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Related Concept Videos

Targeted Cancer Therapies02:57

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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.
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Enhancement of Apoptotic and Autophagic Induction by a Novel Synthetic C-1 Analogue of 7-deoxypancratistatin in Human Breast Adenocarcinoma and Neuroblastoma Cells with Tamoxifen
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PROTACs: Promising approach for anticancer therapy.

Simran Deep Kaur1, Neena Bedi2, Deepak Kumar1

  • 1School of Pharmaceutical Sciences, Shoolini University of Biotechnology and Management Sciences, Solan, 173229, India.

Cancer Letters
|January 15, 2023
PubMed
Summary
This summary is machine-generated.

Proteolysis-targeting chimeras (PROTACs) degrade cancer proteins by hijacking the cell's natural protein disposal system. This review explores how PROTAC design impacts cancer therapy effectiveness and resistance.

Keywords:
Bromodomain-containing protein 4 (BRD4)Galactose-decorated liver tumor-specific nanoliposomes (GALARV)Protein of interest (POI)Proteolysis targeting chimeras (PROTACs)

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A Flow Cytometry-Based Cell Surface Protein Binding Assay for Assessing Selectivity and Specificity of an Anticancer Aptamer
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Area of Science:

  • Biochemistry and Molecular Biology
  • Medicinal Chemistry
  • Oncology

Background:

  • Proteolysis-targeting chimeras (PROTACs) are an emerging therapeutic modality.
  • PROTACs leverage the ubiquitin-proteasome system for targeted protein degradation.
  • Cancer drug resistance necessitates novel therapeutic strategies.

Purpose of the Study:

  • To review the design principles of bifunctional PROTACs.
  • To explore how PROTAC ligand properties influence therapeutic outcomes.
  • To discuss PROTACs as anticancer agents, including overcoming resistance.

Main Methods:

  • Development of diverse bifunctional PROTACs by combining small molecule ligands.
  • Investigation of reversible and irreversible ligand binding modes (orthosteric/allosteric).
  • Analysis of agonist/antagonist PROTAC activity and target protein modulation.

Main Results:

  • PROTACs can be designed with various ligand types to modulate target proteins.
  • Ligand properties significantly impact PROTAC efficacy, selectivity, and delivery.
  • Targeted ligand approaches offer strategies to overcome drug resistance.

Conclusions:

  • Small molecule-based PROTACs represent a promising approach for cancer therapy.
  • Understanding PROTAC-E3 ligase-target protein dynamics is crucial for optimization.
  • Targeted proteolysis offers a versatile platform for developing novel anticancer drugs.