Receptor Tyrosine Kinase-Targeted Cancer Therapy

In the past two decades, several molecular targeted inhibitors have been developed and evaluated clinically to improve the survival of patients with cancer. Molecular targeted inhibitors inhibit the activities of pathogenic tyrosine kinases. Particularly, aberrant receptor tyrosine kinase (RTK) acti...

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Main Authors: Toshimitsu Yamaoka, Sojiro Kusumoto, Koichi Ando, Motoi Ohba, Tohru Ohmori
Format: Article
Language:English
Published: MDPI AG 2018-11-01
Series:International Journal of Molecular Sciences
Subjects:
Online Access:https://www.mdpi.com/1422-0067/19/11/3491
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author Toshimitsu Yamaoka
Sojiro Kusumoto
Koichi Ando
Motoi Ohba
Tohru Ohmori
author_facet Toshimitsu Yamaoka
Sojiro Kusumoto
Koichi Ando
Motoi Ohba
Tohru Ohmori
author_sort Toshimitsu Yamaoka
collection DOAJ
description In the past two decades, several molecular targeted inhibitors have been developed and evaluated clinically to improve the survival of patients with cancer. Molecular targeted inhibitors inhibit the activities of pathogenic tyrosine kinases. Particularly, aberrant receptor tyrosine kinase (RTK) activation is a potential therapeutic target. An increased understanding of genetics, cellular biology and structural biology has led to the development of numerous important therapeutics. Pathogenic RTK mutations, deletions, translocations and amplification/over-expressions have been identified and are currently being examined for their roles in cancers. Therapies targeting RTKs are categorized as small-molecule inhibitors and monoclonal antibodies. Studies are underway to explore abnormalities in 20 types of RTK subfamilies in patients with cancer or other diseases. In this review, we describe representative RTKs important for developing cancer therapeutics and predicting or evaluated resistance mechanisms.
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spelling doaj.art-5f748c95f7124f3997477a7cee2d57982022-12-22T03:33:34ZengMDPI AGInternational Journal of Molecular Sciences1422-00672018-11-011911349110.3390/ijms19113491ijms19113491Receptor Tyrosine Kinase-Targeted Cancer TherapyToshimitsu Yamaoka0Sojiro Kusumoto1Koichi Ando2Motoi Ohba3Tohru Ohmori4Advanced Cancer Translational Research Institute (Formerly, Institute of Molecular Oncology), Showa University, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo 142-8555, JapanDivision of Allergology and Respiratory Medicine, Department of Medicine, Showa University School of Medicine, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo 142-8555, JapanDivision of Allergology and Respiratory Medicine, Department of Medicine, Showa University School of Medicine, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo 142-8555, JapanAdvanced Cancer Translational Research Institute (Formerly, Institute of Molecular Oncology), Showa University, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo 142-8555, JapanDivision of Allergology and Respiratory Medicine, Department of Medicine, Showa University School of Medicine, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo 142-8555, JapanIn the past two decades, several molecular targeted inhibitors have been developed and evaluated clinically to improve the survival of patients with cancer. Molecular targeted inhibitors inhibit the activities of pathogenic tyrosine kinases. Particularly, aberrant receptor tyrosine kinase (RTK) activation is a potential therapeutic target. An increased understanding of genetics, cellular biology and structural biology has led to the development of numerous important therapeutics. Pathogenic RTK mutations, deletions, translocations and amplification/over-expressions have been identified and are currently being examined for their roles in cancers. Therapies targeting RTKs are categorized as small-molecule inhibitors and monoclonal antibodies. Studies are underway to explore abnormalities in 20 types of RTK subfamilies in patients with cancer or other diseases. In this review, we describe representative RTKs important for developing cancer therapeutics and predicting or evaluated resistance mechanisms.https://www.mdpi.com/1422-0067/19/11/3491receptor tyrosine kinasemolecular target inhibitorsresistance mechanisms
spellingShingle Toshimitsu Yamaoka
Sojiro Kusumoto
Koichi Ando
Motoi Ohba
Tohru Ohmori
Receptor Tyrosine Kinase-Targeted Cancer Therapy
International Journal of Molecular Sciences
receptor tyrosine kinase
molecular target inhibitors
resistance mechanisms
title Receptor Tyrosine Kinase-Targeted Cancer Therapy
title_full Receptor Tyrosine Kinase-Targeted Cancer Therapy
title_fullStr Receptor Tyrosine Kinase-Targeted Cancer Therapy
title_full_unstemmed Receptor Tyrosine Kinase-Targeted Cancer Therapy
title_short Receptor Tyrosine Kinase-Targeted Cancer Therapy
title_sort receptor tyrosine kinase targeted cancer therapy
topic receptor tyrosine kinase
molecular target inhibitors
resistance mechanisms
url https://www.mdpi.com/1422-0067/19/11/3491
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AT koichiando receptortyrosinekinasetargetedcancertherapy
AT motoiohba receptortyrosinekinasetargetedcancertherapy
AT tohruohmori receptortyrosinekinasetargetedcancertherapy