Related Experiment Video

Updated: Mar 9, 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

11.9K

Development of Selective Cyclin-Dependent Kinase 4 Inhibitors for Antineoplastic Therapies

Haixing Guan1, Yongli Du1, Weiwei Han1

  • 1School of Chemistry and Pharmaceutical Engineering, Qilu University of Technology, 3501 Daxue Road, Jinan 250353, China.

Anti-Cancer Agents in Medicinal Chemistry
|January 4, 2017
PubMed

Insights

Targeting Cyclin-Dependent Kinases 4 (CDK4) is a promising cancer therapy strategy. This review covers recent advancements in selective CDK4 inhibitors, including their mechanisms, structure-activity relationships, and clinical trial progress.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Cyclin-Dependent Kinases 4 (CDK4) regulates the G1 phase of the cell cycle.
  • Targeting the CDK4 pathway presents a significant therapeutic opportunity for cancer treatment.

Purpose of the Study:

  • To review recent developments in selective small molecule CDK4 inhibitors for cancer therapy.
  • To provide insights into the structure, mechanism, SARs, and clinical progress of these inhibitors.

Main Methods:

  • Literature review of recent scientific publications and clinical trial data.
  • Analysis of structural and mechanistic aspects of CDK4 inhibitors.
  • Evaluation of structure-activity relationships (SARs).

Main Results:

  • Selective small molecule CDK4 inhibitors show promise in preclinical and clinical settings.
  • Understanding SARs is crucial for optimizing inhibitor design.
  • Several CDK4 inhibitors are advancing through clinical trials for various cancers.

Conclusions:

  • CDK4 inhibitors represent a rapidly evolving and attractive area in cancer therapy.
  • Continued research into selective CDK4 inhibitors is warranted to improve efficacy and patient outcomes.
Keywords:
Anti-cancer agentscell cycleclinical trialscyclin-dependent kinases 4selective inhibitorsstructure activity relationship (SAR)

More Related Videos

Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay12:26

Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay

Published on: May 3, 2018

19.4K
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

11.6K

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...
6.1K
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...
6.7K
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...
9.0K
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.
7.0K
Positive Regulator Molecules01:45

Positive Regulator Molecules

To consistently produce healthy cells, the cell cycle—the process that generates daughter cells—must be precisely regulated.
136.9K
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...
6.3K