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Related Concept Videos

Peptide Bonds02:43

Peptide Bonds

81.6K
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...
81.6K

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Updated: Jan 4, 2026

Constructing Thioether/Vinyl Sulfide-tethered Helical Peptides Via Photo-induced Thiol-ene/yne Hydrothiolation
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Utilizing peptide structures as keys for unlocking challenging targets.

David Fry1, Hongmao Sun

  • 1Department of Discovery Chemistry, Hoffmann-La Roche, Nutley, NJ, USA.

Mini Reviews in Medicinal Chemistry
|October 5, 2006
PubMed
Summary
This summary is machine-generated.

Structural insights from peptide ligands aid drug discovery when protein structures are unavailable. This approach helps identify drug targets and design improved small molecule drugs.

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Area of Science:

  • Medicinal Chemistry
  • Structural Biology
  • Pharmacology

Background:

  • Three-dimensional protein structures are crucial for drug design.
  • G-protein coupled receptors (GPCRs) often lack attainable structures.
  • Structural information from active ligands is vital for understanding active sites.

Purpose of the Study:

  • To review the utility of peptide ligands in drug discovery.
  • To demonstrate how peptide structures elucidate target active sites.
  • To guide the design of small molecule drugs.

Main Methods:

  • Utilizing structural information from peptide ligands.
  • Employing nuclear magnetic resonance (NMR) for structural investigation.
  • Developing pharmacophore models from peptide structures.

Main Results:

  • Peptide ligands provide valuable geometrical and chemical insights into protein active sites.
  • Quantitative structure-activity relationships (QSAR) are efficiently generated using peptides.
  • Accurate pharmacophore models are derived from peptide structural data.

Conclusions:

  • Structural studies of peptide ligands enhance understanding of target active sites.
  • Peptide-based structural information aids in virtual screening and drug design.
  • This approach facilitates the development of peptidomimetics and non-peptidic leads.