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CDK4/6 inhibitors: a brief overview and prospective research directions
The discovery of cyclin-dependent kinases (CDK) and their mechanism in regulating the cell cycle process was considered a game-changer in cancer therapy. Cell cycle arrest and apoptosis were both triggered by their inhibition. The CDK4/6 complex acts as a checkpoint during the cell cycle transition...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
The Royal Society of Chemistry
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9040853/ https://www.ncbi.nlm.nih.gov/pubmed/35479560 http://dx.doi.org/10.1039/d1ra03820f |
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author | Adon, Tenzin Shanmugarajan, Dhivya Kumar, Honnavalli Yogish |
author_facet | Adon, Tenzin Shanmugarajan, Dhivya Kumar, Honnavalli Yogish |
author_sort | Adon, Tenzin |
collection | PubMed |
description | The discovery of cyclin-dependent kinases (CDK) and their mechanism in regulating the cell cycle process was considered a game-changer in cancer therapy. Cell cycle arrest and apoptosis were both triggered by their inhibition. The CDK4/6 complex acts as a checkpoint during the cell cycle transition from cell growth (G1) to DNA synthesis (S) phase and its deregulation or overexpression induces abnormal cell proliferation and cancer development. Consequently, targeting CDK4/6 has been proposed as a paradigm shift in the anticancer approach. The design and development of effective CDK4/6 inhibitors are increasingly becoming a promising cancer therapy evident with approved drugs such as palbociclib, ribociclib, and abemaciclib, etc. In this article, we explore the biological importance of CDK4/6 in cancer therapy, the development of resistance to monotherapy, and a short overview of PROTAC (Proteolysis Targeting Chimera), a unique and pioneering technique for degrading CDK4/6 enzymes. Overall, our prime focus is to discuss novel CDK4/6 inhibitors with diverse chemical classes and their correlation with computational studies. |
format | Online Article Text |
id | pubmed-9040853 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | The Royal Society of Chemistry |
record_format | MEDLINE/PubMed |
spelling | pubmed-90408532022-04-26 CDK4/6 inhibitors: a brief overview and prospective research directions Adon, Tenzin Shanmugarajan, Dhivya Kumar, Honnavalli Yogish RSC Adv Chemistry The discovery of cyclin-dependent kinases (CDK) and their mechanism in regulating the cell cycle process was considered a game-changer in cancer therapy. Cell cycle arrest and apoptosis were both triggered by their inhibition. The CDK4/6 complex acts as a checkpoint during the cell cycle transition from cell growth (G1) to DNA synthesis (S) phase and its deregulation or overexpression induces abnormal cell proliferation and cancer development. Consequently, targeting CDK4/6 has been proposed as a paradigm shift in the anticancer approach. The design and development of effective CDK4/6 inhibitors are increasingly becoming a promising cancer therapy evident with approved drugs such as palbociclib, ribociclib, and abemaciclib, etc. In this article, we explore the biological importance of CDK4/6 in cancer therapy, the development of resistance to monotherapy, and a short overview of PROTAC (Proteolysis Targeting Chimera), a unique and pioneering technique for degrading CDK4/6 enzymes. Overall, our prime focus is to discuss novel CDK4/6 inhibitors with diverse chemical classes and their correlation with computational studies. The Royal Society of Chemistry 2021-09-01 /pmc/articles/PMC9040853/ /pubmed/35479560 http://dx.doi.org/10.1039/d1ra03820f Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by-nc/3.0/ |
spellingShingle | Chemistry Adon, Tenzin Shanmugarajan, Dhivya Kumar, Honnavalli Yogish CDK4/6 inhibitors: a brief overview and prospective research directions |
title | CDK4/6 inhibitors: a brief overview and prospective research directions |
title_full | CDK4/6 inhibitors: a brief overview and prospective research directions |
title_fullStr | CDK4/6 inhibitors: a brief overview and prospective research directions |
title_full_unstemmed | CDK4/6 inhibitors: a brief overview and prospective research directions |
title_short | CDK4/6 inhibitors: a brief overview and prospective research directions |
title_sort | cdk4/6 inhibitors: a brief overview and prospective research directions |
topic | Chemistry |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9040853/ https://www.ncbi.nlm.nih.gov/pubmed/35479560 http://dx.doi.org/10.1039/d1ra03820f |
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