A potent inhibitor of platelet-derived growth factor receptor tyrosine kinase

Do Sik Min, Young Han Lee, Lin Woo Kang, Chang Hyoun Byoun, Jong Soo Chang, Sung Ho Ryu, Pann Ghill Suh

Research output: Contribution to journalArticle

Abstract

To find inhibitors that block the PDGF receptor-mediated mitogenic signal, we have established a screening system using NIH 3T3 cells (3T3-γ1) that overexpress PLC-γ1. The 3T3-γ1 cells formed 10 times more inositol phosphates than, the control cells by PDGF treatment Using this system, various herb extracts have been examined inhibitory effects for PDGF receptor mediated signalling. Among the medicinal plant extracts tested, the extract of Rhus javanica showed the highest level of inhibition and was selected as a source of potent inhibitory materials. The extract was fractionated with organic solvents and on C-18 HPLC column. Effects of the inhibitory fraction on the growth signal pathway was examined. The inhibitory effect of the fraction on the protein tyrosine kinase activity of the PDGF receptor correlated with inhibition of PDGF-dependent inositol phosphate formation and tyrosine phosphorylation of PLC-γ1. The inhibitory fraction, however, did not affect response to EGF in A431 cell, a ligand whose receptor also possesses intrinsic tyrosine kinase. These results suggest that the fraction from the extracts of Rhus javanica contains a specific inhibitor on PDGF-dependent growth signalling.

Original languageEnglish
Pages (from-to)463-468
Number of pages6
JournalMolecules and cells
Volume6
Issue number4
Publication statusPublished - 1996 Aug 31

Fingerprint

Platelet-Derived Growth Factor Receptors
Rhus
Inositol Phosphates
Protein-Tyrosine Kinases
3T3 Cells
NIH 3T3 Cells
Plant Extracts
Medicinal Plants
Growth
Epidermal Growth Factor
Tyrosine
Signal Transduction
High Pressure Liquid Chromatography
Phosphorylation
Ligands
PDGF receptor tyrosine kinase

All Science Journal Classification (ASJC) codes

  • Molecular Biology
  • Cell Biology

Cite this

Min, D. S., Lee, Y. H., Kang, L. W., Byoun, C. H., Chang, J. S., Ryu, S. H., & Suh, P. G. (1996). A potent inhibitor of platelet-derived growth factor receptor tyrosine kinase. Molecules and cells, 6(4), 463-468.
Min, Do Sik ; Lee, Young Han ; Kang, Lin Woo ; Byoun, Chang Hyoun ; Chang, Jong Soo ; Ryu, Sung Ho ; Suh, Pann Ghill. / A potent inhibitor of platelet-derived growth factor receptor tyrosine kinase. In: Molecules and cells. 1996 ; Vol. 6, No. 4. pp. 463-468.
@article{fdf9c7da1ce7475985342b0d60e07e69,
title = "A potent inhibitor of platelet-derived growth factor receptor tyrosine kinase",
abstract = "To find inhibitors that block the PDGF receptor-mediated mitogenic signal, we have established a screening system using NIH 3T3 cells (3T3-γ1) that overexpress PLC-γ1. The 3T3-γ1 cells formed 10 times more inositol phosphates than, the control cells by PDGF treatment Using this system, various herb extracts have been examined inhibitory effects for PDGF receptor mediated signalling. Among the medicinal plant extracts tested, the extract of Rhus javanica showed the highest level of inhibition and was selected as a source of potent inhibitory materials. The extract was fractionated with organic solvents and on C-18 HPLC column. Effects of the inhibitory fraction on the growth signal pathway was examined. The inhibitory effect of the fraction on the protein tyrosine kinase activity of the PDGF receptor correlated with inhibition of PDGF-dependent inositol phosphate formation and tyrosine phosphorylation of PLC-γ1. The inhibitory fraction, however, did not affect response to EGF in A431 cell, a ligand whose receptor also possesses intrinsic tyrosine kinase. These results suggest that the fraction from the extracts of Rhus javanica contains a specific inhibitor on PDGF-dependent growth signalling.",
author = "Min, {Do Sik} and Lee, {Young Han} and Kang, {Lin Woo} and Byoun, {Chang Hyoun} and Chang, {Jong Soo} and Ryu, {Sung Ho} and Suh, {Pann Ghill}",
year = "1996",
month = "8",
day = "31",
language = "English",
volume = "6",
pages = "463--468",
journal = "Molecules and Cells",
issn = "1016-8478",
publisher = "Korean Society for Molecular and Cellular Biology",
number = "4",

}

Min, DS, Lee, YH, Kang, LW, Byoun, CH, Chang, JS, Ryu, SH & Suh, PG 1996, 'A potent inhibitor of platelet-derived growth factor receptor tyrosine kinase', Molecules and cells, vol. 6, no. 4, pp. 463-468.

