Biochemistry & Pharmacology: Open Access
Open Access

C Rougeot

Publications

• Research Article
  Structure- Activity Relationship Study and Function-Based Petidomimetic Design of Human Opiorphin with Improved Bioavailability Property and Unaltered Analgesic Activity
  Author(s): Alexandra Bogeas, Evelyne Dufour, Jean-François Bisson, Michael Messaoudi and C RougeotAlexandra Bogeas, Evelyne Dufour, Jean-François Bisson, Michael Messaoudi and C Rougeot
  
  Human opiorphin inhibits enkephalin-inactivating ectopeptidases to produce analgesic and antidepressant-like effects in standard murine models via activation of μ and/or δ opioid pathways. It is an endogenous peptide regulator of enkephalin bioavailability. Opiorphin molecule, a QRFSR-peptide, is thus a promising prototype for the design of an improved class of analgesics. The major limitation on the clinical use of peptide drugs is their rapid degradation by circulating peptidases. Our goal was, therefore, to search for functional derivatives of opiorphin with improved metabolic stability. In order to identify the functional amino acid groups required for opiorphin inhibitory potency toward both AP-N and NEP human ectopeptidases, we used the Structure-Activity Relationship (SAR) method. From this data, a series of opiorphin derivatives was designed and selected. The best per.. View More»
  DOI: 10.4172/2167-0501.1000122

  Abstract PDF

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