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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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) |
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receptor tyrosine kinases drug resistance targeted therapy cancer mutation clinical trials Biology (General) QH301-705.5 Chemistry QD1-999 |
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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? |
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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 |
work_keys_str_mv |
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_version_ |
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