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Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
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Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.
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Body tissues, comprising approximately 40% of the body weight, are crucial in drug distribution and localization. These tissues can serve as drug storage sites, competing with plasma binding sites for drug molecules.
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Zwitterionic Modification of PSMA Ligands Reduces Off-Target Binding and Tissue Retention.

Lennart F V Spickschen1, Roland Thünauer2, Aleksander J Swierzewski1

  • 1Department of Chemistry, Institute of Pharmacy, University of Hamburg, Bundesstrasse 45, Hamburg 20146, Germany.

Journal of Medicinal Chemistry
|March 13, 2026
PubMed
Summary
This summary is machine-generated.

Zwitterionic modifications in prostate-specific membrane antigen (PSMA)-ligands significantly reduce off-target tissue retention. This strategy enhances tumor uptake and PSMA-binding affinity, offering a promising approach for targeted drug delivery.

Keywords:
PSMA targetingPSMA-617off-target toxicityprostate cancerzwitterions

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Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Molecular Imaging

Background:

  • Prostate-specific membrane antigen (PSMA)-targeted therapies face limitations due to off-target tissue retention.
  • Optimizing PSMA-ligand design is crucial for improving drug biodistribution and therapeutic efficacy.

Purpose of the Study:

  • To investigate the impact of zwitterionic modifications on PSMA-ligand properties.
  • To evaluate the role of zwitterionic groups in influencing tissue distribution and tumor uptake.

Main Methods:

  • Synthesis of fluorescent PSMA-ligands with varying zwitterionic modifications.
  • In vitro evaluation of PSMA-binding affinity (IC50).
  • In vivo biodistribution studies in mice using tumor xenografts.

Main Results:

  • Introduction of two zwitterionic groups in the linker domain proved advantageous.
  • Compound 10 demonstrated high, specific PSMA-binding (IC50 = 4.39 ± 1.69 nM).
  • Compound 10 exhibited excellent tumor cell and xenograft uptake with minimal off-target retention.

Conclusions:

  • Zwitterionization of PSMA-ligands effectively minimizes off-target tissue retention.
  • This strategy simplifies synthesis via solid-phase peptide synthesis and click chemistry.
  • Zwitterionization is a versatile approach transferable to other targeting vectors and radiopharmaceuticals.