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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...
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...
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...
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.
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...

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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

CDK9 a potential target for drug development.

Fernanda Canduri1, Patrícia Cardoso Perez, Rafael Andrade Caceres

  • 1Faculdade de Biociências-PUCRS-Av. Ipiranga,6681. Porto Alegre-RS Brazil. walter.junior@pucrs.br.

Medicinal Chemistry (Shariqah (United Arab Emirates))
|May 14, 2008
PubMed
Summary
This summary is machine-generated.

Cyclin-Dependent Kinase 9 (CDK9) plays a key role in transcription and cell differentiation. Inhibiting CDK9 with drugs like Roscovitine and Flavopiridol shows promise for treating HIV and certain cancers.

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

  • Molecular Biology
  • Biochemistry
  • Cell Biology

Background:

  • Cyclin-Dependent Kinases (CDKs) regulate cell cycle and transcription.
  • CDK9 is the catalytic subunit of positive transcription elongation factor b (P-TEFb).
  • CDK9's interaction with HIV Tat protein suggests a role in AIDS progression.

Purpose of the Study:

  • To review the role of CDK9 in transcription, cell differentiation, and HIV infection.
  • To discuss the therapeutic potential of CDK9 inhibitors.

Main Methods:

  • The study is a review of existing literature on CDK9.
  • Focuses on the mechanism of CDK9 action and inhibition.
  • Examines the role of CDK9 in HIV Tat transactivation and tumor differentiation.

Main Results:

  • CDK9/cyclin T1 complex mediates HIV Tat transactivation and stimulates RNA Pol II phosphorylation.
  • CDK9 expression correlates with differentiation grade in neuroectodermal and neuroblastoma tumors.
  • Roscovitine and Flavopiridol inhibit CDK9 and prevent HIV replication by blocking Tat transactivation.

Conclusions:

  • CDK9 is a critical regulator of transcription and differentiation with implications for HIV and cancer.
  • CDK9 inhibitors like Roscovitine and Flavopiridol demonstrate therapeutic potential.
  • Further structural studies could lead to more targeted CDK9 inhibitors.