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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...

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Related Experiment Video

Updated: Jun 20, 2026

Preparing a 68Ga-labeled Arginine Glycine Aspartate (RGD)-peptide for Angiogenesis
07:48

Preparing a 68Ga-labeled Arginine Glycine Aspartate (RGD)-peptide for Angiogenesis

Published on: January 7, 2019

Extracellularly Activatable Conjugates of RGD Peptidomimetics and Cryptophycin for αVβ3-Targeted Cancer Therapy.

Dominic Seißenschmidt1, Henriette Hartung1, Jonah Kammer1

  • 1Organic and Bioorganic Chemistry, Faculty of Chemistry, Bielefeld University, Bielefeld, Germany.

Chemistry (Weinheim an Der Bergstrasse, Germany)
|June 18, 2026
PubMed
Summary

Small molecule-drug conjugates (SMDCs) offer targeted cancer therapy. This study developed integrin αVβ3-targeting SMDCs with a potent payload, demonstrating effective tumor cell killing upon enzymatic payload release.

Keywords:
RGD peptidomimeticantitumor agentscryptophycindrug deliveryneutrophil elastase

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Initial Evaluation of Antibody-conjugates Modified with Viral-derived Peptides for Increasing Cellular Accumulation and Improving Tumor Targeting
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Initial Evaluation of Antibody-conjugates Modified with Viral-derived Peptides for Increasing Cellular Accumulation and Improving Tumor Targeting

Published on: March 8, 2018

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Last Updated: Jun 20, 2026

Preparing a 68Ga-labeled Arginine Glycine Aspartate (RGD)-peptide for Angiogenesis
07:48

Preparing a 68Ga-labeled Arginine Glycine Aspartate (RGD)-peptide for Angiogenesis

Published on: January 7, 2019

Initial Evaluation of Antibody-conjugates Modified with Viral-derived Peptides for Increasing Cellular Accumulation and Improving Tumor Targeting
11:58

Initial Evaluation of Antibody-conjugates Modified with Viral-derived Peptides for Increasing Cellular Accumulation and Improving Tumor Targeting

Published on: March 8, 2018

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Drug Delivery

Background:

  • Small molecule-drug conjugates (SMDCs) are emerging as a targeted cancer therapy strategy.
  • These agents combine tumor-targeting ligands with potent cytotoxic payloads.
  • Integrin αVβ3 is a validated target in various cancers.

Purpose of the Study:

  • To design, synthesize, and evaluate novel integrin αVβ3-targeting SMDCs.
  • To utilize a potent cryptophycin payload and a neutrophil elastase cleavable linker.
  • To assess the impact of linker stereochemistry on payload release and cytotoxicity.

Main Methods:

  • Synthesis of stereochemically defined RGD peptidomimetics and linker epimers.
  • Preparation and characterization of corresponding SMDCs.
  • In vitro assays including plasma stability, integrin binding (ELISA), enzymatic payload release, and cytotoxicity studies.

Main Results:

  • Conjugates demonstrated stability in human plasma and retained integrin-binding affinity.
  • Rapid payload release was observed upon exposure to human neutrophil elastase, dependent on linker stereochemistry.
  • Enzymatic cleavage restored cryptophycin activity to near free-drug levels, achieving picomolar potency in vitro.

Conclusions:

  • Novel integrin αVβ3-targeting SMDCs were successfully developed.
  • The neutrophil elastase cleavable linker enables targeted payload release and potent anti-cancer activity.
  • These findings support the potential of SMDCs for targeted cancer treatment.