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Related Concept Videos

siRNA - Small Interfering RNAs02:30

siRNA - Small Interfering RNAs

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Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a significant...
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Inhibition of Cdk Activity02:34

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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...
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Related Experiment Video

Updated: Jun 23, 2026

Deacetylation Assays to Unravel the Interplay between Sirtuins (SIRT2) and Specific Protein-substrates
14:32

Deacetylation Assays to Unravel the Interplay between Sirtuins (SIRT2) and Specific Protein-substrates

Published on: February 27, 2016

Sirtuin inhibitors.

Francisco J Alcaín1, José M Villalba

  • 1Universidad de Córdoba, Departamento de Biología Celular, Fisiología e Inmunología, Facultad de Ciencias, Campus Rabanales, Edificio Severo Ochoa, Córdoba, Spain.

Expert Opinion on Therapeutic Patents
|May 16, 2009
PubMed
Summary
This summary is machine-generated.

Sirtuin inhibitors offer potential therapeutic benefits for diseases like cancer and Parkinson's. By modulating sirtuin activity, these small molecules may increase lifespan and combat neurodegeneration.

Related Experiment Videos

Last Updated: Jun 23, 2026

Deacetylation Assays to Unravel the Interplay between Sirtuins (SIRT2) and Specific Protein-substrates
14:32

Deacetylation Assays to Unravel the Interplay between Sirtuins (SIRT2) and Specific Protein-substrates

Published on: February 27, 2016

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • The sirtuin (silent information regulator) family comprises seven NAD(+)-dependent deacetylase enzymes (SIRT1-7) with varied subcellular localization.
  • Sirtuin expression is generally upregulated by caloric restriction and oxidative stress.
  • SIRT1, a key mammalian sirtuin, deacetylates targets like the transcription factor p53, influencing lifespan and stress resistance.

Purpose of the Study:

  • To review the discovery and development of small molecules that modulate sirtuin activity.
  • To focus on sirtuin inhibitors and their therapeutic potential.

Main Methods:

  • Literature review of sirtuin inhibitors.
  • Analysis of reported mechanisms of action and therapeutic applications.

Main Results:

  • Specific SIRT1 inhibitors have been identified, potentially useful in cancer treatment by enhancing p53 activity to induce apoptosis.
  • One SIRT1 inhibitor demonstrates p53-independent apoptosis induction.
  • A selective SIRT2 inhibitor shows promise for treating Parkinson disease by reducing alpha-synuclein fibril formation.

Conclusions:

  • Sirtuin inhibitors represent a promising class of therapeutics for various human diseases.
  • SIRT1 inhibitors may be valuable in oncology and SIRT2 inhibitors in neurodegenerative disorders.