Protein kinase catalyzes the transfer of the γ-phosphoryl group from ATP to the hydroxyl groups of protein side chains, which plays critical roles in signal transduction pathways by transmitting extracellular signals...Protein kinase catalyzes the transfer of the γ-phosphoryl group from ATP to the hydroxyl groups of protein side chains, which plays critical roles in signal transduction pathways by transmitting extracellular signals across the plasma membrane and nuclear membrane to the destination sites in the cytoplasm and the nucleus. Protein kinase C (PKC) is a superfamily of phospholipid-dependent Ser/Thr kinase. There are at least 12 isozymes in PKC family. They are distributed in different tissues and play different roles in physiological processes. On account of their concern with a variety of pathophysiologic states, such as cancer, inflammatory conditions, autoimmune disorder, and cardiac diseases, the inhibitors, which can inhibit the activity of PKC and the interaction of cytokine with receptor, and interfere signal transduction pathway, may be candidates of therapeu-tic drugs. Therefore, intense efforts have been made to de-velop specific protein kinase inhibitors as biological tools and therapeutic agents. This article reviews the recent develop-ment of some of PKC inhibitors based on their interaction with different conserved domains and different inhibition mechanisms.展开更多
Apoptosis as a mechanism of deleting cells from tissues plays an important role in physiological and varieties of pathological situations, especially cancer conditions. In order to search for tumor cells apoptosis ind...Apoptosis as a mechanism of deleting cells from tissues plays an important role in physiological and varieties of pathological situations, especially cancer conditions. In order to search for tumor cells apoptosis inducers, the inhibition effects on K562 cells of N-phosphoryl dipeptide methyl esters were studied by MTT assays, and (DIPP-L-Leu)2- L-Lys-OCH3 was the compound which had the best activity. From the studies of the typical apoptotic morphologic changes, DNA agarose gel electrophoresis, and flow cytometry analysis, it could be concluded that (DIPP-L-Leu)2- L-Lys-OCH3 could induce apoptosis of K562 cells in a dose-dependent manner, and the IC50 was 22.66 mol/L according to MTT assays.展开更多
基金supported by the National Natural Science Foundation of China(Grant No.20472043).
文摘Protein kinase catalyzes the transfer of the γ-phosphoryl group from ATP to the hydroxyl groups of protein side chains, which plays critical roles in signal transduction pathways by transmitting extracellular signals across the plasma membrane and nuclear membrane to the destination sites in the cytoplasm and the nucleus. Protein kinase C (PKC) is a superfamily of phospholipid-dependent Ser/Thr kinase. There are at least 12 isozymes in PKC family. They are distributed in different tissues and play different roles in physiological processes. On account of their concern with a variety of pathophysiologic states, such as cancer, inflammatory conditions, autoimmune disorder, and cardiac diseases, the inhibitors, which can inhibit the activity of PKC and the interaction of cytokine with receptor, and interfere signal transduction pathway, may be candidates of therapeu-tic drugs. Therefore, intense efforts have been made to de-velop specific protein kinase inhibitors as biological tools and therapeutic agents. This article reviews the recent develop-ment of some of PKC inhibitors based on their interaction with different conserved domains and different inhibition mechanisms.
基金supported by the National Natural Science Foundation of China(Grant No.20132020).
文摘Apoptosis as a mechanism of deleting cells from tissues plays an important role in physiological and varieties of pathological situations, especially cancer conditions. In order to search for tumor cells apoptosis inducers, the inhibition effects on K562 cells of N-phosphoryl dipeptide methyl esters were studied by MTT assays, and (DIPP-L-Leu)2- L-Lys-OCH3 was the compound which had the best activity. From the studies of the typical apoptotic morphologic changes, DNA agarose gel electrophoresis, and flow cytometry analysis, it could be concluded that (DIPP-L-Leu)2- L-Lys-OCH3 could induce apoptosis of K562 cells in a dose-dependent manner, and the IC50 was 22.66 mol/L according to MTT assays.
