Related Experiment Video
Updated: Nov 4, 2025
06:29
Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
Published on: July 30, 2020
3.2K
Aurora kinase inhibitors as potential anticancer agents: Recent advances
Tathagata Pradhan1, Ojasvi Gupta1, Gurpreet Singh1
1Department of Pharmaceutical Chemistry, ISF College of Pharmacy, GT Road, Ghal Kalan, Moga, 142001, Punjab, India.
European Journal of Medicinal Chemistry
|May 21, 2021
Summary
Aurora kinases are key regulators of cell division and are validated anticancer drug targets. This review details recent advancements in designing Aurora kinase inhibitors for cancer therapy.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Aurora kinases are serine/threonine kinases crucial for cell cycle regulation and mitotic spindle function.
- Overexpression of Aurora kinases is linked to various cancers, making them promising drug targets.
- Inhibiting Aurora kinases can induce tumor cell apoptosis and growth inhibition.
Purpose of the Study:
- To review recent strategies in the design and development of Aurora kinase inhibitors.
- To summarize the bioactivity, structure-activity relationships (SARs), molecular modeling, and mechanistic studies of these inhibitors.
- To provide insights for developing novel, selective, and effective anticancer drug candidates.
Main Methods:
- Literature review of research from 2011-2020.
- Analysis of various structural classes of Aurora kinase inhibitors.
- Compilation of data on bioactivity, SARs, molecular modeling, and mechanistic studies.
Main Results:
- Numerous Aurora kinase inhibitors across different structural classes have been explored.
- Preclinical and clinical investigations are ongoing for several inhibitors.
- Detailed SARs and mechanistic insights are available for various inhibitor designs.
Conclusions:
- The development of Aurora kinase inhibitors is a dynamic field with significant therapeutic potential.
- Continued research in inhibitor design, selectivity, and efficacy is crucial.
- This review offers a comprehensive resource for future drug discovery efforts in this area.
Related Concept Videos
02:34Inhibition of Cdk Activity
5.1K
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...
5.1K
02:57Targeted Cancer Therapies
8.0K
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...
There are several types of targeted therapies against...
8.0K
02:15M-Cdk Drives Transition Into Mitosis
5.8K
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...
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...
5.8K
03:03mTOR Signaling and Cancer Progression
4.0K
The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
The mTOR pathway or the...
4.0K
01:22PI3K/mTOR/AKT Signaling Pathway
4.3K
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...
4.3K
02:38Mitogens and the Cell Cycle
7.2K
Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
7.2K