Double-Faced Immunological Effects of CDK4/6 Inhibitors on Cancer Treatment: Challenges and Perspectives

Cyclin-dependent kinases (CDKs) are generally involved in the progression of cell cycle and cell division in normal cells, while abnormal activations of CDKs are deemed to be a driving force for accelerating cell proliferation and tumorigenesis. Therefore, CDKs have become ideal therapeutic targets...

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Main Authors: Yongqin Liu, Yiying Deng, Chang Yang, Hua Naranmandura
Format: Article
Language:English
Published: MDPI AG 2024-10-01
Series:Bioengineering
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Online Access:https://www.mdpi.com/2306-5354/11/11/1084
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author Yongqin Liu
Yiying Deng
Chang Yang
Hua Naranmandura
author_facet Yongqin Liu
Yiying Deng
Chang Yang
Hua Naranmandura
author_sort Yongqin Liu
collection DOAJ
description Cyclin-dependent kinases (CDKs) are generally involved in the progression of cell cycle and cell division in normal cells, while abnormal activations of CDKs are deemed to be a driving force for accelerating cell proliferation and tumorigenesis. Therefore, CDKs have become ideal therapeutic targets for cancer treatment. The U.S FDA has approved three CDK4/6 inhibitors (CDK4/6is) for the treatment of patients with hormone receptor-positive (HR<sup>+</sup>) or human epidermal growth factor receptor 2-negative (HER2<sup>−</sup>) advanced or metastatic breast cancer, and these drugs showed impressive results in clinics. Besides cell-cycle arrest, there is growing evidence that CDK4/6is exert paradoxical roles on cancer treatment by altering the immune system. Indeed, clinical data showed that CDK4/6is could change the immune system to exert antitumor effects, while these changes also caused tumor resistance to CDK4/6i. However, the molecular mechanism for the regulation of the immune system by CDK4/6is is unclear. In this review, we comprehensively discuss the paradoxical immunological effects of CDK4/6is in cancer treatment, elucidating their anticancer mechanisms through immunomodulatory activity and induction of acquired drug resistance by dysregulating the immune microenvironment. More importantly, we suggest a few strategies including combining CDK4/6is with immunotherapy to overcome drug resistance.
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spelling doaj-art-3c3dead5307b4d1592dfa476970c94d82024-11-26T17:51:52ZengMDPI AGBioengineering2306-53542024-10-011111108410.3390/bioengineering11111084Double-Faced Immunological Effects of CDK4/6 Inhibitors on Cancer Treatment: Challenges and PerspectivesYongqin Liu0Yiying Deng1Chang Yang2Hua Naranmandura3Department of Public Health, Zhejiang University School of Medicine, Hangzhou 310058, ChinaDepartment of Public Health, Zhejiang University School of Medicine, Hangzhou 310058, ChinaDepartment of Public Health, Zhejiang University School of Medicine, Hangzhou 310058, ChinaDepartment of Public Health, Zhejiang University School of Medicine, Hangzhou 310058, ChinaCyclin-dependent kinases (CDKs) are generally involved in the progression of cell cycle and cell division in normal cells, while abnormal activations of CDKs are deemed to be a driving force for accelerating cell proliferation and tumorigenesis. Therefore, CDKs have become ideal therapeutic targets for cancer treatment. The U.S FDA has approved three CDK4/6 inhibitors (CDK4/6is) for the treatment of patients with hormone receptor-positive (HR<sup>+</sup>) or human epidermal growth factor receptor 2-negative (HER2<sup>−</sup>) advanced or metastatic breast cancer, and these drugs showed impressive results in clinics. Besides cell-cycle arrest, there is growing evidence that CDK4/6is exert paradoxical roles on cancer treatment by altering the immune system. Indeed, clinical data showed that CDK4/6is could change the immune system to exert antitumor effects, while these changes also caused tumor resistance to CDK4/6i. However, the molecular mechanism for the regulation of the immune system by CDK4/6is is unclear. In this review, we comprehensively discuss the paradoxical immunological effects of CDK4/6is in cancer treatment, elucidating their anticancer mechanisms through immunomodulatory activity and induction of acquired drug resistance by dysregulating the immune microenvironment. More importantly, we suggest a few strategies including combining CDK4/6is with immunotherapy to overcome drug resistance.https://www.mdpi.com/2306-5354/11/11/1084CDK4/6 inhibitorimmunomodulatory effectdrug resistanceimmune microenvironmentimmunotherapy
spellingShingle Yongqin Liu
Yiying Deng
Chang Yang
Hua Naranmandura
Double-Faced Immunological Effects of CDK4/6 Inhibitors on Cancer Treatment: Challenges and Perspectives
Bioengineering
CDK4/6 inhibitor
immunomodulatory effect
drug resistance
immune microenvironment
immunotherapy
title Double-Faced Immunological Effects of CDK4/6 Inhibitors on Cancer Treatment: Challenges and Perspectives
title_full Double-Faced Immunological Effects of CDK4/6 Inhibitors on Cancer Treatment: Challenges and Perspectives
title_fullStr Double-Faced Immunological Effects of CDK4/6 Inhibitors on Cancer Treatment: Challenges and Perspectives
title_full_unstemmed Double-Faced Immunological Effects of CDK4/6 Inhibitors on Cancer Treatment: Challenges and Perspectives
title_short Double-Faced Immunological Effects of CDK4/6 Inhibitors on Cancer Treatment: Challenges and Perspectives
title_sort double faced immunological effects of cdk4 6 inhibitors on cancer treatment challenges and perspectives
topic CDK4/6 inhibitor
immunomodulatory effect
drug resistance
immune microenvironment
immunotherapy
url https://www.mdpi.com/2306-5354/11/11/1084
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AT yiyingdeng doublefacedimmunologicaleffectsofcdk46inhibitorsoncancertreatmentchallengesandperspectives
AT changyang doublefacedimmunologicaleffectsofcdk46inhibitorsoncancertreatmentchallengesandperspectives
AT huanaranmandura doublefacedimmunologicaleffectsofcdk46inhibitorsoncancertreatmentchallengesandperspectives