Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Yea Christopher Martyn"'
Autor:
Yea Christopher Martyn, Marc Princivalle, Gaell Mayer, Jessica Meyer, Lucy Elliott, Pierre Broqua, Ketil Bjarnason, Richard E. White, Robert Haigh
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 320:1113-1118
Degarelix (FE 200486) is a member of a new class of water-soluble (50 mg/ml) gonadotropin-releasing hormone (GnRH) antagonists in clinical development for prostate cancer. Upon subcutaneous administration, degarelix forms a gel that results in a sust
Autor:
Pitt Gary Robert William, Rooker David Philip, Robert Haigh, Andrew M. Penson, Andrzej Roman Batt, André Tartar, Peter A. Robson, Julie E. Trim, Michael Bryan Roe, Yea Christopher Martyn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:4585-4589
A library of compounds targeted to the vasopressin/oxytocin family of receptors was screened for activity at a cloned human oxytocin receptor using a reporter gene assay. Potency and selectivity were optimised to afford compound 39, EC50 = 33 nM. Thi
Autor:
Erik Ruuthb, Richard A. Williamson, Yea Christopher Martyn, T. Andrew Thomson, Elizabeth Anne Kuo, Robert Westwood, Adam P. Curnock
Publikováno v:
Biochemical Pharmacology. 61:227-235
HR325 (2-cyano-3-cyclopropyl-3-hydroxy- N -[3′-methyl-4′(trifluoromethyl)-phenyl]-propenamide) is an immunomodulatory compound through pyrimidine biosynthesis inhibition with antiproliferative properties which was derived from the isoxazol compou
Autor:
Catherine Sautes, Richard A. Williamson, Erik Ruuth, Claude Fudali, Peter A. Robson, Elizabeth Anne Kuo, Jean-Michel Bruneau, Katherine Woodward, Robert Westwood, Sylviane Spinella-Jaegle, Yea Christopher Martyn
Publikováno v:
Biochemical Journal. 336:299-303
Leflunomide is currently in phase-III clinical trials for the treatment of rheumatoid arthritis. In this study, we have focused our efforts on the study of the mechanism of action of the active metabolite of leflunomide, A77 1726, in cells and tissue
Autor:
S. Spinella-Jaegle, A. B. Hambleton, Adam P. Curnock, P. Hambleton, K. Woodward, J.-M. Bruneau, Erik Ruuth, Yea Christopher Martyn, E. A. Kuo, O. Courtin, Robert Westwood, D. Moss, T. A. Thomson, Catherine Sautes, Richard A. Williamson, Suresh Gadher, Peter A. Robson, P. Morand, T. Hercend
Publikováno v:
Journal of Biological Chemistry. 270:22467-22472
A protein with high affinity (Kd 12 nM) for the immunomodulatory compound A77 1726 has been isolated from mouse spleen and identified as the mitochondrial enzyme dihydroorotate dehydrogenase (EC 1.3.3.1). The purified protein had a pI 9.6-9.8 and a s
Autor:
James Barnett, Andy Sheppard, Andy J Baxter, Robert Haigh, Doreen Mary Ashworth, John Horton, Janice D Broadbridge, Michael Bryan Roe, Christine Elizabeth Allan, Richard Jeremy Franklin, Sally L Hampton, Peter A. Robson, Graeme San Diego Semple, Andy M Penson, Pierre Riviere, Rooker David Philip, Peter Hudson, Pitt Gary Robert William, Yea Christopher Martyn, Paul David Jenkins
Publikováno v:
Journal of medicinal chemistry. 51(24)
Vasopressin (AVP) is a hormone that stimulates an increase in water permeability through activation of V2 receptors in the kidney. The analogue of AVP, desmopressin, has proven an effective drug for diseases where a reduction of urine output is desir
Autor:
C. B. Jones, E. A. Kuo, Yea Christopher Martyn, C. J. R. Hedgecock, Peter W. Hairsine, N. Mcdowall, R. A. Williamson, P. Hambleton, W. R. Tully, Robert Westwood, Saroop S. Matharu, Ian R. Ager, David Kay, A. W. E. Chan, P. L. Evans, E. Little
Publikováno v:
Journal of medicinal chemistry. 39(23)
The active metabolite (2) of the novel immunosuppressive agent leflunomide (1) has been shown to inhibit the enzyme dihydroorotate dehydrogenase (DHODH). This enzyme catalyzes the fourth step in de novo pyrimidine biosynthesis. A series of analogues