Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

6.2K
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...
6.2K
Inhibition of CDK Activity02:34

Inhibition of CDK Activity

5.7K
5.7K
M-Cdk Drives Transition Into Mitosis02:15

M-Cdk Drives Transition Into Mitosis

6.8K
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...
6.8K
Positive Regulator Molecules02:39

Positive Regulator Molecules

7.1K
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.
7.1K
Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

2.2K
Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
2.2K
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

9.2K
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...
9.2K

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Design, Synthesis, and Antitumor Evaluation of Benzamide Derivatives Targeting HOXA1 Function.

Journal of medicinal chemistry·2026
Same author

Design, Synthesis, and Mechanistic Evaluation of l-Theanine Derivatives Targeting Cathepsin D for Anti-Hepatic Fibrosis.

Journal of medicinal chemistry·2026
Same author

Inhibitory Effects of Alkaloids on BCRP Implicated in Reversing Multidrug Resistance: A Case Example of Enhancing Temozolomide Cytotoxicity.

Chemical research in toxicology·2025
Same author

Cathepsin D promotes acute myeloid leukemia progression through stabilization of the anti-apoptotic proteins.

Cell death & disease·2025
Same author

Discovery of Novel Isoindolin-1-one Derivatives as GABA<sub>A</sub> Receptors Positive Allosteric Modulators with Antiepileptic Efficacy.

Journal of medicinal chemistry·2025
Same author

Inhibitory Effects of Alkaloids on OATP1B1 In Vitro and In Vivo: Prediction for Food/Herb-Drug Interactions and Hepatoprotective Effects Based on Structure-Activity Relationships.

Chemical research in toxicology·2025

Related Experiment Video

Updated: Apr 16, 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

Design, Synthesis, and Biological Evaluation of Selective CDK4/9 Inhibitors.

Siqi Li1, Xiaotang Yang1, Weiyi Yin1

  • 1Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.

ACS Medicinal Chemistry Letters
|April 15, 2026
PubMed
Summary

A new drug, LS-Q2, selectively inhibits CDK4/9 to fight cancer. This orally available compound shows potent antitumor effects and synergistic potential with other cancer therapies.

Keywords:
CDK4/9 inhibitorsantiproliferationpyrrolo[2,3-d]pyrimidine derivativesstructure−activity relationshipsynthesis

More Related Videos

Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay
12:26

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

Published on: May 3, 2018

19.5K
A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English
14:34

A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English

Published on: April 3, 2026

207

Related Experiment Videos

Last Updated: Apr 16, 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
Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay
12:26

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

Published on: May 3, 2018

19.5K
A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English
14:34

A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English

Published on: April 3, 2026

207

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Pharmacology

Background:

  • Targeting cyclin-dependent kinases (CDKs) is a key strategy in cancer therapy.
  • Simultaneous inhibition of cell cycle and transcriptional CDKs offers a novel therapeutic approach.

Purpose of the Study:

  • To synthesize and evaluate novel pyrrolo-[2,3-d]-pyrimidine derivatives as potential CDK inhibitors.
  • To identify a potent, selective, and orally bioavailable CDK4/9 inhibitor for cancer treatment.

Main Methods:

  • Synthesis of 2-((4-substitutedphenyl)-amino)-pyrrolo-[2,3-d]-pyrimidine derivatives.
  • In vitro evaluation of antiproliferative activity and CDK enzymatic inhibition.
  • In vivo pharmacokinetic and efficacy studies.
  • Combination studies with BET and Bcl-2 inhibitors.

Main Results:

  • Several novel derivatives demonstrated improved in vitro antitumor potency, metabolic stability, and kinase selectivity.
  • Derivative 6m (LS-Q2) was identified as a highly selective CDK4/9 inhibitor with oral bioavailability.
  • LS-Q2 exhibited potent antiproliferative activity and synergistic effects with BET and Bcl-2 inhibitors in vivo.

Conclusions:

  • LS-Q2 is a promising next-generation CDK inhibitor lead for treating malignant solid tumors.
  • Orally available and selective CDK4/9 inhibitors represent a valuable therapeutic strategy in oncology.
  • The findings support further development of LS-Q2 for broad cancer applications.