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Better agonist for the opioid receptors

Authors
  • Badshah, Syed Lal1
  • Ullah, Asad1
  • Al-showiman, Salim S.2
  • Mabkhot, Yahia Nasser2
  • 1 Islamia College University, Department of Chemistry, Peshawar, 25120, Pakistan , Peshawar (Pakistan)
  • 2 King Saud University, Department of Chemistry, College of Sciences, Riyadh, Saudi Arabia , Riyadh (Saudi Arabia)
Type
Published Article
Journal
Chemistry Central Journal
Publisher
Springer International Publishing
Publication Date
Feb 08, 2018
Volume
12
Issue
1
Identifiers
DOI: 10.1186/s13065-018-0383-8
Source
Springer Nature
Keywords
License
Green

Abstract

This commentary highlights the recent work published in journal Nature on the structural based discovery of novel analgesic compounds for opioid receptors with minimal effects. Manglik et al. selectively targeted the Gi based μOR pathway instead of the β-arrestin pathway of the opioids. The computational screening of millions of compounds showed a list of several competent ligands. From these ligands they synthesized the compounds with the best docking score, which were further optimized by adding side residues for better interaction with the μOR. A promising compound, PZM21, was a selective agonist of μOR. It has better analgesic properties with minimal side effects of respiratory depression and constipation. This work is a step towards better drug designing and synthesizing in terms of efficacy, specificity with least side effects of targeted GPCR proteins present in the human proteome.

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