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Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

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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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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.
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Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...
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Related Experiment Video

Updated: Feb 23, 2026

A Flow Cytometry-based Assay to Identify Compounds That Disrupt Binding of Fluorescently-labeled CXC Chemokine Ligand 12 to CXC Chemokine Receptor 4
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A Flow Cytometry-based Assay to Identify Compounds That Disrupt Binding of Fluorescently-labeled CXC Chemokine Ligand 12 to CXC Chemokine Receptor 4

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CXCR4 Ligands: The Next Big Hit?

Annemiek M E Walenkamp1, Constantin Lapa2, Ken Herrmann3,4

  • 1Department of Medical Oncology, University Medical Center Groningen, University of Groningen, Groningen, The Netherlands a.walenkamp@umcg.nl.

Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine
|September 3, 2017
PubMed
Summary

Targeting the CXCR4-CXCL12 axis offers new cancer treatment strategies. CXCR4 antagonists disrupt tumor microenvironments and enhance therapies, with novel ligands in clinical trials for improved patient outcomes.

Keywords:
CXCR4endoradiotherapyimmunotherapytumor microenvironment

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Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • The C-X-C chemokine receptor 4 (CXCR4) is overexpressed in various cancers.
  • CXCR4 and its ligand C-X-C chemokine ligand 12 (CXCL12) drive cancer cell proliferation, metastasis, and survival.
  • The CXCR4-CXCL12 axis mediates critical interactions within the tumor microenvironment.

Purpose of the Study:

  • To review novel strategies for enhancing cancer treatment by targeting the CXCR4-CXCL12 interaction.
  • To explore the therapeutic potential of CXCR4 antagonists in oncology.
  • To highlight advancements in molecular imaging for patient selection in CXCR4-targeted therapies.

Main Methods:

  • Review of current literature on CXCR4-CXCL12 axis in cancer.
  • Analysis of peptidic and nonpeptidic CXCR4 antagonists.
  • Discussion of molecular imaging techniques for CXCR4-targeted therapy.

Main Results:

  • CXCR4 antagonists disrupt the protective tumor microenvironment.
  • Targeting CXCR4 can sensitize cancer cells to chemotherapy and radiotherapy.
  • Development of novel CXCR4 ligands for therapeutic and diagnostic applications.

Conclusions:

  • Targeting the CXCR4-CXCL12 axis represents a promising approach for cancer therapy.
  • CXCR4-directed therapies, including endoradiotherapy, show potential for improved patient outcomes.
  • Molecular imaging can guide patient selection for CXCR4-targeted treatments.