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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| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
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Wiley
2010-01-01
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| Series: | Bioinorganic Chemistry and Applications |
| Online Access: | http://dx.doi.org/10.1155/2010/252348 |
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| author | Spyridon Papazacharias Vassiliki Magafa Nicole Bernad George Pairas Georgios A. Spyroulias Jean Martinez Paul Cordopatis |
| author_facet | Spyridon Papazacharias Vassiliki Magafa Nicole Bernad George Pairas Georgios A. Spyroulias Jean Martinez Paul Cordopatis |
| author_sort | Spyridon Papazacharias |
| collection | DOAJ |
| 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. |
| format | Article |
| id | doaj-art-3f83686e654e46b88608536af3098f0e |
| institution | Kabale University |
| issn | 1565-3633 1687-479X |
| language | English |
| publishDate | 2010-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Bioinorganic Chemistry and Applications |
| spelling | doaj-art-3f83686e654e46b88608536af3098f0e2025-02-03T06:05:26ZengWileyBioinorganic Chemistry and Applications1565-36331687-479X2010-01-01201010.1155/2010/252348252348Synthesis and Biological Evaluation of New CRH AnaloguesSpyridon Papazacharias0Vassiliki Magafa1Nicole Bernad2George Pairas3Georgios A. Spyroulias4Jean Martinez5Paul Cordopatis6Laboratory of Pharmacognosy and Chemistry of Natural Products, Department of Pharmacy, University of Patras, 26500 Patras, GreeceLaboratory of Pharmacognosy and Chemistry of Natural Products, Department of Pharmacy, University of Patras, 26500 Patras, GreeceInstitut des Biomolécules Max Mousseron (IBMM), UMR-CNRS, Faculté de Pharmacie, Universités Montpellier 1 et 2, 15 Av. C. Flahault, 34093 Montpellier, FranceLaboratory of Pharmacognosy and Chemistry of Natural Products, Department of Pharmacy, University of Patras, 26500 Patras, GreeceLaboratory of Pharmacognosy and Chemistry of Natural Products, Department of Pharmacy, University of Patras, 26500 Patras, GreeceInstitut des Biomolécules Max Mousseron (IBMM), UMR-CNRS, Faculté de Pharmacie, Universités Montpellier 1 et 2, 15 Av. C. Flahault, 34093 Montpellier, FranceLaboratory of Pharmacognosy and Chemistry of Natural Products, Department of Pharmacy, University of Patras, 26500 Patras, GreeceA 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.http://dx.doi.org/10.1155/2010/252348 |
| spellingShingle | Spyridon Papazacharias Vassiliki Magafa Nicole Bernad George Pairas Georgios A. Spyroulias Jean Martinez Paul Cordopatis Synthesis and Biological Evaluation of New CRH Analogues Bioinorganic Chemistry and Applications |
| 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 |
| url | http://dx.doi.org/10.1155/2010/252348 |
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