Journal ArticleDOI
Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent.
Doriano Fabbro,Elisabeth Buchdunger,Jeannette Wood,Jürgen Mestan,Francesco Hofmann,Stefano Ferrari,Helmut Mett,Terence O'reilly,Thomas Meyer +8 more
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TLDR
CGP 41251 showed in vivo antitumor activity as single agent and inhibited angiogenesis in vivo, and is able to reverse the p-glycoprotein-mediated multidrug resistance of tumor cells in vitro, showing broad antiproliferative activity against various tumor and normal cell lines in vitro.About:
This article is published in Pharmacology & Therapeutics.The article was published on 1999-05-01. It has received 125 citations till now. The article focuses on the topics: Growth factor receptor & Growth factor receptor inhibitor.read more
Citations
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The influence of natural products upon drug discovery.
Journal ArticleDOI
Dissecting Temporal and Spatial Control of Cytokinesis with a Myosin II Inhibitor
Aaron F. Straight,Amy Cheung,John Limouze,Irene A. Chen,Nicholas J. Westwood,James R. Sellers,Timothy J. Mitchison +6 more
TL;DR: It is shown that exit from the cytokinetic phase of the cell cycle depends on ubiquitin-mediated proteolysis and continuous signals from microtubules are required to maintain the position of the cleavage furrow, and these signals control the localization of myosin II independently of other furrow components.
Journal ArticleDOI
VEGF Receptor Signaling in Tumor Angiogenesis
TL;DR: The growth of human tumors and development of metastases depend on the de novo formation of blood vessels, and inhibition of the VEGF tyrosine kinase signaling pathway blocks new blood vessel formation in growing tumors, leading to stasis or regression of tumor growth.
Journal ArticleDOI
Patients with acute myeloid leukemia and an activating mutation in FLT3 respond to a small-molecule FLT3 tyrosine kinase inhibitor, PKC412
Richard Stone,Daniel J. DeAngelo,Virginia M. Klimek,Ilene Galinsky,Eli Estey,Stephen D. Nimer,Wilson Grandin,David Lebwohl,Yanfeng Wang,Pamela S. Cohen,Edward A. Fox,Donna Neuberg,Jennifer J. Clark,D. Gary Gilliland,James D. Griffin +14 more
TL;DR: KC412 is an oral tyrosine kinase inhibitor with clinical activity in patients with AML whose blasts have an activating mutation of FLT3, suggesting potential use in combination with active agents, such as chemotherapy.
Journal ArticleDOI
Natural products in cancer chemotherapy: past, present and future
TL;DR: The quickening pace of (aberrant) gene identification, and the new technologies of combinatorial chemistry and high-throughput screening, should provide access to a wide range of new, totally synthetic drugs.
References
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Journal Article
Nucleotide sequence and expression of a novel human receptor-type tyrosine kinase gene (flt) closely related to the fms family.
Masabumi Shibuya,Sachiko Yamaguchi,Akira Yamane,Toshio Ikeda,Arinobu Tojo,Hitoshi Matsushime,Misako Sato +6 more
TL;DR: A new human gene encoding a receptor-type tyrosine kinase was isolated by a weak cross-hybridization with v-ros oncogene and designated as flt (fms-like tyrosin kinase) gene, which was strongly suppressed in most of the tumor cell lines examined so far.
Journal ArticleDOI
Protein kinase C - a question of specificity
TL;DR: This review focuses on the heterogeneity within the PKC family and highlights some of the recent evidence that the isotypes might have separate and unique functions in the cell.
Journal ArticleDOI
Overexpression of vascular permeability factor/vascular endothelial growth factor and its receptors in psoriasis
Michael Detmar,Lawrence F. Brown,Kevin P. Claffey,Kiang-Teck J. Yeo,Olivier Kocher,Robert W. Jackman,Brygida Berse,Harold F. Dvorak +7 more
TL;DR: It is reported here that the hyperplastic epidermis of psoriatic skin expresses strikingly increased amounts of vascular permeability factor (VPF; vascular endothelial growth factor), a selective endothelial cell mitogen that enhances microvascular permeability.
Journal Article
Identification of a new endothelial cell growth factor receptor tyrosine kinase
TL;DR: A new growth factor receptor tyrosine kinase (RTK) gene (designated KDR) has been cloned from a human endothelial cell cDNA library, and is expressed as a 7.0 kb transcript and localized to human chromosome 4.
Journal ArticleDOI
Vascular endothelial growth factor is essential for corpus luteum angiogenesis
Napoleone Ferrara,Helen Hsifei Chen,Terri Lynn Davis-Smyth,Hans-Peter Gerber,Thuy-Nhung Nguyen,David H. Peers,Vanessa Chisholm,Kenneth J. Hillan,Ralph H. Schwall +8 more
TL;DR: The unexpected finding that treatment with truncated soluble Flt-1 receptors, which inhibit vascular endothelial growth factor (VEGF) bioac-tivity, resulted in virtually complete suppression of CL angiogenesis in a rat model of hormonally induced ovulation is reported.
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