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Updated: Jan 20, 2026
Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay
Published on: May 3, 2018
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019)
Concepción Sánchez-Martínez1, María José Lallena1, Sonia Gutiérrez Sanfeliciano1
1Discovery Chemistry Research and Technologies, Eli Lilly and Company, Alcobendas (Madrid) 28108, Spain.
Abstract:
Sustained proliferative capacity and gene dysregulation are hallmarks of cancer. In mammalian cells, cyclin-dependent kinases (CDKs) control critical cell cycle checkpoints and key transcriptional events in response to extracellular and intracellular signals leading to proliferation. Significant clinical activity for the treatment of hormone receptor positive metastatic breast cancer has been demonstrated by palbociclib, ribociclib and abemaciclib, dual CDK4/6 inhibitors recently FDA-approved. SY-1365, a CDK7 inhibitor has shown initial encouraging data in phase I for solid tumors treatment. These results have rejuvenated the CDKs research field. This review provides an overview of relevant advances on CDK inhibitor research since 2015 to 2019, with special emphasis on transcriptional CDK inhibitors, new emerging strategies such as target protein degradation and compounds under clinical evaluation.
Insights
Cancer cells exhibit uncontrolled proliferation due to gene dysregulation. This review covers advances in cyclin-dependent kinase (CDK) inhibitors, including transcriptional CDK inhibitors and novel strategies for cancer treatment.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Cancer is characterized by sustained proliferation and gene dysregulation.
- Cyclin-dependent kinases (CDKs) regulate cell cycle checkpoints and transcription crucial for proliferation.
- Approved CDK4/6 inhibitors show efficacy in hormone receptor-positive metastatic breast cancer.
Purpose of the Study:
- To review advances in CDK inhibitor research from 2015-2019.
- To highlight transcriptional CDK inhibitors and emerging therapeutic strategies.
- To discuss compounds currently under clinical evaluation for cancer treatment.
Main Methods:
- Literature review of CDK inhibitor research.
- Focus on transcriptional CDK inhibitors and target protein degradation.
- Analysis of compounds in clinical trials.
Main Results:
- Recent approvals of CDK4/6 inhibitors (palbociclib, ribociclib, abemaciclib) for breast cancer.
- Promising Phase I data for CDK7 inhibitor SY-1365 in solid tumors.
- Renewed interest and research in the CDK inhibitor field.
Conclusions:
- CDK inhibitors represent a significant therapeutic advancement in oncology.
- Transcriptional CDK inhibitors and novel strategies like target protein degradation offer new avenues for cancer therapy.
- Ongoing clinical evaluations are crucial for developing next-generation CDK-targeted treatments.
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