Zobrazeno 1 - 4
of 4
pro vyhledávání: '"Damien Fraysse"'
Autor:
Clare M. Bolton, Peter Weber, Peter Chiu, Julie Jones, Damien Fraysse, Jimenez Juan Miguel, Elisabeth Doyle, Matthias Hesse, Adam P. Curnock
Publikováno v:
Biochemical Society Transactions. 42:1524-1528
Protein kinase Cθ (PKCθ) is a member of a large family of serine/threonine kinases that are involved in diverse cellular functions. PKCθ has roles in T-cell activation and survival, where the dependency of T-cell responses on this enzyme appears t
Autor:
John Pollard, Francesca Mazzei, Chau Mak, Damien Fraysse, Sanjay Patel, Sharn Ramaya, David Bebbington, John Studley, Joanne Pinder, Ronald Knegtel, Daniel Robinson, Andrew Miller, Francoise Pierard, Michael O'donnell, Alistair Rutherford, Jean-Damien Charrier, David Kay, Michael Mortimore, Simon Everitt, Hayley Binch, Golec Julian M C, James Westcott
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:3586-3592
The identification of a novel series of Aurora kinase inhibitors and exploitation of their SAR is described. Replacement of the initial quinazoline core with a pyrimidine scaffold and modification of substituents led to a series of very potent inhibi
Autor:
Damien Fraysse, Peter Chiu, Philip N. Collier, Heather Twin, Luca Settimo, Francoise Pierard, Dean Boyall, Shazia Keily, Claire M. Bolton, Christopher John Davis, Guy Brenchley, Adam P. Curnock, Jaclyn Henderson, Adam Tanner, Juan-Miguel Jimenez, Andrew Miller, Stephen Clinton Young
Publikováno v:
Journal of medicinal chemistry. 56(5)
Protein kinase C θ (PKCθ) has a central role in T cell activation and survival; however, the dependency of T cell responses to the inhibition of this enzyme appears to be dictated by the nature of the antigen and by the inflammatory environment. St
Autor:
Ronald Knegtel, Ian Ager, Luca Settimo, Stephen Clinton Young, Dean Boyall, Richele K Rasmussen, Claire M. Bolton, Peter Chiu, Adam P. Curnock, Christopher John Davis, Adam Tanner, Juan-Miguel Jimenez, Damien Fraysse
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(14)
The identification of a novel series of PKCθ inhibitors and subsequent optimization using docking based on a crystal structure of PKCθ is described. SAR was rapidly generated around an amino pyridine-ketone hit; (6-aminopyridin-2-yl)(2-aminopyridin