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Related Concept Videos

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...
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...
EDTA: Chemistry and Properties01:22

EDTA: Chemistry and Properties

Polydentate ligands are most widely used in complexometric titrations because they form more stable complexes with the metal ions than mono- or bidentate ligands due to the chelate effect. Examples of polydentate ligands are ethylenediaminetetraacetic acid (EDTA), crown ethers, and cryptands. The most important feature of optimal polydentate ligands is the ability to form 1:1 complexes in a single-step process. Amino carboxylic acid derivatives are frequently used as complexing agents. EDTA is...
Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...

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A11-positive &#946;-amyloid Oligomer Preparation and Assessment Using Dot Blotting Analysis
06:17

A11-positive β-amyloid Oligomer Preparation and Assessment Using Dot Blotting Analysis

Published on: May 22, 2018

Multivalent & multifunctional ligands to beta-amyloid.

YoungSoo Kim1, Ji Hoon Lee, Jiyeon Ryu

  • 1Center for Chemoinformatics Research, Life Sciences Research Division, Korea Institute of Science and Technology, Seoul, South Korea.

Current Pharmaceutical Design
|February 10, 2009
PubMed
Summary

Multivalent ligands targeting beta-amyloid offer a promising strategy for Alzheimer's disease therapeutics and diagnostics. These advanced ligands enhance binding affinity and address multiple pathological factors for improved treatment outcomes.

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Selection of Aptamers for Amyloid &beta;-Protein, the Causative Agent of Alzheimer&#39;s Disease
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Selection of Aptamers for Amyloid &beta;-Protein, the Causative Agent of Alzheimer&#39;s Disease
15:23

Selection of Aptamers for Amyloid β-Protein, the Causative Agent of Alzheimer's Disease

Published on: May 13, 2010

Area of Science:

  • Neuroscience
  • Pharmacology
  • Biochemistry

Background:

  • Alzheimer's disease (AD) is characterized by beta-amyloid (Aβ) aggregation, posing challenges for effective therapeutics and early diagnosis.
  • Current monovalent Aβ ligands show limitations due to incomplete understanding of AD pathology.
  • The Aβ cascade involves protein misfolding, oxidative stress, inflammation, and metal interactions, necessitating multifaceted therapeutic approaches.

Purpose of the Study:

  • To review multivalent and multifunctional Aβ ligands as an alternative therapeutic and diagnostic strategy for Alzheimer's disease.
  • To highlight the advantages of multivalent approaches in enhancing binding affinity and targeting diverse pathological aspects of AD.
  • To discuss the potential of these ligands in addressing the complexities of the Aβ cascade.

Main Methods:

  • Review of existing literature on monovalent and multivalent beta-amyloid ligands.
  • Analysis of studies focusing on targeting different stages of Aβ aggregation (monomers, oligomers, fibrils).
  • Examination of strategies incorporating multivalent effects and multifunctional designs for enhanced efficacy.

Main Results:

  • Multivalent Aβ ligands demonstrate enhanced binding affinity compared to monovalent counterparts.
  • Multifunctional ligands can simultaneously target multiple pathological pathways involved in AD.
  • These approaches show potential for both therapeutic intervention and diagnostic imaging in Alzheimer's disease.

Conclusions:

  • Multivalent and multifunctional Aβ ligands represent a promising advancement in Alzheimer's disease research.
  • These ligands offer a more comprehensive strategy by improving binding and addressing the multifaceted nature of AD pathology.
  • Further investigation into these ligands is crucial for developing effective treatments and diagnostic tools for Alzheimer's disease.