DOI: 10.1126/science.3263702. Blocking of EGF-Dependent Cell Proliferation by EGF Receptor Kinase Inhibitors

Blocking of EGF-Dependent Cell Proliferation by EGF Receptor Kinase Inhibitors

10.1126/science.3263702

Crossref journal-article

American Association for the Advancement of Science (AAAS)

Science (221)

Abstract

A systematic series of low molecular weight protein tyrosine kinase inhibitors were synthesized; they had progressively increasing affinity over a 2500-fold range toward the substrate site of epidermal growth factor (EGF) receptor kinase domain. These compounds inhibited EGF receptor kinase activity up to three orders of magnitude more than they inhibited insulin receptor kinase, and they also effectively inhibited the EGF-dependent autophosphorylation of the receptor. The most potent compounds effectively inhibited the EGF-dependent proliferation of A431/clone 15 cells with little or no effect on the EGF-independent proliferation of these cells. The potential use of tyrosine protein kinase inhibitors as antiproliferative agents is demonstrated.

Bibliography

Yaish, P., Gazit, A., Gilon, C., & Levitzki, A. (1988). Blocking of EGF-Dependent Cell Proliferation by EGF Receptor Kinase Inhibitors. Science, 242(4880), 933â935.

Authors 4

Pnina Yaish (first)
Aviv Gazit (additional)
Chaim Gilon (additional)
Alexander Levitzki (additional)

