Tyrosine kinases as targets for cancer therapy

A Levitzki - European journal of cancer, 2002 - Elsevier
Enhanced protein tyrosine kinase (PTK) activity correlates with the development of cancer
and other proliferative diseases. The hypothesis that PTK inhibitors may be of value in the …

Design of a selective insulin receptor tyrosine kinase inhibitor and its effect on glucose uptake and metabolism in intact cells

R Saperstein, PP Vicario, HV Strout, E Brady… - Biochemistry, 1989 - ACS Publications
Revised Manuscript Received March 22, 1989 abstract: An inhibitor of the insulin receptor
tyrosine kinase (IRTK),(hydroxy-2-naphthalenylmethyl) phosphonic acid, was designed and …

A specific inhibitor of the epidermal growth factor receptor tyrosine kinase

DW Fry, AJ Kraker, A McMichael, LA Ambroso… - Science, 1994 - science.org
A small molecule called PD 153035 inhibited the epidermal growth factor (EGF) receptor
tyrosine kinase with a 5-pM inhibition constant. The inhibitor was specific for the EGF …

[HTML][HTML] Development of new insulin-like growth factor-1 receptor kinase inhibitors using catechol mimics

G Blum, A Gazit, A Levitzki - Journal of Biological Chemistry, 2003 - ASBMB
Because insulin-like growth factor-1 (IGF-1) and its receptor play a pivotal role in many
cancers, it is an attractive target for the design of inhibitors. Here we present a new family of …

Tyrosine Kinase Inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(Phenylamino)pyrido[d]pyrimidine Acrylamides as Irreversible Inhibitors of the ATP Binding Site of …

JB Smaill, BD Palmer, GW Rewcastle… - Journal of Medicinal …, 1999 - ACS Publications
A series of 6-and 7-acrylamide derivatives of the 4-(phenylamino) quinazoline and-
pyridopyrimidine classes of epidermal growth factor receptor (EGFR) inhibitors were …

Tyrosine kinase inhibitors

MT Bilodeau, ME Fraley, RW Hungate - US Patent 6,245,759, 2001 - Google Patents
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine
kinase Signal transduction, compositions which contain these compounds, and methods of …

Tyrosine kinase inhibitors

ME Fraley, KL Arrington, MT Bilodeau… - US Patent …, 2001 - Google Patents
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine
kinase Signal transduction, compositions which contain these compounds, and methods of …

Preparation of fluoro-and hydroxy-4-(phosphonomethyl)-D, L-phenylalanine suitably protected for solid-phase synthesis of peptides containing hydrolytically stable …

TR Burke Jr, MS Smyth, M Nomizu… - The Journal of …, 1993 - ACS Publications
4-[(Di-tert-butylphosphono) methyl]-N-(fluoren-9-ylmethoxycarbonyl)-D, L-phenylalanine [O-
di-f erf-butyl-Pmp-N-Fmoc, 3] has previously been shown to be a useful reagent for the solid …

Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor …

L Sun, N Tran, F Tang, H App, P Hirth… - Journal of medicinal …, 1998 - ACS Publications
3-Substituted indolin-2-ones have been designed and synthesized as a novel class of
tyrosine kinase inhibitors which exhibit selectivity toward different receptor tyrosine kinases …

Inhibitors of tyrosine kinase

WD Klohs, DW Fry, AJ Kraker - Current opinion in oncology, 1997 - journals.lww.com
This review covers the literature on significant studies of small molecule inhibitors of the
epidermal growth factor receptor (EGF R), platelet-derived growth factor receptor (PDGF R) …