Potent selective inhibitors of protein kinase C.
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).
Davis
P D
PD
Research Centre, Roche Products Ltd., Welwyn Garden City, Herts., England.
Hill
C H
CH
Keech
E
E
Lawton
G
G
Nixon
J S
JS
Sedgwick
A D
AD
Wadsworth
J
J
Westmacott
D
D
Wilkinson
S E
SE
D000470:Alkaloids / Q000494:pharmacology; D000818:Animals; D000945:Antigens, Differentiation, T-Lymphocyte / Q000378:metabolism; D001792:Blood Platelets / Q000378:metabolism; D001921:Brain / Q000201:enzymology; D017252:CD3 Complex; D002227:Carbazoles / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D015536:Down-Regulation / Q000187:drug effects; D007094:Imides; D026121:Indole Alkaloids; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*; D047428:Protein Kinase Inhibitors; D051381:Rats; D011948:Receptors, Antigen, T-Cell / Q000378:metabolism; D019311:Staurosporine; D013329:Structure-Activity Relationship
D000470:Alkaloids; D000945:Antigens, Differentiation, T-Lymphocyte; D017252:CD3 Complex; D002227:Carbazoles; D007094:Imides; D026121:Indole Alkaloids; D047428:Protein Kinase Inhibitors; D011948:Receptors, Antigen, T-Cell; C049985:staurosporine aglycone; D011493:Protein Kinase C; D019311:Staurosporine