Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug
R Capdeville, E Buchdunger, J Zimmermann… - Nature reviews Drug …, 2002 - nature.com
In the early 1980s, it became apparent that the work of pioneers such as Robert Weinberg,
Mariano Barbacid and many others in identifying cancer-causing genes in humans was …
Mariano Barbacid and many others in identifying cancer-causing genes in humans was …
The development of imatinib as a therapeutic agent for chronic myeloid leukemia
M Deininger, E Buchdunger, BJ Druker - Blood, 2005 - ashpublications.org
Imatinib has revolutionized drug therapy of chronic myeloid leukemia (CML). Preclinical
studies were promising but the results of clinical trials by far exceeded expectations …
studies were promising but the results of clinical trials by far exceeded expectations …
Small cell lung cancer
T Sher, GK Dy, AA Adjei - Mayo Clinic Proceedings, 2008 - Elsevier
Small cell lung cancer accounts for approximately 15% of bronchogenic carcinomas. It is the
cancer most commonly associated with various paraneoplastic syndromes, including the …
cancer most commonly associated with various paraneoplastic syndromes, including the …
Abl protein-tyrosine kinase inhibitor STI571 inhibits in vitro signal transduction mediated by c-kit and platelet-derived growth factor receptors
E Buchdunger, CL Cioffi, N Law, D Stover… - … of Pharmacology and …, 2000 - ASPET
STI571 (formerly known as CGP 57148B) is a protein-tyrosine kinase inhibitor that is
currently in clinical trials for the treatment of chronic myelogenous leukemia. STI571 …
currently in clinical trials for the treatment of chronic myelogenous leukemia. STI571 …
Imatinib mesylate—a new oral targeted therapy
DG Savage, KH Antman - New England Journal of Medicine, 2002 - Mass Medical Soc
This review discusses the development and uses of imatinib mesylate, a protein tyrosine
kinase inhibitor useful in the treatment of chronic myelogenous leukemia and …
kinase inhibitor useful in the treatment of chronic myelogenous leukemia and …
E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on …
J Matsui, Y Yamamoto, Y Funahashi… - … journal of cancer, 2008 - Wiley Online Library
E7080 is an orally active inhibitor of multiple receptor tyrosine kinases including VEGF, FGF
and SCF receptors. In this study, we show the inhibitory activity of E7080 against SCF …
and SCF receptors. In this study, we show the inhibitory activity of E7080 against SCF …
KIT (CD117): a review on expression in normal and neoplastic tissues, and mutations and their clinicopathologic correlation
M Miettinen, J Lasota - Applied immunohistochemistry & molecular …, 2005 - journals.lww.com
CD117 (KIT) is a type III receptor tyrosine kinase operating in cell signal transduction in
several cell types. Normally KIT is activated (phosphorylated) by binding of its ligand, the …
several cell types. Normally KIT is activated (phosphorylated) by binding of its ligand, the …
SU11248 inhibits KIT and platelet-derived growth factor receptor β in preclinical models of human small cell lung cancer
TJ Abrams, LB Lee, LJ Murray, NK Pryer… - Molecular cancer …, 2003 - AACR
The purpose of this study was to evaluate the activity of the indolinone kinase inhibitor
SU11248 against the receptor tyrosine kinase KIT in vitro and in vivo, examine the role of …
SU11248 against the receptor tyrosine kinase KIT in vitro and in vivo, examine the role of …
STI571 inactivation of the gastrointestinal stromal tumor c-KIT oncoprotein: biological and clinical implications
Mutations in the c-KIT receptor occur somatically in many sporadic Gastrointestinal Stromal
Tumors (GIST), and similar mutations have been identified at the germline level in kindreds …
Tumors (GIST), and similar mutations have been identified at the germline level in kindreds …
Inhibition of KIT tyrosine kinase activity: a novel molecular approach to the treatment of KIT-positive malignancies
MC Heinrich, CD Blanke, BJ Druker… - Journal of clinical …, 2002 - ascopubs.org
PURPOSE: Activation of the KIT tyrosine kinase by somatic mutation has been documented
in a number of human malignancies, including gastrointestinal stromal tumor (GIST) …
in a number of human malignancies, including gastrointestinal stromal tumor (GIST) …