A potent inhibitor of platelet-derived growth factor receptor tyrosine kinase. / Min, Do Sik; Lee, Young Han; Kang, Lin Woo; Byoun, Chang Hyoun; Chang, Jong Soo; Ryu, Sung Ho; Suh, Pann Ghill.

In: Molecules and cells, Vol. 6, No. 4, 31.08.1996, p. 463-468.

Research output: Contribution to journalArticle

TY - JOUR

T1 - A potent inhibitor of platelet-derived growth factor receptor tyrosine kinase

AU - Min, Do Sik

AU - Lee, Young Han

AU - Kang, Lin Woo

AU - Byoun, Chang Hyoun

AU - Chang, Jong Soo

AU - Ryu, Sung Ho

AU - Suh, Pann Ghill

PY - 1996/8/31

Y1 - 1996/8/31

N2 - To find inhibitors that block the PDGF receptor-mediated mitogenic signal, we have established a screening system using NIH 3T3 cells (3T3-γ1) that overexpress PLC-γ1. The 3T3-γ1 cells formed 10 times more inositol phosphates than, the control cells by PDGF treatment Using this system, various herb extracts have been examined inhibitory effects for PDGF receptor mediated signalling. Among the medicinal plant extracts tested, the extract of Rhus javanica showed the highest level of inhibition and was selected as a source of potent inhibitory materials. The extract was fractionated with organic solvents and on C-18 HPLC column. Effects of the inhibitory fraction on the growth signal pathway was examined. The inhibitory effect of the fraction on the protein tyrosine kinase activity of the PDGF receptor correlated with inhibition of PDGF-dependent inositol phosphate formation and tyrosine phosphorylation of PLC-γ1. The inhibitory fraction, however, did not affect response to EGF in A431 cell, a ligand whose receptor also possesses intrinsic tyrosine kinase. These results suggest that the fraction from the extracts of Rhus javanica contains a specific inhibitor on PDGF-dependent growth signalling.

AB - To find inhibitors that block the PDGF receptor-mediated mitogenic signal, we have established a screening system using NIH 3T3 cells (3T3-γ1) that overexpress PLC-γ1. The 3T3-γ1 cells formed 10 times more inositol phosphates than, the control cells by PDGF treatment Using this system, various herb extracts have been examined inhibitory effects for PDGF receptor mediated signalling. Among the medicinal plant extracts tested, the extract of Rhus javanica showed the highest level of inhibition and was selected as a source of potent inhibitory materials. The extract was fractionated with organic solvents and on C-18 HPLC column. Effects of the inhibitory fraction on the growth signal pathway was examined. The inhibitory effect of the fraction on the protein tyrosine kinase activity of the PDGF receptor correlated with inhibition of PDGF-dependent inositol phosphate formation and tyrosine phosphorylation of PLC-γ1. The inhibitory fraction, however, did not affect response to EGF in A431 cell, a ligand whose receptor also possesses intrinsic tyrosine kinase. These results suggest that the fraction from the extracts of Rhus javanica contains a specific inhibitor on PDGF-dependent growth signalling.

UR - http://www.scopus.com/inward/record.url?scp=21944432905&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=21944432905&partnerID=8YFLogxK

M3 - Article

AN - SCOPUS:21944432905

VL - 6

SP - 463

EP - 468

JO - Molecules and Cells

JF - Molecules and Cells

SN - 1016-8478

IS - 4

ER -

Min DS, Lee YH, Kang LW, Byoun CH, Chang JS, Ryu SH et al. A potent inhibitor of platelet-derived growth factor receptor tyrosine kinase. Molecules and cells. 1996 Aug 31;6(4):463-468.