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Article: Blockage of epidermal growth factor receptor by quinazoline tyrosine kinase inhibitors suppresses growth of human hepatocellular carcinoma

TitleBlockage of epidermal growth factor receptor by quinazoline tyrosine kinase inhibitors suppresses growth of human hepatocellular carcinoma
Authors
KeywordsApoptosis
Cell cycle
Epidermal growth factor receptor inhibitors
Hepatocellular carcinoma
Proliferation
Issue Date2007
PublisherElsevier Ireland Ltd. The Journal's web site is located at http://www.elsevier.com/locate/canlet
Citation
Cancer Letters, 2007, v. 248 n. 1, p. 32-40 How to Cite?
AbstractEpidermal growth factor receptor (EGFR) is highly expressed in many human tumors including hepatocellular carcinoma (HCC). Therefore, inhibition of EGF receptors could be a potential target for anticancer therapy. In this study, we investigated the effects of two EGFR tyrosine kinase inhibitors, PD153035 and its analogue 4-[[3-chloro-4-fluorophenyl]amino]-6,7-dimethoxyquinazoline hydrochloride (ANAPD) on human HCC cell lines by cell proliferation assay, flow cytometry and Western blot. Our results demonstrated that both EGFR inhibitors inhibited tumor cell growth in a dose-dependent manner, but ANAPD was more potent than PD153035. These specific inhibitors not only blocked EGF-stimulated EGFR autophosphorylation but also targeted EGFR signaling including MAPK and Akt pathways. Furthermore, EGFR inhibitors induced a delay in cell cycle progression and a G 1 arrest together with a partial G 2/M block. EGFR inhibitors also induced tumor cells to undergo apoptosis. In conclusion, this study demonstrated that both PD153035 and ANAPD inhibit tumor cell growth in HCC through inhibition of EGFR signaling pathway, and ANAPD is a more potent inhibitor than PD153035. This suggested that blockage of EGF receptors may provide an effective therapeutic approach for human HCC and ANAPD could be a potential drug candidate for the treatment of HCC. © 2006 Elsevier Ireland Ltd. All rights reserved.
Persistent Identifierhttp://hdl.handle.net/10722/83661
ISSN
2015 Impact Factor: 5.992
2015 SCImago Journal Rankings: 2.331
ISI Accession Number ID
References

 

DC FieldValueLanguage
dc.contributor.authorLiu, Yen_HK
dc.contributor.authorPoon, RTPen_HK
dc.contributor.authorShao, Wen_HK
dc.contributor.authorSun, Xen_HK
dc.contributor.authorChen, Hen_HK
dc.contributor.authorKok, TWen_HK
dc.contributor.authorFan, STen_HK
dc.date.accessioned2010-09-06T08:43:41Z-
dc.date.available2010-09-06T08:43:41Z-
dc.date.issued2007en_HK
dc.identifier.citationCancer Letters, 2007, v. 248 n. 1, p. 32-40en_HK
dc.identifier.issn0304-3835en_HK
dc.identifier.urihttp://hdl.handle.net/10722/83661-
dc.description.abstractEpidermal growth factor receptor (EGFR) is highly expressed in many human tumors including hepatocellular carcinoma (HCC). Therefore, inhibition of EGF receptors could be a potential target for anticancer therapy. In this study, we investigated the effects of two EGFR tyrosine kinase inhibitors, PD153035 and its analogue 4-[[3-chloro-4-fluorophenyl]amino]-6,7-dimethoxyquinazoline hydrochloride (ANAPD) on human HCC cell lines by cell proliferation assay, flow cytometry and Western blot. Our results demonstrated that both EGFR inhibitors inhibited tumor cell growth in a dose-dependent manner, but ANAPD was more potent than PD153035. These specific inhibitors not only blocked EGF-stimulated EGFR autophosphorylation but also targeted EGFR signaling including MAPK and Akt pathways. Furthermore, EGFR inhibitors induced a delay in cell cycle progression and a G 1 arrest together with a partial G 2/M block. EGFR inhibitors also induced tumor cells to undergo apoptosis. In conclusion, this study demonstrated that both PD153035 and ANAPD inhibit tumor cell growth in HCC through inhibition of EGFR signaling pathway, and ANAPD is a more potent inhibitor than PD153035. This suggested that blockage of EGF receptors may provide an effective therapeutic approach for human HCC and ANAPD could be a potential drug candidate for the treatment of HCC. © 2006 Elsevier Ireland Ltd. All rights reserved.en_HK
dc.languageengen_HK
dc.publisherElsevier Ireland Ltd. The Journal's web site is located at http://www.elsevier.com/locate/canleten_HK
dc.relation.ispartofCancer Lettersen_HK
dc.rightsCancer Letters. Copyright © Elsevier Ireland Ltd.en_HK
dc.subjectApoptosisen_HK
dc.subjectCell cycleen_HK
dc.subjectEpidermal growth factor receptor inhibitorsen_HK
dc.subjectHepatocellular carcinomaen_HK
dc.subjectProliferationen_HK
dc.titleBlockage of epidermal growth factor receptor by quinazoline tyrosine kinase inhibitors suppresses growth of human hepatocellular carcinomaen_HK
dc.typeArticleen_HK
dc.identifier.openurlhttp://library.hku.hk:4550/resserv?sid=HKU:IR&issn=0304-3835&volume=248&issue=1&spage=32&epage=40&date=2007&atitle=Blockage+of+epidermal+growth+factor+receptor+by+quinazoline+tyrosine+kinase+inhibitors+suppresses+growth+of+human+hepatocellular+carcinomaen_HK
dc.identifier.emailPoon, RTP: poontp@hkucc.hku.hken_HK
dc.identifier.emailFan, ST: stfan@hku.hken_HK
dc.identifier.authorityPoon, RTP=rp00446en_HK
dc.identifier.authorityFan, ST=rp00355en_HK
dc.description.naturelink_to_subscribed_fulltext-
dc.identifier.doi10.1016/j.canlet.2006.05.018en_HK
dc.identifier.pmid16837130-
dc.identifier.scopuseid_2-s2.0-33847261640en_HK
dc.identifier.hkuros126246en_HK
dc.relation.referenceshttp://www.scopus.com/mlt/select.url?eid=2-s2.0-33847261640&selection=ref&src=s&origin=recordpageen_HK
dc.identifier.volume248en_HK
dc.identifier.issue1en_HK
dc.identifier.spage32en_HK
dc.identifier.epage40en_HK
dc.identifier.isiWOS:000245401600004-
dc.publisher.placeIrelanden_HK
dc.identifier.scopusauthoridLiu, Y=14627533300en_HK
dc.identifier.scopusauthoridPoon, RTP=7103097223en_HK
dc.identifier.scopusauthoridShao, W=35075059600en_HK
dc.identifier.scopusauthoridSun, X=8530833400en_HK
dc.identifier.scopusauthoridChen, H=26642984400en_HK
dc.identifier.scopusauthoridKok, TW=36851058500en_HK
dc.identifier.scopusauthoridFan, ST=7402678224en_HK

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