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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...
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...
Mitogens and the Cell Cycle02:38

Mitogens and the Cell Cycle

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...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Drug-Receptor Interaction: Antagonist01:28

Drug-Receptor Interaction: Antagonist

An antagonist is a drug that binds strongly to a receptor without activating it. An antagonist prevents other molecules, such as neurotransmitters or hormones, from binding to the receptor and triggering a cellular response. Such interaction effectively hinders the normal physiological processes mediated by the receptor, resulting in various pharmacological effects depending on the specific receptor targeted.
Antagonists can be classified as competitive or noncompetitive based on their...
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists01:28

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...

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Polymalic Acid-based Nano Biopolymers for Targeting of Multiple Tumor Markers: An Opportunity for Personalized Medicine?
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Published on: June 13, 2014

HER-2-directed, small-molecule antagonists.

Michelle Arkin1, Mark M Moasser

  • 1Department of Medicine and Comprehensive Cancer Center, Box 0875, San Francisco, CA 94143-0875, USA.

Current Opinion in Investigational Drugs (London, England : 2000)
|November 28, 2008
PubMed
Summary
This summary is machine-generated.

Targeting human epidermal growth factor receptor-2 (HER-2) tyrosine kinase is a promising cancer treatment strategy. Developing selective HER-2 inhibitors is challenging due to its interaction with HER-3.

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Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • The human epidermal growth factor receptor-2 (HER-2) tyrosine kinase is a significant target for cancer therapy.
  • Developing effective HER-2 inhibitors is crucial for advancing cancer treatment strategies.

Purpose of the Study:

  • To explore the potential of HER-2 tyrosine kinase inactivation as a cancer treatment.
  • To review the development of ATP-analog inhibitors targeting HER-2 kinase.
  • To address the challenges in HER-2 inhibition, particularly the role of HER-3.

Main Methods:

  • Structure-based drug design utilizing information from the related EGF receptor.
  • Screening of ATP-analog inhibitors.
  • Analysis of signaling and structural studies involving HER-2 and HER-3.

Main Results:

  • Several classes of ATP-analog inhibitors targeting HER-2 tyrosine kinase have been developed.
  • Structural insights from the EGF receptor have aided in designing HER-2 specific inhibitors.
  • The regulatory role of the inactive HER-3 kinase presents challenges for HER-2 inactivation.

Conclusions:

  • Inactivation of HER-2 tyrosine kinase is a high-value strategy in cancer drug discovery.
  • Exploiting structural similarities with EGF receptor enhances inhibitor development.
  • The complex regulatory network involving HER-3 necessitates further research for effective HER-2 targeted therapies.