Inhibitors of cyclin-dependent kinases as cancer therapeutics.

Whittaker, Steven R.; Mallinger, Aurélie; Workman, Paul; Clarke, Paul A.

doi:10.1016/j.pharmthera.2017.02.008

Cited by 403Advanced Breast Cancer TherapiesCancer-related Molecular PathwaysPI3K/AKT/mTOR signaling in cancer

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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p21 leads to inhibition of phosphorylation of RB family proteins and subsequent association with E2Fs and formation of DREAM complex, leading to cell cycle arrest.
“This leads to inhibition of phosphorylation of the RB family of proteins and subsequent association with E2Fs and formation of the DREAM complex thereby leading to a cell cycle arrest (Chen et al., 1996; Whittaker et al., 2017; Wiedemeyer, 2018).”
From Mechanisms of Cellular Senescence: Cell Cycle Arrest and Senescence Associated Secretory Phenotype (2021) · cites this paper as Whittaker et al., 2017

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Identification and Characterization of the CDK12/Cyclin L1 Complex Involved in Alternative Splicing Regulation
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Mantle cell lymphoma cells express predominantly cyclin D1a isoform and are highly sensitive to selective inhibition of CDK4 kinase activity
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Pygopus activates Wingless target gene transcription through the mediator complex subunits Med12 and Med13
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FoxM1 Regulates Transcription of JNK1 to Promote the G1/S Transition and Tumor Cell Invasiveness
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Cdk8 Is Essential for Preimplantation Mouse Development
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The Structure of CDK8/CycC Implicates Specificity in the CDK/Cyclin Family and Reveals Interaction with a Deep Pocket Binder
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Cleavage of PITSLRE Kinases by ICE/CASP-1 and CPP32/CASP-3 during Apoptosis Induced by Tumor Necrosis Factor
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Cdk1 Participates in BRCA1-Dependent S Phase Checkpoint Control in Response to DNA Damage
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The RNA Polymerase II CTD: The Increasing Complexity of a Low-Complexity Protein Domain
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TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties
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The PITSLRE/CDK11p58 protein kinase promotes centrosome maturation and bipolar spindle formation
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Characterization of Cyclin L1 and L2 Interactions with CDK11 and Splicing Factors
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Expression Signature of IFN/STAT1 Signaling Genes Predicts Poor Survival Outcome in Glioblastoma Multiforme in a Subtype-Specific Manner
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CDK8-Mediated STAT1-S727 Phosphorylation Restrains NK Cell Cytotoxicity and Tumor Surveillance
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The CDK4/6 inhibitor LY2835219 overcomes vemurafenib resistance resulting from MAPK reactivation and cyclin D1 upregulation
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A first-in-human, phase 1, dose-escalation study of dinaciclib, a novel cyclin-dependent kinase inhibitor, administered weekly in subjects with advanced malignancies
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Substituted 4-(Thiazol-5-yl)-2-(phenylamino)pyrimidines Are Highly Active CDK9 Inhibitors: Synthesis, X-ray Crystal Structures, Structure–Activity Relationship, and Anticancer Activities
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Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor
Brasca, M. G., Amboldi, N., Ballinari, D., Cameron, A. D., Casale, E., Cervi, G., Colombo, M., Colotta, F., Croci, V., D’Alessio, R., et al. (2009) · Journal of Medicinal Chemistry · doi:10.1021/jm9006559 · Cited by 130 · see citing works
Identification of Molecular Vulnerabilities in Human Multiple Myeloma Cells by RNA Interference Lethality Screening of the Druggable Genome
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In vitro and In vivo Pharmacokinetic-Pharmacodynamic Relationships for the Trisubstituted Aminopurine Cyclin-Dependent Kinase Inhibitors Olomoucine, Bohemine and CYC202
Raynaud, F. I., Whittaker, S. R., Fischer, P. M., McClue, S. J., Walton, M. I., Barrie, S. E., Garrett, M. D., Rogers, P., Clarke, S. J., Kèlland, L. R., et al. (2005) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-04-2264 · Cited by 130 · see citing works
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Abstract S1-6: Results of a randomized phase 2 study of PD 0332991, a cyclin-dependent kinase (CDK) 4/6 inhibitor, in combination with letrozole vs letrozole alone for first-line treatment of ER+/HER2− advanced breast cancer (BC)
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CrkRS
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Genetic inactivation of Cdk7 leads to cell cycle arrest and induces premature aging due to adult stem cell exhaustion
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Mice thrive without Cdk4 and Cdk2
Barrière, C., Santamarı́a, D., Cerqueira, A., Galán, J., Martín, A. L., Ortega, S., Malumbres, M., Dubus, P. R., & Barbacid, M. (2007) · Molecular Oncology · doi:10.1016/j.molonc.2007.03.001 · Cited by 125 · see citing works
AZD5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts
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Treatment of Relapsed Chronic Lymphocytic Leukemia by 72-Hour Continuous Infusion or 1-Hour Bolus Infusion of Flavopiridol: Results from Cancer and Leukemia Group B Study 19805
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Loss of Cdk2 and cyclin A2 impairs cell proliferation and tumorigenesis.
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Efficacy of the combination of MEK and CDK4/6 inhibitorsin vitroandin vivoin KRAS mutant colorectal cancer models
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Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening
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Dinaciclib is a novel cyclin-dependent kinase inhibitor with significant clinical activity in relapsed and refractory chronic lymphocytic leukemia
Flynn, J. M., Jones, J. A., Johnson, A. J., Andritsos, L. A., Maddocks, K. J., Jaglowski, S. M., Hessler, J. D., Grever, M. R., Im, E., Zhou, H., et al. (2015) · Leukemia · doi:10.1038/leu.2015.31 · Cited by 122 · see citing works
In vitro antitumor properties of a novel cyclin-dependent kinase inhibitor, P276-00
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TFIIH and P-TEFb Coordinate Transcription with Capping Enzyme Recruitment at Specific Genes in Fission Yeast
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Cdk10, a Cdc2-related kinase, associates with the Ets2 transcription factor and modulates its transactivation activity
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Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19
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Characterization of molecular and cellular functions of the cyclin‐dependent kinase CDK9 using a novel specific inhibitor
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CDK8 Maintains Tumor Dedifferentiation and Embryonic Stem Cell Pluripotency
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The CDK Network: Linking Cycles of Cell Division and Gene Expression
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A phase 1 study of SNS-032 (formerly BMS-387032), a potent inhibitor of cyclin-dependent kinases 2, 7 and 9 administered as a single oral dose and weekly infusion in patients with metastatic refractory solid tumors
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Antiproliferative Effects of CDK4/6 Inhibition in CDK4 -Amplified Human Liposarcoma In Vitro and In Vivo
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The Writers, Readers, and Functions of the RNA Polymerase II C-Terminal Domain Code
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Pan-Cancer Analysis of the Mediator Complex Transcriptome Identifies CDK19 and CDK8 as Therapeutic Targets in Advanced Prostate Cancer
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Discovery of Kinase Spectrum Selective Macrocycle (16E)-14-Methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a Potent Inhibitor of Cyclin Dependent Kinases (CDKs), Janus Kinase 2 (JAK2), and Fms-like Tyrosine Kinase-3 (FLT3) for the Treatment of Cancer
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CDK8 expression in 470 colorectal cancers in relation to β‐catenin activation, other molecular alterations and patient survival
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Discovery and Characterization of 2-Anilino-4- (Thiazol-5-yl)Pyrimidine Transcriptional CDK Inhibitors as Anticancer Agents
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Kinome-wide RNAi studies in human multiple myeloma identify vulnerable kinase targets, including a lymphoid-restricted kinase, GRK6
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Cortistatin A is a High‐Affinity Ligand of Protein Kinases ROCK, CDK8, and CDK11
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7 of the 292 references couldn’t be matched to a known paper.

