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Related Concept Videos

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.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
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.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as 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...
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...

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Identifying protein stabilizing ligands using GroEL.

Subhashchandra Naik1, Inamul Haque, Nick Degner

  • 1Department of Biochemistry and Molecular Biology, University of Kansas Medical Center, Kansas City, KS, USA.

Biopolymers
|October 6, 2009
PubMed
Summary

Gene replacement therapies show limited application for protein folding diseases. New screening methods targeting misfolding reactions offer potential for developing targeted drug therapies.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Drug Discovery

Background:

  • Protein folding diseases affect 30-50% of human diseases.
  • Current gene replacement therapies have limited applicability.
  • Targeting fundamental misfolding reactions is a feasible therapeutic approach.

Purpose of the Study:

  • To develop a broad-based screening array method for identifying ligands against protein misfolding reactions.
  • To overcome limitations of current gene replacement therapies for protein folding diseases.

Main Methods:

  • Utilizing a chaperonin-based detection platform.
  • Screening large chemical combinatorial libraries.
  • Identifying specific ligands targeting transient, primary misfolding reactions.

Main Results:

  • A novel screening array method was developed.
  • The method enables identification of ligands against elusive protein misfolding pathways.
  • This approach is applicable to both common and orphan protein folding diseases.

Conclusions:

  • The developed screening method provides a powerful tool for pharmaceutical and academic research.
  • This approach holds significant potential for developing targeted drug therapies for protein folding diseases.
  • Further development can accelerate drug discovery for a wide range of debilitating conditions.