Investigation of the inhibitory effects of HA-1077 and Y-32885 on the translocation of PKCβI, PKCβII and PKCζ in human neutrophils
To transmit the information inside the cell, one possibility is the action of an enzyme called kinase that phosphorylates other proteins. To study these enzymes, chemical compound synthesis was needed to know the function and the mechanism of activation. The major difficulty is creating a specific m...
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| Format: | Article |
| Language: | English |
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Wiley
2001-01-01
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| Series: | Mediators of Inflammation |
| Online Access: | http://dx.doi.org/10.1080/09629350120102334 |
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| _version_ | 1832551699641794560 |
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| author | Xavier Siomboing Bernard Gressier Thierry Dine Claude Brunet Michel Luyckx Michelene Cazin Jean-Claude Cazin |
| author_facet | Xavier Siomboing Bernard Gressier Thierry Dine Claude Brunet Michel Luyckx Michelene Cazin Jean-Claude Cazin |
| author_sort | Xavier Siomboing |
| collection | DOAJ |
| description | To transmit the information inside the cell, one possibility is the action of an enzyme called kinase that phosphorylates other proteins. To study these enzymes, chemical compound synthesis was needed to know the function and the mechanism of activation. The major difficulty is creating a specific molecule for one kinase. In this study, we test the action of Rho-kinase inhibitors (HA-1077 and Y-32885) on protein kinase C (PKC) in the respiratory burst in the human polymorphonuclear neutrophils. We have shown that these compounds could inhibit the anion superoxide production. To prove their action on PKC, we have shown a decrease of binding of a specific ligand (phorbol-12,13-dibutyrate) with each inhibitor. During its activation, PKC was translocated from the cytoplasm to the plasmic membrane. We have also shown an inhibition of this translocation, proving an inhibition of PKC by HA-1077 and Y-32885. |
| format | Article |
| id | doaj-art-c33e3f15b1ec42059d1ab790bddc2ee5 |
| institution | Kabale University |
| issn | 0962-9351 1466-1861 |
| language | English |
| publishDate | 2001-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Mediators of Inflammation |
| spelling | doaj-art-c33e3f15b1ec42059d1ab790bddc2ee52025-02-03T06:00:51ZengWileyMediators of Inflammation0962-93511466-18612001-01-0110631532110.1080/09629350120102334Investigation of the inhibitory effects of HA-1077 and Y-32885 on the translocation of PKCβI, PKCβII and PKCζ in human neutrophilsXavier Siomboing0Bernard Gressier1Thierry Dine2Claude Brunet3Michel Luyckx4Michelene Cazin5Jean-Claude Cazin6Faculté des Sciences Pharmaceutiques et Biologiques, Laboratoire de Pharmacologie, Pharmacocinétique et Pharmacie Cliniques, rue du Professeur Laguesse, B.P. 83, Lille cedex, Lille 59006, FranceFaculté des Sciences Pharmaceutiques et Biologiques, Laboratoire de Pharmacologie, Pharmacocinétique et Pharmacie Cliniques, rue du Professeur Laguesse, B.P. 83, Lille cedex, Lille 59006, FranceFaculté des Sciences Pharmaceutiques et Biologiques, Laboratoire de Pharmacologie, Pharmacocinétique et Pharmacie Cliniques, rue du Professeur Laguesse, B.P. 83, Lille cedex, Lille 59006, FranceFaculté des Sciences Pharmaceutiques et Biologiques, Laboratoire de Pharmacologie, Pharmacocinétique et Pharmacie Cliniques, rue du Professeur Laguesse, B.P. 83, Lille cedex, Lille 59006, FranceFaculté des Sciences Pharmaceutiques et Biologiques, Laboratoire de Pharmacologie, Pharmacocinétique et Pharmacie Cliniques, rue du Professeur Laguesse, B.P. 83, Lille cedex, Lille 59006, FranceFaculté des Sciences Pharmaceutiques et Biologiques, Laboratoire de Pharmacologie, Pharmacocinétique et Pharmacie Cliniques, rue du Professeur Laguesse, B.P. 83, Lille cedex, Lille 59006, FranceFaculté des Sciences Pharmaceutiques et Biologiques, Laboratoire de Pharmacologie, Pharmacocinétique et Pharmacie Cliniques, rue du Professeur Laguesse, B.P. 83, Lille cedex, Lille 59006, FranceTo transmit the information inside the cell, one possibility is the action of an enzyme called kinase that phosphorylates other proteins. To study these enzymes, chemical compound synthesis was needed to know the function and the mechanism of activation. The major difficulty is creating a specific molecule for one kinase. In this study, we test the action of Rho-kinase inhibitors (HA-1077 and Y-32885) on protein kinase C (PKC) in the respiratory burst in the human polymorphonuclear neutrophils. We have shown that these compounds could inhibit the anion superoxide production. To prove their action on PKC, we have shown a decrease of binding of a specific ligand (phorbol-12,13-dibutyrate) with each inhibitor. During its activation, PKC was translocated from the cytoplasm to the plasmic membrane. We have also shown an inhibition of this translocation, proving an inhibition of PKC by HA-1077 and Y-32885.http://dx.doi.org/10.1080/09629350120102334 |
| spellingShingle | Xavier Siomboing Bernard Gressier Thierry Dine Claude Brunet Michel Luyckx Michelene Cazin Jean-Claude Cazin Investigation of the inhibitory effects of HA-1077 and Y-32885 on the translocation of PKCβI, PKCβII and PKCζ in human neutrophils Mediators of Inflammation |
| title | Investigation of the inhibitory effects of HA-1077 and Y-32885 on the translocation of PKCβI, PKCβII and PKCζ in human neutrophils |
| title_full | Investigation of the inhibitory effects of HA-1077 and Y-32885 on the translocation of PKCβI, PKCβII and PKCζ in human neutrophils |
| title_fullStr | Investigation of the inhibitory effects of HA-1077 and Y-32885 on the translocation of PKCβI, PKCβII and PKCζ in human neutrophils |
| title_full_unstemmed | Investigation of the inhibitory effects of HA-1077 and Y-32885 on the translocation of PKCβI, PKCβII and PKCζ in human neutrophils |
| title_short | Investigation of the inhibitory effects of HA-1077 and Y-32885 on the translocation of PKCβI, PKCβII and PKCζ in human neutrophils |
| title_sort | investigation of the inhibitory effects of ha 1077 and y 32885 on the translocation of pkcβi pkcβii and pkcζ in human neutrophils |
| url | http://dx.doi.org/10.1080/09629350120102334 |
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