Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors

A Gazit, P Yaish, C Gilon, A Levitzki - Journal of medicinal …, 1989 - ACS Publications
A novel class of low molecular weight protein tyrosine kinase inhibitors is described. These
compounds constitute a systematic series of molecules with a progressive increase in affinity …

Tyrphostins. II. Heterocyclic and. alpha.-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases

A Gazit, N Osherov, I Posner, P Yaish… - Journal of medicinal …, 1991 - ACS Publications
In recent years it has become apparent that protein tyrosine kinases (PTKs) mediate
proliferative signals as well as metabolic signals. 1 This realization promoted the hypothesis …

[29] Inhibition of protein-tyrosine kinases by tyrphostins

A Levitzki, A Gazit, N Osherov, I Posner, C Gilon - Methods in enzymology, 1991 - Elsevier
Publisher Summary This chapter discusses the inhibition of protein-tyrosine kinases by
tyrphostins. Many protein tyrosine kinases (PTKs) catalyze the phosphorylation of tyrosine …

Specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins

M Párrizas, A Gazit, A Levitzki, E Wertheimer… - …, 1997 - academic.oup.com
A series of the synthetic protein tyrosine kinase inhibitors known as tyrphostins were studied
for their effect on insulin-like growth factor-1 and insulin-stimulated cellular proliferation on …

Tyrphostins inhibit epidermal growth factor (EGF)-receptor tyrosine kinase activity in living cells and EGF-stimulated cell proliferation

RM Lyall, A Zilberstein, A Gazit, C Gilon… - Journal of Biological …, 1989 - ASBMB
Synthetic compounds called tyrphostins were examined for their effects on cells which are
mitogenically responsive to epidermal growth factor (EGF). We studied in detail the effects of …

Tyrphostins: tyrosine kinase blockers as novel antiproliferative agents and dissectors of signal transduction

A Levitzki - The FASEB journal, 1992 - Wiley Online Library
Protein tyrosine kinases (PTKs) are members of a growing family of oncoproteins and
protooncoproteins that play a pivotal role in normal and abnormal proliferative processes …

The Antiproliferative Effects of Tyrosine Kinase Inhibitors Tyrphostins on a Human Squamous Cell Carcinoma in Vitro and in Nude Mice

T Yoneda, RM Lyall, MM Alsina, PE Persons… - Cancer Research, 1991 - AACR
Many human tumors of epithelial origin contain cells overexpressing the epidermal growth
factor (EGF) receptor, and there is convincing evidence that cancer cell growth is correlated …

The tyrosine kinase inhibitor tyrphostin blocks the cellular actions of nerve growth factor

M Ohmichi, L Pang, V Ribon, A Gazit, A Levitzki… - Biochemistry, 1993 - ACS Publications
Revised Manuscript Received February 2, 1993 abstract: A series of the synthetic protein
kinase inhibitors known as tyrphostins were examined for their effects on the tyrosine …

Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: structure− activity relationships in quinoxalines, quinolines, and indole …

A Gazit, H App, G McMahon, J Chen… - Journal of medicinal …, 1996 - ACS Publications
A series of 3-indoleacrylonitrile tyrphostins, 2-chloro-3-phenylquinolines, and 3-
arylquinoxalines were prepared and tested for inhibition of platelet-derived growth factor …

[引用][C] Tyrphostins IV—highly potent inhibitors of EGF receptor kinase. Structure-activity relationship study of 4-anilidoquinazolines

A Gazit, J Chen, H App, G McMahon, P Hirth… - Bioorganic & Medicinal …, 1996 - Elsevier
H~NN JR Page 1 Pergamon Bioorganic & Medicinal Chemistry, Vol. 4, No. 8, pp 1203-1207,
1996 Copyright © 1996 Elsevier Science Ltd Printed in Great Britain. All rights reserved PII …