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Tyrosine Kinase ROR1 as a Target for Anti-Cancer Therapies

Receptor tyrosine kinase ROR1 plays an essential role in embryogenesis and is overexpressed in many types of malignant tumors. Studies have demonstrated that it plays an important role in oncogenesis by activating cell survival signaling events, particularly the non-canonical WNT signaling pathway....

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Detalles Bibliográficos
Autores principales: Zhao, Yuming, Zhang, Dengyang, Guo, Yao, Lu, Bo, Zhao, Zhizhuang Joe, Xu, Xiaojun, Chen, Yun
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8193947/
https://www.ncbi.nlm.nih.gov/pubmed/34123850
http://dx.doi.org/10.3389/fonc.2021.680834
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author Zhao, Yuming
Zhang, Dengyang
Guo, Yao
Lu, Bo
Zhao, Zhizhuang Joe
Xu, Xiaojun
Chen, Yun
author_facet Zhao, Yuming
Zhang, Dengyang
Guo, Yao
Lu, Bo
Zhao, Zhizhuang Joe
Xu, Xiaojun
Chen, Yun
author_sort Zhao, Yuming
collection PubMed
description Receptor tyrosine kinase ROR1 plays an essential role in embryogenesis and is overexpressed in many types of malignant tumors. Studies have demonstrated that it plays an important role in oncogenesis by activating cell survival signaling events, particularly the non-canonical WNT signaling pathway. Antibody-based immunotherapies targeting ROR1 have been developed and evaluated in preclinical and clinical studies with promising outcomes. However, small molecule inhibitors targeting ROR1 are underappreciated because of the initial characterization of ROR1 as a peusdokinase. The function of ROR1 as a tyrosine kinase remains poorly understood, although accumulating evidence have demonstrated its intrinsic tyrosine kinase activity. In this review, we analyzed the structural and functional features of ROR1 and discussed therapeutic strategies targeting this kinase.
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spelling pubmed-81939472021-06-12 Tyrosine Kinase ROR1 as a Target for Anti-Cancer Therapies Zhao, Yuming Zhang, Dengyang Guo, Yao Lu, Bo Zhao, Zhizhuang Joe Xu, Xiaojun Chen, Yun Front Oncol Oncology Receptor tyrosine kinase ROR1 plays an essential role in embryogenesis and is overexpressed in many types of malignant tumors. Studies have demonstrated that it plays an important role in oncogenesis by activating cell survival signaling events, particularly the non-canonical WNT signaling pathway. Antibody-based immunotherapies targeting ROR1 have been developed and evaluated in preclinical and clinical studies with promising outcomes. However, small molecule inhibitors targeting ROR1 are underappreciated because of the initial characterization of ROR1 as a peusdokinase. The function of ROR1 as a tyrosine kinase remains poorly understood, although accumulating evidence have demonstrated its intrinsic tyrosine kinase activity. In this review, we analyzed the structural and functional features of ROR1 and discussed therapeutic strategies targeting this kinase. Frontiers Media S.A. 2021-05-28 /pmc/articles/PMC8193947/ /pubmed/34123850 http://dx.doi.org/10.3389/fonc.2021.680834 Text en Copyright © 2021 Zhao, Zhang, Guo, Lu, Zhao, Xu and Chen https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Oncology
Zhao, Yuming
Zhang, Dengyang
Guo, Yao
Lu, Bo
Zhao, Zhizhuang Joe
Xu, Xiaojun
Chen, Yun
Tyrosine Kinase ROR1 as a Target for Anti-Cancer Therapies
title Tyrosine Kinase ROR1 as a Target for Anti-Cancer Therapies
title_full Tyrosine Kinase ROR1 as a Target for Anti-Cancer Therapies
title_fullStr Tyrosine Kinase ROR1 as a Target for Anti-Cancer Therapies
title_full_unstemmed Tyrosine Kinase ROR1 as a Target for Anti-Cancer Therapies
title_short Tyrosine Kinase ROR1 as a Target for Anti-Cancer Therapies
title_sort tyrosine kinase ror1 as a target for anti-cancer therapies
topic Oncology
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8193947/
https://www.ncbi.nlm.nih.gov/pubmed/34123850
http://dx.doi.org/10.3389/fonc.2021.680834
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