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Related Concept Videos

Metal-Ligand Bonds02:51

Metal-Ligand Bonds

The hemoglobin in the blood, the chlorophyll in green plants, vitamin B-12, and the catalyst used in the manufacture of polyethylene all contain coordination compounds. Ions of the metals, especially the transition metals, are likely to form complexes.
In these complexes, transition metals form coordinate covalent bonds, a kind of Lewis acid-base interaction in which both of the electrons in the bond are contributed by a donor (Lewis base) to an electron acceptor (Lewis acid). The Lewis acid in...
Ligand Binding and Linkage00:49

Ligand Binding and Linkage

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 the...
Ligand Binding and Linkage00:49

Ligand Binding and Linkage

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 the...
Complexometric Titration: Ligands00:43

Complexometric Titration: Ligands

Different monodentate and polydentate ligands are used as complexing agents in complexometric titration reactions. The formation of complexes by mono- and bidentate ligands involves two or more intermediate steps, limiting their use as complexing agents. In comparison, polydentate ligands can form complexes with metal ions in a single-step process, facilitating sharper end points. This means polydentate ligands, such as amino carboxylic acid derivatives, are most commonly employed in...
Complexation Equilibria: The Chelate Effect01:19

Complexation Equilibria: The Chelate Effect

In complexation reactions, metal atoms or cations interact with ligands to form donor-acceptor adducts called metal complexes. Ligands that bind through one donor site are monodentate, ligands with two donor sites are bidentate, and those with more than two donor sites are polydentate ligands. For example, ethylene diamine is a bidentate ligand that binds through two nitrogen donor atoms, forming a five-membered ring. EDTA is a polydentate ligand that binds through four oxygen and two nitrogen...
Ligand Binding Sites02:40

Ligand Binding Sites

Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
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Ligand Nano-cluster Arrays in a Supported Lipid Bilayer
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Published on: April 23, 2017

Bivalent ligands with long nanometer-scale flexible linkers.

Ling Tian1, Tomasz Heyduk

  • 1Edward A. Doisy Department of Biochemistry and Molecular Biology, St. Louis University Medical School, 1100 South Grand Boulevard, St. Louis, Missouri 63104, USA.

Biochemistry
|December 31, 2008
PubMed
Summary

Researchers created high-affinity aptamer ligands by linking two suboptimal aptamers with a flexible linker. This bivalent ligand approach significantly enhances binding affinity and specificity for biomolecule detection and drug discovery.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Drug Discovery

Background:

  • High-affinity ligands with specific biomolecule recognition are vital for drug discovery and detection.
  • Aptamers are nucleic acid-based ligands with great potential in these fields.

Purpose of the Study:

  • To develop a simple method for preparing aptamer-based ligands with enhanced binding affinity.
  • To investigate the principles of affinity enhancement through bivalent ligand construction.

Main Methods:

  • Covalently linking two suboptimal aptamer ligands with a long, flexible linker to create bivalent ligands.
  • Using an oligonucleotide model to study the principles of affinity enhancement.
  • Employing a wormlike chain model to predict bivalent ligand properties.
  • Constructing aptamer-based bivalent ligands for human alpha-thrombin.

Main Results:

  • Linking suboptimal aptamers with a flexible linker significantly improved binding affinity and specificity.
  • The wormlike chain model accurately predicted the binding properties of flexible bivalent ligands.
  • Aptamer-based bivalent ligands for human alpha-thrombin demonstrated enhanced binding affinity and anticlotting activity.

Conclusions:

  • A simple strategy of creating bivalent aptamer ligands by linking suboptimal aptamers with flexible linkers effectively enhances binding affinity and specificity.
  • This approach holds promise for advancing drug discovery and biomolecule detection technologies.