Palbociclib as an Antitumor Drug: A License to Kill
Neoplastic cells are characterized by uncontrolled cell divisions caused by cell cycle dysregulation. Key regulatory proteins governing the transition from the G1 to the S phase are the CDK4 and CDK6 kinases, which are controlled by D-type cyclins. The CDK4/6 kinases enable the use of these proteins...
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MDPI AG
2024-11-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/29/22/5334 |
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| author | Agnieszka Łupicka-Słowik Federica Cossu Marcin Sieńczyk |
| author_facet | Agnieszka Łupicka-Słowik Federica Cossu Marcin Sieńczyk |
| author_sort | Agnieszka Łupicka-Słowik |
| collection | DOAJ |
| description | Neoplastic cells are characterized by uncontrolled cell divisions caused by cell cycle dysregulation. Key regulatory proteins governing the transition from the G1 to the S phase are the CDK4 and CDK6 kinases, which are controlled by D-type cyclins. The CDK4/6 kinases enable the use of these proteins as targets for anticancer therapy because they prevent the growth and the development of malignant cells by inhibiting their activity. This paper surveys the clinical trial results concerning palbociclib, the first in-class FDA-approved anticancer drug for hormone-dependent breast cancer. It discusses the therapeutic applications in breast cancer as well as in solid tumors and hematopoietic malignancies. Additionally, the paper presents an analysis of palbociclib resistance acquired during therapy and explores new approaches, such as modifications to palbociclib that enhance its desired activity or open up new therapeutic possibilities (PROTACs). |
| format | Article |
| id | doaj-art-6adb2913dd944bfb95d58ebd41a49b2d |
| institution | Kabale University |
| issn | 1420-3049 |
| language | English |
| publishDate | 2024-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj-art-6adb2913dd944bfb95d58ebd41a49b2d2024-11-26T18:15:35ZengMDPI AGMolecules1420-30492024-11-012922533410.3390/molecules29225334Palbociclib as an Antitumor Drug: A License to KillAgnieszka Łupicka-Słowik0Federica Cossu1Marcin Sieńczyk2Division of Organic and Medicinal Chemistry, Faculty of Chemistry, Wroclaw University of Science and Technology, Wybrzeze Wyspianskiego 27, 50-370 Wroclaw, PolandNational Research Council, Institute of Biophysics (IBF-CNR), Milan Unit, Via Corti, 12, 20133 Milan, ItalyDivision of Organic and Medicinal Chemistry, Faculty of Chemistry, Wroclaw University of Science and Technology, Wybrzeze Wyspianskiego 27, 50-370 Wroclaw, PolandNeoplastic cells are characterized by uncontrolled cell divisions caused by cell cycle dysregulation. Key regulatory proteins governing the transition from the G1 to the S phase are the CDK4 and CDK6 kinases, which are controlled by D-type cyclins. The CDK4/6 kinases enable the use of these proteins as targets for anticancer therapy because they prevent the growth and the development of malignant cells by inhibiting their activity. This paper surveys the clinical trial results concerning palbociclib, the first in-class FDA-approved anticancer drug for hormone-dependent breast cancer. It discusses the therapeutic applications in breast cancer as well as in solid tumors and hematopoietic malignancies. Additionally, the paper presents an analysis of palbociclib resistance acquired during therapy and explores new approaches, such as modifications to palbociclib that enhance its desired activity or open up new therapeutic possibilities (PROTACs).https://www.mdpi.com/1420-3049/29/22/5334palbociclibantitumorTNBCtargeted therapyPROTACSNIPERS |
| spellingShingle | Agnieszka Łupicka-Słowik Federica Cossu Marcin Sieńczyk Palbociclib as an Antitumor Drug: A License to Kill Molecules palbociclib antitumor TNBC targeted therapy PROTAC SNIPERS |
| title | Palbociclib as an Antitumor Drug: A License to Kill |
| title_full | Palbociclib as an Antitumor Drug: A License to Kill |
| title_fullStr | Palbociclib as an Antitumor Drug: A License to Kill |
| title_full_unstemmed | Palbociclib as an Antitumor Drug: A License to Kill |
| title_short | Palbociclib as an Antitumor Drug: A License to Kill |
| title_sort | palbociclib as an antitumor drug a license to kill |
| topic | palbociclib antitumor TNBC targeted therapy PROTAC SNIPERS |
| url | https://www.mdpi.com/1420-3049/29/22/5334 |
| work_keys_str_mv | AT agnieszkałupickasłowik palbociclibasanantitumordrugalicensetokill AT federicacossu palbociclibasanantitumordrugalicensetokill AT marcinsienczyk palbociclibasanantitumordrugalicensetokill |