Small molecule inhibitors targeting the cancers

Abstract Compared with traditional therapies, targeted therapy has merits in selectivity, efficacy, and tolerability. Small molecule inhibitors are one of the primary targeted therapies for cancer. Due to their advantages in a wide range of targets, convenient medication, and the ability to penetrat...

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Main Authors: Gui‐Hong Liu, Tao Chen, Xin Zhang, Xue‐Lei Ma, Hua‐Shan Shi
Format: Article
Language:English
Published: Wiley 2022-12-01
Series:MedComm
Subjects:
Online Access:https://doi.org/10.1002/mco2.181
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author Gui‐Hong Liu
Tao Chen
Xin Zhang
Xue‐Lei Ma
Hua‐Shan Shi
author_facet Gui‐Hong Liu
Tao Chen
Xin Zhang
Xue‐Lei Ma
Hua‐Shan Shi
author_sort Gui‐Hong Liu
collection DOAJ
description Abstract Compared with traditional therapies, targeted therapy has merits in selectivity, efficacy, and tolerability. Small molecule inhibitors are one of the primary targeted therapies for cancer. Due to their advantages in a wide range of targets, convenient medication, and the ability to penetrate into the central nervous system, many efforts have been devoted to developing more small molecule inhibitors. To date, 88 small molecule inhibitors have been approved by the United States Food and Drug Administration to treat cancers. Despite remarkable progress, small molecule inhibitors in cancer treatment still face many obstacles, such as low response rate, short duration of response, toxicity, biomarkers, and resistance. To better promote the development of small molecule inhibitors targeting cancers, we comprehensively reviewed small molecule inhibitors involved in all the approved agents and pivotal drug candidates in clinical trials arranged by the signaling pathways and the classification of small molecule inhibitors. We discussed lessons learned from the development of these agents, the proper strategies to overcome resistance arising from different mechanisms, and combination therapies concerned with small molecule inhibitors. Through our review, we hoped to provide insights and perspectives for the research and development of small molecule inhibitors in cancer treatment.
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spelling doaj.art-2f790a45ef474ccf97e61be61a3f3ad62022-12-22T04:41:01ZengWileyMedComm2688-26632022-12-0134n/an/a10.1002/mco2.181Small molecule inhibitors targeting the cancersGui‐Hong Liu0Tao Chen1Xin Zhang2Xue‐Lei Ma3Hua‐Shan Shi4Department of Biotherapy State Key Laboratory of Biotherapy Cancer Center, West China Hospital Sichuan University Chengdu ChinaDepartment of Cardiology The First Affiliated Hospital of China Medical University Shenyang Liaoning ChinaDepartment of Biotherapy State Key Laboratory of Biotherapy Cancer Center, West China Hospital Sichuan University Chengdu ChinaDepartment of Biotherapy State Key Laboratory of Biotherapy Cancer Center, West China Hospital Sichuan University Chengdu ChinaDepartment of Biotherapy State Key Laboratory of Biotherapy Cancer Center, West China Hospital Sichuan University Chengdu ChinaAbstract Compared with traditional therapies, targeted therapy has merits in selectivity, efficacy, and tolerability. Small molecule inhibitors are one of the primary targeted therapies for cancer. Due to their advantages in a wide range of targets, convenient medication, and the ability to penetrate into the central nervous system, many efforts have been devoted to developing more small molecule inhibitors. To date, 88 small molecule inhibitors have been approved by the United States Food and Drug Administration to treat cancers. Despite remarkable progress, small molecule inhibitors in cancer treatment still face many obstacles, such as low response rate, short duration of response, toxicity, biomarkers, and resistance. To better promote the development of small molecule inhibitors targeting cancers, we comprehensively reviewed small molecule inhibitors involved in all the approved agents and pivotal drug candidates in clinical trials arranged by the signaling pathways and the classification of small molecule inhibitors. We discussed lessons learned from the development of these agents, the proper strategies to overcome resistance arising from different mechanisms, and combination therapies concerned with small molecule inhibitors. Through our review, we hoped to provide insights and perspectives for the research and development of small molecule inhibitors in cancer treatment.https://doi.org/10.1002/mco2.181combination therapymultikinase molecule inhibitorsresistancesmall molecule inhibitorssmall molecule kinase inhibitors
spellingShingle Gui‐Hong Liu
Tao Chen
Xin Zhang
Xue‐Lei Ma
Hua‐Shan Shi
Small molecule inhibitors targeting the cancers
MedComm
combination therapy
multikinase molecule inhibitors
resistance
small molecule inhibitors
small molecule kinase inhibitors
title Small molecule inhibitors targeting the cancers
title_full Small molecule inhibitors targeting the cancers
title_fullStr Small molecule inhibitors targeting the cancers
title_full_unstemmed Small molecule inhibitors targeting the cancers
title_short Small molecule inhibitors targeting the cancers
title_sort small molecule inhibitors targeting the cancers
topic combination therapy
multikinase molecule inhibitors
resistance
small molecule inhibitors
small molecule kinase inhibitors
url https://doi.org/10.1002/mco2.181
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