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Related Concept Videos

Site-Targeted Drug Delivery Systems: Polymeric Carriers01:24

Site-Targeted Drug Delivery Systems: Polymeric Carriers

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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A peptide bond covalently attaches amino acids through a dehydration reaction. One amino acid's carboxyl group and another amino acid's amino group combine, releasing a water molecule. The resulting bond is the peptide bond. The products that such linkages form are peptides. As more amino acids join this growing chain, the resulting chain is a polypeptide. Each polypeptide has a free amino group at one end. This end has the N-terminal, or the amino-terminal, and the other end has a free...

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Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
08:48

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Published on: January 26, 2016

Polycyclic peptide therapeutics.

Vanessa Baeriswyl1, Christian Heinis

  • 1Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne, 1015 Lausanne, Switzerland.

Chemmedchem
|January 29, 2013
PubMed
Summary
This summary is machine-generated.

Polycyclic peptides offer stable, targeted therapeutic potential. New technologies enable the development of novel polycyclic peptide drugs for diverse diseases, expanding therapeutic options beyond natural sources.

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Area of Science:

  • Medicinal Chemistry
  • Molecular Biology
  • Drug Discovery

Background:

  • Polycyclic peptides possess advantageous properties like high stability, strong binding affinity, and low toxicity, making them promising therapeutic candidates.
  • Current clinically approved polycyclic peptide drugs are exclusively derived from natural sources, limiting their application to targets for which natural ligands exist.
  • The scarcity of naturally occurring polycyclic peptides for many therapeutic targets necessitates the development of synthetic strategies.

Purpose of the Study:

  • To review the molecular architectures and properties of existing polycyclic peptide therapeutics.
  • To discuss emerging technologies for creating novel, unnatural polycyclic peptide ligands.
  • To highlight the potential of these advanced technologies in developing polycyclic peptide therapeutics for a wider range of diseases.

Main Methods:

  • Analysis of existing polycyclic peptide drugs and their natural origins.
  • Exploration of methods for engineering natural polycyclic peptide scaffolds with artificial binding sites (rational design, directed evolution).
  • Discussion of de novo generation of genetically encoded bicyclic peptide libraries and screening via phage display.

Main Results:

  • Existing polycyclic peptide drugs demonstrate the therapeutic value linked to their unique molecular structures.
  • Engineered scaffolds and de novo libraries have successfully generated novel peptide ligands.
  • Recent technological advancements show promising results in developing polycyclic peptides for previously untargeted diseases.

Conclusions:

  • Polycyclic peptides represent a versatile and potent class of molecules for therapeutic development.
  • Synthetic biology and combinatorial approaches are crucial for overcoming the limitations of natural product discovery.
  • The continued innovation in polycyclic peptide technology holds significant promise for future drug development across various medical fields.