Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Sandra E. Wilkinson"'
Autor:
Harris William, Sandra E. Wilkinson
Publikováno v:
Emerging Drugs. 5:287-297
The tyrosine specific protein kinases (TK) are a subgroup of the largest known gene family, the kinases. Latest estimates suggest that there are over 2000 kinases encoded in the human genome [1]. TKs catalyse the transfer of phosphate to the phenolic
Publikováno v:
Biochemistry. 37:9579-9585
By using high throughput screening of microbial broths, we have identified a compound, designated Ro 09-2210, which is able to block anti-CD3 induced peripheral blood T cell activation with an IC50 = 40 nM. Ro 09-2210 was also able to block antigen-i
Publikováno v:
Expert Opinion on Therapeutic Patents. 7:63-68
The serine/threonine protein kinase isoenzyme family, protein kinase C (PKC), is a group of closely-related enzymes which apparently mediate a range of responses in different cell types. Their involvement in cellular proliferation and differentiation
Autor:
Andrew C. Chan, Sandra E. Wilkinson, David Williams, Paul R. Findell, Robin Johnson, Juliane Bubeck Wardenburg, Janet Jackman, Guanghui Kong, Horst Flotow, Chong Fu
Publikováno v:
Journal of Biological Chemistry. 271:19641-19644
Two families of tyrosine kinases, the Src and Syk families, are required for T-cell receptor activation. While the Src kinases are responsible for phosphorylation of receptor-encoded signaling motifs and for up-regulation of ZAP-70 activity, the down
Autor:
Sandra E. Wilkinson, Janet L. Smith, Peter D. Davis, Harris William, David R. Vesey, John S. Nixon, Geoffrey Lawton, Christopher H. Hill, Trevor J. Hallam
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:1303-1308
A pharmacophore model for the localisation of the cationic binding site of bisindolylmaleimide PKC inhibitors is described. This model has been used to guide selection of further conformationally restricted tertiary amine analogues, culminating in th
Autor:
Sandra E. Wilkinson, Trevor J. Hallam
Publikováno v:
Trends in Pharmacological Sciences. 15:53-57
Evidence has emerged over the past decade to suggest that protein kinase C (PKC) is a widespread family of kinases responsible for many diverse and critical cellular functions. With the development of selective agents to activate or inhibit the indiv
Autor:
H. Kumar, J. Bishop, Hill Christopher Huw, D. Westmacott, Geoffrey Lawton, Peter D. Davis, J. S. Nixon, David Bradshaw, Sandra E. Wilkinson, L H Elliott, E. J. Lewis, MJ Mulqueen, J. Wadsworth
Publikováno v:
Biochemical Society Transactions. 20:419-425
Autor:
Peter D. Davis, Susan E. Turner, Elizabeth Keech, Geoffrey Lawton, Steven A. Hurst, John S. Nixon, Hill Christopher Huw, Sandra E. Wilkinson
Publikováno v:
Journal of Medicinal Chemistry. 35:177-184
The design and synthesis of a series of novel inhibitors of protein kinase C (PKC) is described. These 2,3-bisarylmaleimides were derived from the structural lead provided by the indolocarbazoles, staurosporine and K252a. Optimum activity required th
Autor:
Anthony D. Sedgwick, Peter D. Davis, L H Elliott, Geoffrey Lawton, J. S. Nixon, Sandra E. Wilkinson, Hill Christopher Huw
Publikováno v:
Biochemical and Biophysical Research Communications. 171:148-154
The inhibition of phosphorylase kinase by a number of protein kinase inhibitors was examined. Both K252a and staurosporine are potent inhibitors of phosphorylase kinase with IC50 values of 1.7 nM and 0.5 nM respectively. K252a shows a 300-fold select
Publikováno v:
Cellular signalling. 9(1)
Previous studies implicating a role for protein kinase C (PKC) in mediating stimulation of cellular responses by physiological agonists have relied on use of non-specific inhibitors or direct stimulation of PKC by phorbol esters. However, much of thi