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Related Concept Videos

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...
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...
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Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers

Receptor tyrosine kinase inhibitors (TKIs) and calcium channel blockers (CCBs) are two critical categories of drugs employed in the treatment of pulmonary artery hypertension (PAH). PAH is a disease that causes high blood pressure in the pulmonary arteries, resulting in chest pain, fatigue, and shortness of breath.
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Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists

Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy.  SP binds and activates these...
PI3K/mTOR/AKT Signaling Pathway01:22

PI3K/mTOR/AKT Signaling Pathway

The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a rapamycin-insensitive companion...
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Antiarrhythmic Drugs: Class III Agents as Potassium Channel Blockers

Class III antiarrhythmic drugs are a group of medications that can prolong action potentials in the heart. They achieve this by blocking potassium channels or enhancing inward currents from sodium channels. However, these drugs have a unique property of "reverse use-dependence," which is most pronounced at slower heart rates and can lead to torsades de pointes—a specific type of arrhythmia. However, it is essential to note that excessive QT interval prolongation—a measure of the heart's...

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Related Experiment Video

Updated: May 25, 2026

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
06:29

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells

Published on: July 30, 2020

Danusertib, an aurora kinase inhibitor.

Hielke J Meulenbeld1, Ron Hj Mathijssen, Jaap Verweij

  • 1Erasmus University Medical Center, Daniel den Hoed Cancer Center, Department of Medical Oncology, Groene Hilledijk 301, Rotterdam, the Netherlands. h.meulenbeld@erasmusmc.nl

Expert Opinion on Investigational Drugs
|January 17, 2012
PubMed
Summary
This summary is machine-generated.

Danusertib, an inhibitor of aurora and tyrosine kinases, shows potential as an anticancer therapeutic. Future research should explore combining danusertib with other treatments, particularly for leukemias.

Related Experiment Videos

Last Updated: May 25, 2026

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
06:29

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells

Published on: July 30, 2020

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Mitotic inhibitors are crucial in cancer treatment.
  • Aurora kinases, frequently overexpressed in cancers, regulate mitosis.
  • Danusertib is an ATP-competitive inhibitor of aurora A, B, and C kinases.

Purpose of the Study:

  • To review preclinical and clinical data on danusertib up to July 2011.
  • To assess danusertib's potential as an anticancer therapeutic.
  • To explore danusertib's multi-targeting profile.

Main Methods:

  • Literature review of preclinical studies.
  • Analysis of clinical trial data (Phase I and II).
  • Summary of danusertib's inhibitory effects on aurora and receptor tyrosine kinases.

Main Results:

  • Danusertib inhibits aurora A, B, and C kinases.
  • Danusertib also inhibits receptor tyrosine kinases (Abl, Ret, FGFR-1, TrkA).
  • This multi-targeting may enhance antitumor activity.

Conclusions:

  • Future studies should investigate danusertib combinations (chemotherapy, radiotherapy, targeted agents).
  • Danusertib may be more effective as a single agent in leukemias than in solid tumors.