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Mechanisms of Cellular Senescence: Cell Cycle Arrest and Senescence Associated Secretory Phenotype
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Cell cycle control in cancer
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The broken cycle: E2F dysfunction in cancer
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Off-target toxicity is a common mechanism of action of cancer drugs undergoing clinical trials
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The Roles of Cyclin-Dependent Kinases in Cell-Cycle Progression and Therapeutic Strategies in Human Breast Cancer
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Challenges and Opportunities in Cancer Drug Resistance
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Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry
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Interconnection between Metabolism and Cell Cycle in Cancer
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Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update
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Differences in the Conformational Energy Landscape of CDK1 and CDK2 Suggest a Mechanism for Achieving Selective CDK Inhibition
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Cancer Hallmarks and MicroRNAs: The Therapeutic Connection
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Anticancer Activity of Fascaplysin against Lung Cancer Cell and Small Cell Lung Cancer Circulating Tumor Cell Lines
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Micro-Current Stimulation Has Potential Effects of Hair Growth-Promotion on Human Hair Follicle-Derived Papilla Cells and Animal Model
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Investigational drugs targeting cyclin-dependent kinases for the treatment of cancer: an update on recent findings (2013-2016)
Giovanni, C. D., Novellino, E., Chilin, A., Lavecchia, A., & Marzaro, G. (2016) · Expert Opinion on Investigational Drugs · doi:10.1080/13543784.2016.1234603 · Cited by 25 · see citing works

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 › Pulmonary and Respiratory Medicine › 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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