Related Experiment Video

Updated: Jul 7, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

Next-Generation CDK Inhibitors in Breast Cancer: Expanding the Therapeutic Landscape beyond CDK4/6 Inhibitors

Jiayi Wu1, Yinglu Lai1, Guang Lu1

  • 1Affiliated Xiaoshan Hospital, Hangzhou Normal University, Hangzhou, China.

Breast Care (Basel, Switzerland)
|July 6, 2026
PubMed
Abstract

Insights

Targeting additional cyclin-dependent kinases (CDKs) beyond CDK4/6 offers new hope for breast cancer patients. Exploring these targets may overcome resistance and treat aggressive forms of the disease.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Cyclin-dependent kinases (CDKs) are crucial regulators of the cell cycle.
  • Aberrant CDK activation drives breast cancer progression through cell cycle-dependent and independent pathways.
  • Existing CDK4/6 inhibitors highlight the therapeutic potential of targeting CDKs in breast cancer.

Purpose of the Study:

  • To review the pathological roles of key CDKs (CDK 1, 2, 5, 7, 8, 9, 12) in breast cancer.
  • To update on novel CDK inhibitors targeting resistance mechanisms and aggressive subtypes.
  • To explore innovative therapeutic strategies involving CDK inhibitors.

Main Methods:

  • Systematic literature review of CDK roles in breast cancer.
  • Analysis of current development and clinical trial data for novel CDK inhibitors.
  • Examination of emerging therapeutic applications, including immunotherapy combinations and antibody-drug conjugates.

Main Results:

  • Key CDKs (CDK 1, 2, 5, 7, 8, 9, 12) promote breast cancer proliferation, metastasis, and resistance to various therapies.
  • Novel CDK inhibitors are in development to overcome resistance to chemotherapy, anti-HER2 agents, and CDK4/6 inhibitors.
  • Innovative strategies like immunotherapy combinations and CDK inhibitor-based antibody-drug conjugates are being explored.

Conclusions:

  • Targeting a broader range of CDKs is a promising strategy for unmet needs in breast cancer.
  • Expanding CDK-targeted therapies, as single agents or combinations, will reshape breast cancer treatment.
  • These approaches hold significant potential for overcoming therapy resistance and managing aggressive breast cancer subtypes.
Keywords:
Breast cancerCDK inhibitorCell cycleResistance

More Related Videos

Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics06:00

Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics

Published on: May 14, 2016

Related Concept Videos

Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
Inhibition of CDK Activity02:34

Inhibition of CDK Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
M-Cdk Drives Transition Into Mitosis02:15

M-Cdk Drives Transition Into Mitosis

Checkpoints throughout the cell cycle serve as safeguards and gatekeepers, allowing the cell cycle to progress in favorable conditions and slow or halt it in problematic ones. This regulation is known as the cell cycle control system.
Cyclin-dependent kinases, or Cdks, work in concert with cyclins to control cell cycle transitions. M-Cdk, a complex of Cdk1 bound to M cyclin, is a well-known example of this coordinated control that drives the transition from the G2 to the M phase.
M cyclin...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Cancer-Critical Genes II: Tumor Suppressor Genes01:05

Cancer-Critical Genes II: Tumor Suppressor Genes

Genes usually encode proteins necessary for the proper functioning of a healthy cell. Mutations can often cause changes to the gene expression pattern, thereby altering the phenotype.
When the function of certain critical genes, especially those involved in cell cycle regulation and cell growth signaling cascades, gets disrupted, it upsets the cell cycle progression. Such cells with unchecked cell cycles start proliferating uncontrollably and eventually develop into tumors.
Such genes that act...