Cited by 402Advanced Breast Cancer TherapiesCancer-related Molecular PathwaysPI3K/AKT/mTOR signaling in cancer

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Inhibitors of cyclin-dependent kinases as cancer therapeutics.

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Whittaker, Steven R., Mallinger, Aurélie, Workman, Paul, Clarke, Paul A.·2017·Pharmacology & Therapeutics

DOI 10.1016/j.pharmthera.2017.02.008PMC PMC6141011

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Abstract

Over the past two decades there has been a great deal of interest in the development of inhibitors of the cyclin-dependent kinases (CDKs). This attention initially stemmed from observations that different CDK isoforms have key roles in cancer cell proliferation through loss of regulation of the cell cycle, a hallmark feature of cancer. CDKs have now been shown to regulate other processes, particularly various aspects of transcription. The early non-selective CDK inhibitors exhibited considerable toxicity and proved to be insufficiently active in most cancers. The lack of patient selection biomarkers and an absence of understanding of the inhibitory profile required for efficacy hampered the development of these inhibitors. However, the advent of potent isoform-selective inhibitors with accompanying biomarkers has re-ignited interest. Palbociclib, a selective CDK4/6 inhibitor, is now approved for the treatment of ER+/HER2- advanced breast cancer. Current developments in the field include the identification of potent and selective inhibitors of the transcriptional CDKs; these include tool compounds that have allowed exploration of individual CDKs as cancer targets and the determination of their potential therapeutic windows. Biomarkers that allow the selection of patients likely to respond are now being discovered. Drug resistance has emerged as a major hurdle in the clinic for most protein kinase inhibitors and resistance mechanism are beginning to be identified for CDK inhibitors. This suggests that the selective inhibitors may be best used combined with standard of care or other molecularly targeted agents now in development rather than in isolation as monotherapies.

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Authors: Whittaker, S. R., Mallinger, A., Workman, P., & Clarke, P. A.
Affiliations: Institute of Cancer Research (GB)
Corresponding author: Clarke, Paul A.
ORCID: Whittaker, Steven R.
Workman, Paul
Clarke, Paul A.
Venue: Pharmacology & Therapeutics
Publisher: Elsevier BV
Published: 2017-05
Volume: 173
Pages: 83-105
ISSN: 0163-7258 (ISSN-L)
DOI: 10.1016/j.pharmthera.2017.02.008
PMC: PMC6141011
OpenAlex: W2583136106
Cited by: 384
References: 292
Citations by year: 2026: 25 · 2025: 38 · 2024: 37 · 2023: 47 · 2022: 38 · 2021: 53 · 2020: 55 · 2019: 51 · 2018: 25 · 2017: 15
FWCI: 7.38
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: Pharmacology & Therapeutics (publishedVersion)
PubMed (publishedVersion)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
Funders: Cancer Research UK (C309/A11566, C368/A6743, A368/A7990)
Topics: Health Sciences › Medicine › Oncology › Advanced Breast Cancer Therapies
Health Sciences › Medicine › Oncology › Cancer-related Molecular Pathways
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › PI3K/AKT/mTOR signaling in cancer
Keywords: cyclin-dependent kinases, cyclin-dependent kinase inhibitors, isoform-selective inhibitors, CDK4/6 inhibitors, palbociclib, breast cancer, cell cycle regulation, tumor cell proliferation, biomarkers, drug resistance, combination therapy, protein kinase inhibitors
MeSH terms: Animals, Antineoplastic Agents, Cell Cycle, Humans, Neoplasms, Drug Design, Cyclin-Dependent Kinases, Protein Kinase Inhibitors, Cell Proliferation, Molecular Targeted Therapy

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Inhibitors of cyclin-dependent kinases as cancer therapeutics.

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