Potent selective inhibitors of protein kinase C

P D Davis; C H Hill; E Keech; G Lawton; J S Nixon; A D Sedgwick; J Wadsworth; D Westmacott; S E Wilkinson

doi:10.1016/0014-5793(89)81494-2

Potent selective inhibitors of protein kinase C

FEBS Lett. 1989 Dec 18;259(1):61-3. doi: 10.1016/0014-5793(89)81494-2.

Authors

P D Davis¹, C H Hill, E Keech, G Lawton, J S Nixon, A D Sedgwick, J Wadsworth, D Westmacott, S E Wilkinson

Affiliation

¹ Research Centre, Roche Products Ltd., Welwyn Garden City, Herts., England.

PMID: 2532156
DOI: 10.1016/0014-5793(89)81494-2

Abstract

A series of potent, selective inhibitors of protein kinase C has been derived from the structural lead provided by the microbial broth products, staurosporine and K252a. Our inhibitors block PCK in intact cells (platelets and T cells), and prevent the proliferation of mononuclear cells in response to interleukin 2 (IL2).

MeSH terms

Alkaloids / pharmacology
Animals
Antigens, Differentiation, T-Lymphocyte / metabolism
Blood Platelets / metabolism
Brain / enzymology
CD3 Complex
Carbazoles / pharmacology
Dose-Response Relationship, Drug
Down-Regulation / drug effects
Imides
Indole Alkaloids
Protein Kinase C / antagonists & inhibitors*
Protein Kinase Inhibitors
Rats
Receptors, Antigen, T-Cell / metabolism
Staurosporine
Structure-Activity Relationship

Substances

Alkaloids
Antigens, Differentiation, T-Lymphocyte
CD3 Complex
Carbazoles
Imides
Indole Alkaloids
Protein Kinase Inhibitors
Receptors, Antigen, T-Cell
staurosporine aglycone
Protein Kinase C
Staurosporine