Synthesis and Biological Evaluation of New CRH Analogues

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 rega...

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Autores principales: Papazacharias, Spyridon, Magafa, Vassiliki, Bernad, Nicole, Pairas, George, Spyroulias, Georgios A., Martinez, Jean, Cordopatis, Paul
Formato: Texto
Lenguaje:English
Publicado: Hindawi Publishing Corporation 2010
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2905701/
https://www.ncbi.nlm.nih.gov/pubmed/20689735
http://dx.doi.org/10.1155/2010/252348
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author Papazacharias, Spyridon
Magafa, Vassiliki
Bernad, Nicole
Pairas, George
Spyroulias, Georgios A.
Martinez, Jean
Cordopatis, Paul
author_facet Papazacharias, Spyridon
Magafa, Vassiliki
Bernad, Nicole
Pairas, George
Spyroulias, Georgios A.
Martinez, Jean
Cordopatis, Paul
author_sort Papazacharias, Spyridon
collection PubMed
description 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.
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spelling pubmed-29057012010-08-05 Synthesis and Biological Evaluation of New CRH Analogues Papazacharias, Spyridon Magafa, Vassiliki Bernad, Nicole Pairas, George Spyroulias, Georgios A. Martinez, Jean Cordopatis, Paul Bioinorg Chem Appl Research Article 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. Hindawi Publishing Corporation 2010 2010-06-28 /pmc/articles/PMC2905701/ /pubmed/20689735 http://dx.doi.org/10.1155/2010/252348 Text en Copyright © 2010 Spyridon Papazacharias et al. https://creativecommons.org/licenses/by/3.0/ This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Article
Papazacharias, Spyridon
Magafa, Vassiliki
Bernad, Nicole
Pairas, George
Spyroulias, Georgios A.
Martinez, Jean
Cordopatis, Paul
Synthesis and Biological Evaluation of New CRH Analogues
title Synthesis and Biological Evaluation of New CRH Analogues
title_full Synthesis and Biological Evaluation of New CRH Analogues
title_fullStr Synthesis and Biological Evaluation of New CRH Analogues
title_full_unstemmed Synthesis and Biological Evaluation of New CRH Analogues
title_short Synthesis and Biological Evaluation of New CRH Analogues
title_sort synthesis and biological evaluation of new crh analogues
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2905701/
https://www.ncbi.nlm.nih.gov/pubmed/20689735
http://dx.doi.org/10.1155/2010/252348
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