Related Experiment Video

Updated: Sep 13, 2025

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

11.4K

Research progress of dual-targeting CDKs regulators for cancer therapy

Fei-Xia Yue1, Ya-Lan Wang1, Rui-Yan1

  • 1Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affifiliated Ministry of Education, College of Pharmacy, Yanbian University, Yanji, Jilin 133002, China.

Bioorganic Chemistry
|July 25, 2025
PubMed

Insights

Targeting multiple cyclin-dependent kinases (CDKs) with dual-action regulators offers a promising strategy to overcome resistance and improve efficacy in cancer therapy, addressing limitations of single-target drugs.

Area of Science:

  • Molecular Biology
  • Pharmacology
  • Oncology

Background:

  • Cyclin-dependent kinases (CDKs) regulate cell cycle progression and transcription.
  • CDKs are crucial targets for anticancer drug development.
  • Recent CDK inhibitors offer improved selectivity and safety over older pan-CDK inhibitors.

Purpose of the Study:

  • To review the design of dual-target CDK regulators.
  • To explore the potential of these regulators in cancer therapy.
  • To address the limitations of single-target CDK inhibitors in complex cancer networks.

Main Methods:

  • Literature review of CDK dual-target regulator designs.
  • Analysis of polypharmacology strategies for CDK inhibition.
  • Evaluation of potential therapeutic applications in oncology.

Main Results:

  • Selective CDK inhibitors show improved safety but face challenges like resistance.
  • Dual-targeting CDK regulators offer a strategy to overcome single-target drug limitations.
  • Various designs for dual-target CDK regulators are being explored.

Conclusions:

  • Dual-targeting CDK regulators represent an effective strategy for cancer therapy.
  • Polypharmacology approaches are advancing cancer treatment by targeting multiple pathways.
  • Further research into CDK dual-target regulators holds significant promise for oncology.
Keywords:
CDKCDK inhibitorsCancerDual-targeting

More Related Videos

Methods for Evaluating the Role of c-Fos and Dusp1 in Oncogene Dependence10:09

Methods for Evaluating the Role of c-Fos and Dusp1 in Oncogene Dependence

Published on: January 7, 2019

8.4K
Development and Maintenance of a Preclinical Patient Derived Tumor Xenograft Model for the Investigation of Novel Anti-Cancer Therapies09:29

Development and Maintenance of a Preclinical Patient Derived Tumor Xenograft Model for the Investigation of Novel Anti-Cancer Therapies

Published on: September 30, 2016

13.9K

Related Concept Videos

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...
5.7K
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...
4.9K
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...
7.8K
Mitogens and the Cell Cycle02:38

Mitogens and the Cell Cycle

Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
6.9K
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
5.1K
Positive Regulator Molecules02:39

Positive Regulator Molecules

Mitotic cell division results in daughter cells that exactly resemble the parent cell. However, errors in the DNA replication or distribution of genetic material may lead to genetic mutations that may be passed down to every new cell formed from the resulting abnormal cell. Propagation of such mutant cells is restricted through checkpoint mechanisms present at different stages of the cell cycle. These checkpoints involve regulator molecules that either promote or demote cell cycle events.
5.7K