Synthesis and Biological Evaluation of New CRH Analogues-Reference-Cited by-同舟云学术

Synthesis and Biological Evaluation of New CRH Analogues

Published:2010 Issue: Volume:2010 Page:1-8
ISSN:1565-3633
Container-title:Bioinorganic Chemistry and Applications
language:en
Short-container-title:Bioinorganic Chemistry and Applications

Author:

Papazacharias Spyridon¹,Magafa Vassiliki¹,Bernad Nicole²,Pairas George¹,Spyroulias Georgios A.¹,Martinez Jean²,Cordopatis Paul¹

Affiliation:

1. Laboratory of Pharmacognosy and Chemistry of Natural Products, Department of Pharmacy, University of Patras, 26500 Patras, Greece

2. Institut des Biomolécules Max Mousseron (IBMM), UMR-CNRS, Faculté de Pharmacie, Universités Montpellier 1 et 2, 15 Av. C. Flahault, 34093 Montpellier, France

Abstract

A series of 7 new human/rat Corticotropin Releasing Hormone (h/r-CRH) analogues were synthesized. The induced alterations include substitution of Phe at position 12 with D-Phe, Leu at positions 14 and 15 with Aib and Met at positions 21 and 38 with Cys(Et) and Cys(Pr). The analogues were tested regarding their binding affinity to the CRH-1 receptor and their activity which is represented by means of percentage of maximum response in comparison to the native molecule. The results indicated that the introduction of Aib, or Cys derivatives although altering the secondary structure of the molecule, did not hinder receptor recognition and binding.

Publisher

Hindawi Limited

Subject

Inorganic Chemistry,Organic Chemistry,Biochemistry

Link

http://downloads.hindawi.com/journals/bca/2010/252348.pdf

Reference40 articles.

1. Characterization of a 41-Residue Ovine Hypothalamic Peptide That Stimulates Secretion of Corticotropin and β-Endorphin

2. Hypothalamic Control of Adrenocorticotropin Secretion: Advances since the Discovery of 41-Residue Corticotropin-Releasing Factor

3. Corticotropin-releasing hormone in humans

4. The rationale for corticotropin-releasing hormone receptor (CRH-R) antagonists to treat depression and anxiety