Advances in the structural biology, design and clinical development of VEGF-R kinase inhibitors for the treatment of angiogenesis

Tumor Angiogenesis: Therapeutic Implications

1971 • 9,898 citations

The Protein Kinase Complement of the Human Genome

2002 • 7,708 citations

Vascular Endothelial Growth Factor Is a Secreted Angiogenic Mitogen

1989 • 4,988 citations

Tumorigenesis and the angiogenic switch

2003 • 3,398 citations

A Randomized Trial of Bevacizumab, an Anti–Vascular Endothelial Growth Factor Antibody, for Metastatic Renal Cancer

2003 • 2,723 citations

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 relationship.

2003 • 1,939 citations

Phase II, Randomized Trial Comparing Bevacizumab Plus Fluorouracil (FU)/Leucovorin (LV) With FU/LV Alone in Patients With Metastatic Colorectal Cancer

2002 • 1,699 citations

The Conformational Plasticity of Protein Kinases

2002 • 1,691 citations

Basement membranes: structure, assembly and role in tumour angiogenesis

2003 • 1,652 citations

VEGF-Trap: A VEGF blocker with potent antitumor effects

2002 • 1,641 citations

Clinical translation of angiogenesis inhibitors

2002 • 1,518 citations

Continuous low-dose therapy with vinblastine and VEGF receptor-2 antibody induces sustained tumor regression without overt toxicity

2000 • 1,159 citations

Crystal structure of the tyrosine kinase domain of the human insulin receptor

1994 • 1,071 citations

Role of vascular endothelial growth factor in regulation of physiological angiogenesis

2001 • 1,068 citations

Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571).

2002 • 925 citations

PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration.

2000 • 848 citations

Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site

2002 • 818 citations

ZD6474 inhibits vascular endothelial growth factor signaling, angiogenesis, and tumor growth following oral administration.

2002 • 784 citations

Vasculogenic mimicry and tumour-cell plasticity: lessons from melanoma

2003 • 781 citations

Role of PlGF in the intra- and intermolecular cross talk between the VEGF receptors Flt1 and Flk1

2003 • 758 citations

Dynamic Contrast-Enhanced Magnetic Resonance Imaging As a Biomarker for the Pharmacological Response of PTK787/ZK 222584, an Inhibitor of the Vascular Endothelial Growth Factor Receptor Tyrosine Kinases, in Patients With Advanced Colorectal Cancer and Liver Metastases: Results From Two Phase I Studies

2003 • 651 citations

Issues and progress with protein kinase inhibitors for cancer treatment

2003 • 529 citations

Discovery of 5-[5-Fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic Acid (2-Diethylaminoethyl)amide, a Novel Tyrosine Kinase Inhibitor Targeting Vascular Endothelial and Platelet-Derived Growth Factor Receptor Tyrosine Kinase

2003 • 498 citations

Antitumor effects of ZD6474, a small molecule vascular endothelial growth factor receptor tyrosine kinase inhibitor, with additional activity against epidermal growth factor receptor tyrosine kinase.

2003 • 318 citations

Vascular endothelial growth factor: A new member of the platelet-derived growth factor gene family

1989 • 308 citations

Novel 4-Anilinoquinazolines with C-7 Basic Side Chains: Design and Structure Activity Relationship of a Series of Potent, Orally Active, VEGF Receptor Tyrosine Kinase Inhibitors

2002 • 308 citations

Dose-Finding and Pharmacokinetic Study of Cisplatin, Gemcitabine, and SU5416 in Patients With Solid Tumors

2002 • 253 citations

Development of SU5416, a selective small molecule inhibitor of VEGF receptor tyrosine kinase activity, as an anti-angiogenesis agent.

2000 • 237 citations

New Anilinophthalazines as Potent and Orally Well Absorbed Inhibitors of the VEGF Receptor Tyrosine Kinases Useful as Antagonists of Tumor-Driven Angiogenesis

2000 • 214 citations

PTK787/ZK 222584, a specific vascular endothelial growth factor-receptor tyrosine kinase inhibitor, affects the anatomy of the tumor vascular bed and the functional vascular properties as detected by dynamic enhanced magnetic resonance imaging.

2002 • 207 citations

Crystal structure of the kinase domain of human vascular endothelial growth factor receptor 2: a key enzyme in angiogenesis

1999 • 196 citations

Results of a Phase I dose-escalating study of the antiangiogenic agent, SU5416, in patients with advanced malignancies.

2002 • 152 citations

Dose-Finding and Pharmacokinetic Study of Cisplatin, Gemcitabine, and SU5416 in Patients With Solid Tumors

2002 • 126 citations

Efficacy and toxicity of the angiogenesis inhibitor SU5416 as a single agent in patients with advanced renal cell carcinoma, melanoma, and soft tissue sarcoma.

2003 • 126 citations

Inhibition of vascular endothelial growth factor in the treatment of colorectal cancer

2003 • 107 citations

Bcr-Abl inhibition as a modality of CML therapeutics

2001 • 104 citations

Anthranilic Acid Amides: A Novel Class of Antiangiogenic VEGF Receptor Kinase Inhibitors

2002 • 102 citations

Vascular endothelial growth factor receptor tyrosine kinase inhibitors: PTK787/ZK 222584

2003 • 99 citations

Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching

2003 • 61 citations

Vascular endothelial growth factor receptor tyrosine kinase inhibitors: PTK787/ZK 222584

2003 • 54 citations

Inhibition of vascular endothelial growth factor in the treatment of colorectal cancer

2003 • 54 citations

The Snark is a Boojum: the continuing problem of drug resistance in the antiangiogenic era

2002 • 38 citations

Light-Dark-Shift Stress, With Special Reference to Spontaneous Tumor Incidence in Female BN Rats<xref ref-type="fn" rid="FN2">2</xref>

1986 • 22 citations

Su-6668. SUGEN.

2001 • 21 citations

CGP 79787D (PTK787/ZK222584), CGP 84738, NVP-AAC789, NVP-AAD777 and related 1-anilino-(4-pyridylmethyl)phthalazines as inhibitors of VEGF- and bFGF-induced angiogenesis

2002 • 18 citations

Capecitabine/Bevacizumab Compared to Capecitabine Alone in Pretreated Metastatic Breast Cancer: Results of a Phase III Study)

2003 • 11 citations

Effects of ZD6474, an orally active inhibitor of VEGF receptor tyrosine kinase, in patients with solid tumors: Results from a phase I study

2001 • 2 citations