Inhibition of epidermal growth factor-induced DNA synthesis by tyrosine kinase inhibitors

Kazuo Umezawa; Takashi Hori; Hirohisa Tajima; Masaya Imoto; Kunio Isshiki; Tomio Takeuchi

doi:10.1016/0014-5793(90)80102-O

Inhibition of epidermal growth factor-induced DNA synthesis by tyrosine kinase inhibitors

Kazuo Umezawa, Takashi Hori, Hirohisa Tajima, Masaya Imoto, Kunio Isshiki, Tomio Takeuchi

Research output: Contribution to journal › Article › peer-review

1 Citation (Scopus)

Abstract

We prepared methyl 2,5-dihydroxycinnamate as a stable analogue of erbstatin, a tyrosine kinase inhibitor. This analogue was about 4 times more stable than erbstatin in calf serum. It inhibited epidermal growth factor receptor-associated tyrosine kinase in vitro with an IC₅₀ of 0.15 μg ml. It also inhibited in situ autophosphorylation of epidermal growth factor receptor in A431 cells. Methyl 2,5-dihydroxycinnamate was shown to delay the S-phase induction by epidermal growth factor in quiescent normal rat kidney cells, without affecting the total amount ofDNA synthesis. The effect of erbstatin on S-phase induction was smaller, possibly because of its shorter life time.

Original language	English
Pages (from-to)	198-200
Number of pages	3
Journal	FEBS Letters
Volume	260
Issue number	2
DOIs	https://doi.org/10.1016/0014-5793(90)80102-O
Publication status	Published - 1990 Jan 29
Externally published	Yes

Keywords

(Normal rat kidney cell)
Cell cycle
DNA synthesis
Epidermal growth factor
Erbstatin

ASJC Scopus subject areas

Biophysics
Structural Biology
Biochemistry
Molecular Biology
Genetics
Cell Biology

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10.1016/0014-5793(90)80102-O

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title = "Inhibition of epidermal growth factor-induced DNA synthesis by tyrosine kinase inhibitors",

abstract = "We prepared methyl 2,5-dihydroxycinnamate as a stable analogue of erbstatin, a tyrosine kinase inhibitor. This analogue was about 4 times more stable than erbstatin in calf serum. It inhibited epidermal growth factor receptor-associated tyrosine kinase in vitro with an IC50 of 0.15 μg ml. It also inhibited in situ autophosphorylation of epidermal growth factor receptor in A431 cells. Methyl 2,5-dihydroxycinnamate was shown to delay the S-phase induction by epidermal growth factor in quiescent normal rat kidney cells, without affecting the total amount ofDNA synthesis. The effect of erbstatin on S-phase induction was smaller, possibly because of its shorter life time.",

keywords = "(Normal rat kidney cell), Cell cycle, DNA synthesis, Epidermal growth factor, Erbstatin",

author = "Kazuo Umezawa and Takashi Hori and Hirohisa Tajima and Masaya Imoto and Kunio Isshiki and Tomio Takeuchi",

note = "Funding Information: AcknowledgementTsh: is work was partly supportedb y a Grant-in-Aid for theC omprehensivleO -yearS trategyfo r CancerC ontrol from the Ministry of Healtha nd Welfareo f Japan and by a grantf rom the Foundationf or Promotion of CancerR esearch( Japan).",

year = "1990",

month = jan,

day = "29",

doi = "10.1016/0014-5793(90)80102-O",

language = "English",

volume = "260",

pages = "198--200",

journal = "FEBS Letters",

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T1 - Inhibition of epidermal growth factor-induced DNA synthesis by tyrosine kinase inhibitors

AU - Umezawa, Kazuo

AU - Hori, Takashi

AU - Tajima, Hirohisa

AU - Imoto, Masaya

AU - Isshiki, Kunio

AU - Takeuchi, Tomio

N1 - Funding Information: AcknowledgementTsh: is work was partly supportedb y a Grant-in-Aid for theC omprehensivleO -yearS trategyfo r CancerC ontrol from the Ministry of Healtha nd Welfareo f Japan and by a grantf rom the Foundationf or Promotion of CancerR esearch( Japan).

PY - 1990/1/29

Y1 - 1990/1/29

N2 - We prepared methyl 2,5-dihydroxycinnamate as a stable analogue of erbstatin, a tyrosine kinase inhibitor. This analogue was about 4 times more stable than erbstatin in calf serum. It inhibited epidermal growth factor receptor-associated tyrosine kinase in vitro with an IC50 of 0.15 μg ml. It also inhibited in situ autophosphorylation of epidermal growth factor receptor in A431 cells. Methyl 2,5-dihydroxycinnamate was shown to delay the S-phase induction by epidermal growth factor in quiescent normal rat kidney cells, without affecting the total amount ofDNA synthesis. The effect of erbstatin on S-phase induction was smaller, possibly because of its shorter life time.

AB - We prepared methyl 2,5-dihydroxycinnamate as a stable analogue of erbstatin, a tyrosine kinase inhibitor. This analogue was about 4 times more stable than erbstatin in calf serum. It inhibited epidermal growth factor receptor-associated tyrosine kinase in vitro with an IC50 of 0.15 μg ml. It also inhibited in situ autophosphorylation of epidermal growth factor receptor in A431 cells. Methyl 2,5-dihydroxycinnamate was shown to delay the S-phase induction by epidermal growth factor in quiescent normal rat kidney cells, without affecting the total amount ofDNA synthesis. The effect of erbstatin on S-phase induction was smaller, possibly because of its shorter life time.

KW - (Normal rat kidney cell)

KW - Cell cycle

KW - DNA synthesis

KW - Epidermal growth factor

KW - Erbstatin

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DO - 10.1016/0014-5793(90)80102-O

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VL - 260

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EP - 200

JO - FEBS Letters

JF - FEBS Letters

IS - 2

ER -

Inhibition of epidermal growth factor-induced DNA synthesis by tyrosine kinase inhibitors

Abstract

Keywords

ASJC Scopus subject areas

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