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Cyclizing Painkillers: Development of Backbone-Cyclic TAPS Analogs.

Alaa Talhami1, Avi Swed2, Shmuel Hess3

  • 1Department of Organic Chemistry, Institute of Chemistry, The Hebrew University of Jerusalem, Jerusalem, Israel.

Frontiers in Chemistry
|December 7, 2020
PubMed
Summary

Researchers developed a novel backbone-cyclic peptide painkiller, TAPS c(2-6), offering improved drug properties over traditional painkillers. This metabolically stable compound acts as a full μ opioid receptor agonist, showing potential as a peripheral painkiller.

Keywords:
TAPSbackbone cyclizationcycloscanperipheral painkillerreductive alkylation

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Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Peptide Science

Background:

  • Native peptide painkillers have limitations, and small molecule options like morphine are addictive.
  • Developing safer and more effective pain management solutions is a priority.

Purpose of the Study:

  • To create a novel peptidomimetic painkiller using backbone-cyclization.
  • To design and synthesize a library of backbone-cyclic Tyr-Arg-Phe-Sar (TAPS) analogs.
  • To identify a potent and metabolically stable peptide painkiller candidate.

Main Methods:

  • Backbone-cyclization of the linear peptide Tyr-Arg-Phe-Sar (TAPS).
  • Synthesis of a focused TAPS backbone-cyclic library (TAPS c(n-m)).
  • Combined screening for pharmacological properties and potency, including in vivo evaluation.
  • Optimization of solid-phase peptide synthesis (SPPS) for TAPS c(2-6) production.
  • Nuclear Magnetic Resonance (NMR) spectroscopy for conformational analysis.

Main Results:

  • A library of backbone-cyclic TAPS analogs was synthesized.
  • TAPS c(2-6) demonstrated in vivo activity, metabolic stability, and full μ opioid receptor agonism.
  • Optimized SPPS conditions enhanced the yield of TAPS c(2-6).
  • The solution conformation of TAPS c(2-6) was determined by NMR.

Conclusions:

  • Backbone-cyclization is a viable strategy for developing improved peptide painkillers.
  • TAPS c(2-6) is a promising lead compound for a new class of peripheral painkillers.
  • Further development of TAPS c(2-6) could lead to safer pain management alternatives.