
SUGEN, Inc, Preclinical Research and Translational Medicine, South San Francisco, California 94080, USA
FASEB J 16:681-90. 2002..These data demonstrate that SU6668-induced inhibition of angiogenic receptor tyrosine kinase activity in vivo is associated with rapid vessel killing in tumors, leading to broad and potent antitumor effects... - Novel robust hepatitis C virus mouse efficacy modelQing Zhu
Department of Pharmacology, Novartis Vaccines and Diagnostics, Chiron Corportion, Emeryville, CA 94608
Antimicrob Agents Chemother 50:3260-8. 2006..This robust mouse efficacy model provides a powerful tool for rapid evaluation of potential anti-HCV compounds in vivo as part of aggressive drug discovery efforts...