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Ligand Specific Efficiency (LSE) Index for PET Tracer Optimization.

Yves P Auberson1, Emmanuelle Briard2, David Sykes3

  • 1Novartis Institutes for BioMedical Research, Klybeckstrasse 141, 4057, Basel, Switzerland. yves.auberson@novartis.com.

Chemmedchem
|May 20, 2016
PubMed
Summary

A new index, ligand specific efficiency (LSE), uses experimental hydrophobicity to predict nonspecific binding in drug discovery. This aids optimization of imaging agents like PET tracers by quantifying target affinity versus off-target binding.

Keywords:
imaging agentsinhibitor designligand efficiencymedicinal chemistryprostacyclin receptor

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Area of Science:

  • Medicinal Chemistry
  • Radiopharmaceutical Chemistry

Background:

  • Ligand efficiency indices guide early drug discovery but are less effective in later stages.
  • Positron emission tomography (PET) imaging agent development faces challenges with nonspecific binding (NSB), which in silico methods cannot predict.

Purpose of the Study:

  • To introduce and validate the ligand specific efficiency (LSE) index for optimizing NSB in drug discovery.
  • To utilize the experimental chromatographic hydrophobicity index on immobilized artificial membranes (CHI(IAM)) for NSB prediction.

Main Methods:

  • Defined LSE as the ratio of affinity (pIC50 or pKd) to the logarithmic CHI(IAM) value.
  • Applied LSE to guide the optimization of PET tracer candidates for the prostacyclin receptor.

Main Results:

  • The LSE index quantifies target binding affinity relative to NSB.
  • Demonstrated the utility of LSE in optimizing PET tracer candidates, addressing a critical gap in late-stage drug development.

Conclusions:

  • The LSE index, based on experimental CHI(IAM), provides a valuable tool for predicting and optimizing NSB.
  • This approach enhances the development of successful PET imaging agents by improving target specificity.