Emerging Importance of Tyrosine Kinase Inhibitors against Cancer: Quo Vadis to Cure?

GLOBOCAN 2020 estimated more than 19.3 million new cases, and about 10 million patients were deceased from cancer in 2020. Clinical manifestations showed that several growth factor receptors consisting of transmembrane and cytoplasmic tyrosine kinase (TK) domains play a vital role in cancer progress...

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Autores principales: Raj Kumar Mongre, Chandra Bhushan Mishra, Arvind Kumar Shukla, Amresh Prakash, Samil Jung, Md Ashraf-Uz-Zaman, Myeong-Sok Lee
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Publicado: MDPI AG 2021
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Acceso en línea:https://doaj.org/article/f7e4e2d1c4f14ffe8d65c0a026304786
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spelling oai:doaj.org-article:f7e4e2d1c4f14ffe8d65c0a0263047862021-11-11T17:07:44ZEmerging Importance of Tyrosine Kinase Inhibitors against Cancer: Quo Vadis to Cure?10.3390/ijms2221116591422-00671661-6596https://doaj.org/article/f7e4e2d1c4f14ffe8d65c0a0263047862021-10-01T00:00:00Zhttps://www.mdpi.com/1422-0067/22/21/11659https://doaj.org/toc/1661-6596https://doaj.org/toc/1422-0067GLOBOCAN 2020 estimated more than 19.3 million new cases, and about 10 million patients were deceased from cancer in 2020. Clinical manifestations showed that several growth factor receptors consisting of transmembrane and cytoplasmic tyrosine kinase (TK) domains play a vital role in cancer progression. Receptor tyrosine kinases (RTKs) are crucial intermediaries of the several cellular pathways and carcinogenesis that directly affect the prognosis and survival of higher tumor grade patients. Tyrosine kinase inhibitors (TKIs) are efficacious drugs for targeted therapy of various cancers. Therefore, RTKs have become a promising therapeutic target to cure cancer. A recent report shows that TKIs are vital mediators of signal transduction and cancer cell proliferation, angiogenesis, and apoptosis. In this review, we discuss the structure and function of RTKs to explore their prime role in cancer therapy. Various TKIs have been developed to date that contribute a lot to treating several types of cancer. These TKI based anticancer drug molecules are also discussed in detail, incorporating their therapeutic efficacy, mechanism of action, and side effects. Additionally, this article focuses on TKIs which are running in the clinical trial and pre-clinical studies. Further, to gain insight into the pathophysiological mechanism of TKIs, we also reviewed the impact of RTK resistance on TKI clinical drugs along with their mechanistic acquired resistance in different cancer types.Raj Kumar MongreChandra Bhushan MishraArvind Kumar ShuklaAmresh PrakashSamil JungMd Ashraf-Uz-ZamanMyeong-Sok LeeMDPI AGarticlereceptor tyrosine kinasesdrug resistancetargeted therapycancermutationclinical trialsBiology (General)QH301-705.5ChemistryQD1-999ENInternational Journal of Molecular Sciences, Vol 22, Iss 11659, p 11659 (2021)
institution DOAJ
collection DOAJ
language EN
topic receptor tyrosine kinases
drug resistance
targeted therapy
cancer
mutation
clinical trials
Biology (General)
QH301-705.5
Chemistry
QD1-999
spellingShingle receptor tyrosine kinases
drug resistance
targeted therapy
cancer
mutation
clinical trials
Biology (General)
QH301-705.5
Chemistry
QD1-999
Raj Kumar Mongre
Chandra Bhushan Mishra
Arvind Kumar Shukla
Amresh Prakash
Samil Jung
Md Ashraf-Uz-Zaman
Myeong-Sok Lee
Emerging Importance of Tyrosine Kinase Inhibitors against Cancer: Quo Vadis to Cure?
description GLOBOCAN 2020 estimated more than 19.3 million new cases, and about 10 million patients were deceased from cancer in 2020. Clinical manifestations showed that several growth factor receptors consisting of transmembrane and cytoplasmic tyrosine kinase (TK) domains play a vital role in cancer progression. Receptor tyrosine kinases (RTKs) are crucial intermediaries of the several cellular pathways and carcinogenesis that directly affect the prognosis and survival of higher tumor grade patients. Tyrosine kinase inhibitors (TKIs) are efficacious drugs for targeted therapy of various cancers. Therefore, RTKs have become a promising therapeutic target to cure cancer. A recent report shows that TKIs are vital mediators of signal transduction and cancer cell proliferation, angiogenesis, and apoptosis. In this review, we discuss the structure and function of RTKs to explore their prime role in cancer therapy. Various TKIs have been developed to date that contribute a lot to treating several types of cancer. These TKI based anticancer drug molecules are also discussed in detail, incorporating their therapeutic efficacy, mechanism of action, and side effects. Additionally, this article focuses on TKIs which are running in the clinical trial and pre-clinical studies. Further, to gain insight into the pathophysiological mechanism of TKIs, we also reviewed the impact of RTK resistance on TKI clinical drugs along with their mechanistic acquired resistance in different cancer types.
format article
author Raj Kumar Mongre
Chandra Bhushan Mishra
Arvind Kumar Shukla
Amresh Prakash
Samil Jung
Md Ashraf-Uz-Zaman
Myeong-Sok Lee
author_facet Raj Kumar Mongre
Chandra Bhushan Mishra
Arvind Kumar Shukla
Amresh Prakash
Samil Jung
Md Ashraf-Uz-Zaman
Myeong-Sok Lee
author_sort Raj Kumar Mongre
title Emerging Importance of Tyrosine Kinase Inhibitors against Cancer: Quo Vadis to Cure?
title_short Emerging Importance of Tyrosine Kinase Inhibitors against Cancer: Quo Vadis to Cure?
title_full Emerging Importance of Tyrosine Kinase Inhibitors against Cancer: Quo Vadis to Cure?
title_fullStr Emerging Importance of Tyrosine Kinase Inhibitors against Cancer: Quo Vadis to Cure?
title_full_unstemmed Emerging Importance of Tyrosine Kinase Inhibitors against Cancer: Quo Vadis to Cure?
title_sort emerging importance of tyrosine kinase inhibitors against cancer: quo vadis to cure?
publisher MDPI AG
publishDate 2021
url https://doaj.org/article/f7e4e2d1c4f14ffe8d65c0a026304786
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