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
A novel intermolecular phosphoryl transfer from O-trimethylsilyl-N-(O, O-diisopropyl) phosphoryl serine trimethylsilyl ester to N, Nbis(trimethylsilyl) histidine trimethylsilyl ester was studied through electrospray i...A novel intermolecular phosphoryl transfer from O-trimethylsilyl-N-(O, O-diisopropyl) phosphoryl serine trimethylsilyl ester to N, Nbis(trimethylsilyl) histidine trimethylsilyl ester was studied through electrospray ionization mass spectrometry (ESI-MS). It was proposed that the transfer reaction went through penta-coordinated phosphorus intermediate.展开更多
Hydrolysis procedure of N-phosphoryl phenylalanine (DIPP-Phe) was studied by HPLC-ESI-MS/MS. The results showed that (HO)(i-PrO)P(O)Phe was the main intermediate and the hydrolysis of DIPP-Phe also occurred through a ...Hydrolysis procedure of N-phosphoryl phenylalanine (DIPP-Phe) was studied by HPLC-ESI-MS/MS. The results showed that (HO)(i-PrO)P(O)Phe was the main intermediate and the hydrolysis of DIPP-Phe also occurred through a penta-coordinate transition state.展开更多
N-Phosphoryl peptide libraries were constructed by transformation from homo-oligopeptide libraries, which was synthesized by self-assembly of amino acids with the assistance of phosphorus oxychloride. Electrospray ion...N-Phosphoryl peptide libraries were constructed by transformation from homo-oligopeptide libraries, which was synthesized by self-assembly of amino acids with the assistance of phosphorus oxychloride. Electrospray ionization mass spectrometry (ESI-MS) was used to monitor the reaction.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.
文摘A novel intermolecular phosphoryl transfer from O-trimethylsilyl-N-(O, O-diisopropyl) phosphoryl serine trimethylsilyl ester to N, Nbis(trimethylsilyl) histidine trimethylsilyl ester was studied through electrospray ionization mass spectrometry (ESI-MS). It was proposed that the transfer reaction went through penta-coordinated phosphorus intermediate.
文摘Hydrolysis procedure of N-phosphoryl phenylalanine (DIPP-Phe) was studied by HPLC-ESI-MS/MS. The results showed that (HO)(i-PrO)P(O)Phe was the main intermediate and the hydrolysis of DIPP-Phe also occurred through a penta-coordinate transition state.
文摘N-Phosphoryl peptide libraries were constructed by transformation from homo-oligopeptide libraries, which was synthesized by self-assembly of amino acids with the assistance of phosphorus oxychloride. Electrospray ionization mass spectrometry (ESI-MS) was used to monitor the reaction.
