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Related Concept Videos

Peptide Bonds02:43

Peptide Bonds

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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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Ligand Binding and Linkage00:49

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Allosteric proteins have more than one ligand binding site; the binding of a ligand to any of these sites influences the binding of ligands to the other sites. When a protein is allosteric, its binding sites are called coupled or linked.  In the case of enzymes, the site that binds to the substrate is known as the active site and the other site is known as the regulatory site. When a ligand binds to the regulatory site, this leads to conformational changes in the protein that can influence...
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Phase II Conjugation Reactions: Overview01:14

Phase II Conjugation Reactions: Overview

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Conjugation, a key component of phase II biotransformation reactions, is a vital process in drug detoxification. It involves transferring endogenous substances like glucuronic acid, sulfate, and glycine to drugs or their metabolites formed in phase I reactions. These conjugation reactions, often catalyzed by specific enzymes, transform potentially harmful metabolites into inactive, water-soluble forms easily excreted in urine or bile. By enhancing polarity and eliminating pharmacological...
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Linkers for effective peptide-drug conjugates.

Mohamad Fajar1, Rani Maharani2, Unang Supratman2

  • 1Department of Chemistry, Chemistry, Faculty of Mathematics and Natural Sciences, Universitas Padjadjaran, Sumedang 45363, West Java, Indonesia.

Bioorganic & Medicinal Chemistry
|December 11, 2025
PubMed
Summary

Peptide-drug conjugates (PDCs) offer targeted cancer therapy by using peptides to deliver cytotoxic drugs specifically to tumor cells, minimizing side effects and improving treatment outcomes.

Keywords:
Anticancer agentLinker designPeptide-drug conjugateTargeted therapy

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Area of Science:

  • Oncology
  • Pharmacology
  • Bioconjugation Chemistry

Background:

  • Conventional chemotherapies lack tumor selectivity, causing significant side effects and limiting therapeutic efficacy.
  • Existing treatments often harm healthy cells alongside cancerous ones, reducing the therapeutic index.
  • Targeted delivery systems are needed to enhance cancer treatment precision.

Purpose of the Study:

  • To review advancements in peptide-drug conjugate (PDC) chemistry for targeted cancer therapy.
  • To emphasize the critical role of linkers in PDC design and function.
  • To explore future research directions in PDC-based drug delivery systems.

Main Methods:

  • Comprehensive literature review of existing peptide-drug conjugate strategies.
  • Analysis of linker chemistries and their impact on conjugate stability and drug release.
  • Examination of synthetic methodologies for creating PDCs.
  • Discussion of receptor targeting mechanisms utilized by PDCs.

Main Results:

  • PDCs demonstrate improved drug delivery to cancer cells compared to conventional agents.
  • Linker selection significantly influences PDC pharmacokinetics, bioavailability, and efficacy.
  • Understanding drug-active sites and peptide-recognition sites is crucial for effective PDC synthesis.
  • PDCs offer a promising strategy to enhance anticancer efficacy while reducing systemic toxicity.

Conclusions:

  • Peptide-drug conjugates represent a significant advancement in targeted cancer therapy.
  • Optimizing linker design and synthetic methods is key to maximizing PDC therapeutic potential.
  • Further research into PDC chemistries can lead to more effective and safer cancer treatments.