References 19 Referenced 453

AKIYAMA, T, GENISTEIN, A SPECIFIC INHIBITOR OF TYROSINE-SPECIFIC PROTEIN-KINASES, JOURNAL OF BIOLOGICAL CHEMISTRY 262: 5592 (1987). (10.1016/S0021-9258(18)45614-1) / JOURNAL OF BIOLOGICAL CHEMISTRY (1987)
BRAUN, S, SYNTHETIC TYROSINE POLYMERS AS SUBSTRATES AND INHIBITORS OF TYROSINE-SPECIFIC PROTEIN-KINASES, JOURNAL OF BIOLOGICAL CHEMISTRY 259: 2051 (1984). (10.1016/S0021-9258(17)43311-4) / JOURNAL OF BIOLOGICAL CHEMISTRY (1984)
BRAVO, R, STIMULATION AND INHIBITION OF GROWTH BY EGF IN DIFFERENT A431 CELL CLONES IS ACCOMPANIED BY THE RAPID INDUCTION OF C-FOS AND C-MYC PROTO-ONCOGENES, EMBO JOURNAL 4: 1193 (1985). (10.1002/j.1460-2075.1985.tb03759.x) / EMBO JOURNAL (1985)
CARPENTER, G, RECEPTORS FOR EPIDERMAL GROWTH-FACTOR AND OTHER POLYPEPTIDE MITOGENS, ANNUAL REVIEW OF BIOCHEMISTRY 56: 881 (1987). (10.1146/annurev.bi.56.070187.004313) / ANNUAL REVIEW OF BIOCHEMISTRY (1987)
CHEN, W.S., REQUIREMENT FOR INTRINSIC PROTEIN TYROSINE KINASE IN THE IMMEDIATE AND LATE ACTIONS OF THE EGF RECEPTOR, NATURE 328: 820 (1987). (10.1038/328820a0) / NATURE (1987)
DIXON, M, THE DETERMINATION OF ENZYME INHIBITOR CONSTANTS, BIOCHEMICAL JOURNAL 55: 170 (1953). (10.1042/bj0550170) / BIOCHEMICAL JOURNAL (1953)
EK, B, STIMULATION OF TYROSINE-SPECIFIC PHOSPHORYLATION BY PLATELET-DERIVED GROWTH-FACTOR, NATURE 295: 419 (1982). (10.1038/295419a0) / NATURE (1982)
GLOSSMANN, H, QUERCETIN INHIBITS TYROSINE PHOSPHORYLATION BY THE CYCLIC NUCLEOTIDE-INDEPENDENT, TRANSFORMING PROTEIN-KINASE, PP60SRC, NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY 317: 100 (1981). (10.1007/BF00506266) / NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY (1981)
GRAZIANI, Y, THE EFFECT OF QUERCETIN ON THE PHOSPHORYLATION ACTIVITY OF THE ROUS-SARCOMA VIRUS TRANSFORMING GENE-PRODUCT INVITRO AND INVIVO, EUROPEAN JOURNAL OF BIOCHEMISTRY 135: 583 (1983). (10.1111/j.1432-1033.1983.tb07692.x) / EUROPEAN JOURNAL OF BIOCHEMISTRY (1983)
HELDIN, C.H., SUBVERSION OF GROWTH REGULATORY PATHWAYS IN MALIGNANT TRANSFORMATION, BIOCHIMICA ET BIOPHYSICA ACTA 907: 219 (1987). / BIOCHIMICA ET BIOPHYSICA ACTA (1987)
HONEGGER, A.M., A MUTANT EPIDERMAL GROWTH-FACTOR RECEPTOR WITH DEFECTIVE PROTEIN TYROSINE KINASE IS UNABLE TO STIMULATE PROTOONCOGENE EXPRESSION AND DNA-SYNTHESIS, MOLECULAR AND CELLULAR BIOLOGY 7: 4568 (1987). / MOLECULAR AND CELLULAR BIOLOGY (1987)
10.1126/science.7031900
LEHNINGER, A, PRINCIPLES BIOCH: 225 (1982). / PRINCIPLES BIOCH (1982)
RIEDEL, H, A CHIMERIC RECEPTOR ALLOWS INSULIN TO STIMULATE TYROSINE KINASE-ACTIVITY OF EPIDERMAL GROWTH-FACTOR RECEPTOR, NATURE 324: 68 (1986). (10.1038/324068a0) / NATURE (1986)
10.1126/science.2442814
SCHECHTER Y unpublished data.
UMEZAWA, H, STUDIES ON A NEW EPIDERMAL GROWTH FACTOR-RECEPTOR KINASE INHIBITOR, ERBSTATIN, PRODUCED BY MH435-HF3, JOURNAL OF ANTIBIOTICS 39: 170 (1986). (10.7164/antibiotics.39.170) / JOURNAL OF ANTIBIOTICS (1986)
YARDEN, Y, SELF-PHOSPHORYLATION OF EPIDERMAL GROWTH-FACTOR RECEPTOR - EVIDENCE FOR A MODEL OF INTERMOLECULAR ALLOSTERIC ACTIVATION, BIOCHEMISTRY 26: 1434 (1987). (10.1021/bi00379a034) / BIOCHEMISTRY (1987)
YARDEN, Y, A NONMITOGENIC ANALOG OF EPIDERMAL GROWTH-FACTOR INDUCES EARLY RESPONSES MEDIATED BY EPIDERMAL GROWTH-FACTOR, JOURNAL OF CELL BIOLOGY 92: 687 (1982). (10.1083/jcb.92.3.687) / JOURNAL OF CELL BIOLOGY (1982)

Dates

Type	When
Created	18 years, 10 months ago (Oct. 5, 2006, 5:21 p.m.)
Deposited	1 year, 7 months ago (Jan. 13, 2024, 10:24 p.m.)
Indexed	3 weeks, 4 days ago (Aug. 2, 2025, 12:24 a.m.)
Issued	36 years, 9 months ago (Nov. 11, 1988)
Published	36 years, 9 months ago (Nov. 11, 1988)
Published Print	36 years, 9 months ago (Nov. 11, 1988)

Funders 0

None

BibTeX

@article{Yaish_1988, title={Blocking of EGF-Dependent Cell Proliferation by EGF Receptor Kinase Inhibitors}, volume={242}, ISSN={1095-9203}, url={http://dx.doi.org/10.1126/science.3263702}, DOI={10.1126/science.3263702}, number={4880}, journal={Science}, publisher={American Association for the Advancement of Science (AAAS)}, author={Yaish, Pnina and Gazit, Aviv and Gilon, Chaim and Levitzki, Alexander}, year={1988}, month=nov, pages={933–935} }

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