Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Stephen Clinton Young"'
Autor:
Paul S.H. Wang, Michael O'donnell, Alistair Rutherford, John Pollard, Jean-Damien Charrier, Somhairle Maccormick, Ronald Knegtel, Philip Michael Reaper, David Kay, Joanne Pinder, Steven Durrant, Michael Mortimore, Stephen Clinton Young, Golec Julian M C
Publikováno v:
Journal of Medicinal Chemistry. 54:2320-2330
DNA-damaging agents are among the most frequently used anticancer drugs. However, they provide only modest benefit in most cancers. This may be attributed to a genome maintenance network, the DNA damage response (DDR), that recognizes and repairs dam
Autor:
Jothirajah Marimuthu, Mark W. Farmen, Wayne W. Weber, Stuart Donald Jones, Kyle Ja, Michael Robert Wiley, John Walter Liebeschuetz, David Birenbaum Engel, Jeffrey K. Smallwood, Jeffrey B. Franciskovich, Christopher W. Murray, John Joseph Masters, Gerald F. Smith, Scott Martin Sheehan, Stephen Clinton Young
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:2255-2259
A novel isonitrile derivative was synthesized and used in an Ugi four component coupling reaction to explore aryl group substitution effects on inhibition of the coagulation cascade serine protease factor Xa.
Autor:
Jonathan Michael Ernest Roscoe, Bohdan Waszkowycz, Stuart Donald Jones, Andrew David Rimmer, John Walter Liebeschuetz, Jacqui Mahler, Pauline Mary Welsh, William Alexander Wylie, Phillip John Morgan, Harry Martin, KW Wilkinson, Christopher W. Murray, Stephen Clinton Young, Leo Brady
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:733-736
Factor Xa, a critical serine protease in the blood coagulation cascade, has become a target for inhibition as a strategy for the invention of novel anti-thrombotic agents. Here we describe the development of phenylglycine containing benzamidine carbo
Publikováno v:
Drug Discovery Today. 3:105-112
A powerful new approach emerging in drug discovery research combines computational screening of virtual combinatorial libraries against a therapeutic target and targeted combinatorial library synthesis. This new approach includes positive features fr
Autor:
Michael A. Firth, David R. Westhead, Timothy R. Auton, Bohdan Waszkowycz, Jin Li, Richard A. Sykes, Stephen Clinton Young, David E. Clark, Christopher W. Murray
Publikováno v:
Journal of Computer-Aided Molecular Design. 11:193-207
This paper describes a novel methodology, PRO_SELECT, which combines elements of structure-based drug design and combinatorial chemistry to create a new paradigm for accelerated lead discovery. Starting with a synthetically accessible template positi
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
Autor:
Pauline Mary Welsh, Leo Brady, Andrew David Rimmer, William Alexander Wylie, Jonathan Michael Ernest Roscoe, Stuart Donald Macclesfield Jones, KW Wilkinson, Phillip John Morgan, Harry Martin, Jacqui Mahler, Stephen Clinton Young, Bohdan Waszkowycz, Christopher William Murray, John Walter Liebeschuetz
Publikováno v:
Journal of medicinal chemistry. 45(6)
In silico screening of combinatorial libraries prior to synthesis promises to be a valuable aid to lead discovery. PRO_SELECT, a tool for the virtual screening of libraries for fit to a protein active site, has been used to find novel leads against t