The effects of 2-[p-(Dimethylamino)styryl] pyridine methiodide(DSPM)on slow response action potential(SRAP)and slow inward current(Isi) of guinea pig papillary muscles were studied by intracellular microelectrodes and...The effects of 2-[p-(Dimethylamino)styryl] pyridine methiodide(DSPM)on slow response action potential(SRAP)and slow inward current(Isi) of guinea pig papillary muscles were studied by intracellular microelectrodes and voltage clamp techniques.The APA and V_(max) of SRAP induced by high K￣+were decreased after 50 min of perfusion with DSPM solu- tion. Isi was suppressed from a peak value of8.8± 1.6μA to 5.7± 1.8μA, The results indicated that DSPM has a selective blocking effect on calcium channel.展开更多
14-3-3 is a highly conserved acidic protein family, composed of seven isoforms in mammals. 14-3-3 protein caninteract with over 200 target proteins by phosphoserine-dependent and phosphoserine-independent manners. Lit...14-3-3 is a highly conserved acidic protein family, composed of seven isoforms in mammals. 14-3-3 protein caninteract with over 200 target proteins by phosphoserine-dependent and phosphoserine-independent manners. Little isknown about the consequences of these interactions, and thus are the subjects of ongoing studies. 14-3-3 controls cellcycle, cell growth, differentiation, survival, apoptosis, migration and spreading. Recent studies have revealed newmechanisms and new functions of 14-3-3, giving us more insights on this fascinating and complex family of proteins.Of all the seven isoforms, 14-3-3σ seems to be directly involved in human cancer. 14-3-3σ itself is subject to regulationby p53 upon DNA damage and by epigenetic deregulation. Gene silencing of 14-3-3σ by CpG methylation has beenfound in many human cancer types. This suggests that therapy-targeting 14-3-3σ may be beneficial for future cancertreatment.展开更多
An efficient Cu catalyzed selective arylation/annulation cascade reaction of 2-alkynylanilines with diaryliodonium salts was developed.This reaction was selective to N-arylation instead of C-arylation,which provides a...An efficient Cu catalyzed selective arylation/annulation cascade reaction of 2-alkynylanilines with diaryliodonium salts was developed.This reaction was selective to N-arylation instead of C-arylation,which provides a simple synthetic method for N-aryl indoles.展开更多
A new crystalline form of carboxypeptidase A (CPA) complexes withan inactivator was obtained by the method of hanging drop vapor diffusion. The inacti-’vator, 2-benzyl-3-iodo-propanoic acid (BIPA ), binds covalently ...A new crystalline form of carboxypeptidase A (CPA) complexes withan inactivator was obtained by the method of hanging drop vapor diffusion. The inacti-’vator, 2-benzyl-3-iodo-propanoic acid (BIPA ), binds covalently to an active siteresidue Glu-27O of CPA. The complex was crystallized in space group P212121 with a= 48. 8 A, b=66. 9 A, c= 96. 0 A. The complex structure was determined by molecu-lar replacement using the native CPA crystal structure as the search model. The finalcrystallographic residual is 0. 152. Except for the modification of Glu-270, the inactiva-tor exhibits normal binding mode compared with other ligand complexes of CPA. Inthe final different electron density maps (2Fo-Fc, Fo-Fc), the density of the iodo ioncould not be found while the conserved molecule remains coordinated to Zn2+ as in thenative CPA. Comparisons of complex of CPA-BIPA with the native CPA and theCPA/D-Phe complex are presented. The mechanism of inactivation of CPA was dis-cussed.展开更多
A simple and direct route for double C–C bond formation by copper-catalyzed Meerwein carboarylation process has been developed. In the presence of Cu I(5 mol%), tert-butyl nitrite and anilines, a wide variety of N-ar...A simple and direct route for double C–C bond formation by copper-catalyzed Meerwein carboarylation process has been developed. In the presence of Cu I(5 mol%), tert-butyl nitrite and anilines, a wide variety of N-arylacrylamides underwent tandem Meerwein arylation/C–H cyclization to produce pharmaceutically important 3-benzyl-3-alkyloxindole in moderate to good yield.展开更多
文摘The effects of 2-[p-(Dimethylamino)styryl] pyridine methiodide(DSPM)on slow response action potential(SRAP)and slow inward current(Isi) of guinea pig papillary muscles were studied by intracellular microelectrodes and voltage clamp techniques.The APA and V_(max) of SRAP induced by high K￣+were decreased after 50 min of perfusion with DSPM solu- tion. Isi was suppressed from a peak value of8.8± 1.6μA to 5.7± 1.8μA, The results indicated that DSPM has a selective blocking effect on calcium channel.
文摘14-3-3 is a highly conserved acidic protein family, composed of seven isoforms in mammals. 14-3-3 protein caninteract with over 200 target proteins by phosphoserine-dependent and phosphoserine-independent manners. Little isknown about the consequences of these interactions, and thus are the subjects of ongoing studies. 14-3-3 controls cellcycle, cell growth, differentiation, survival, apoptosis, migration and spreading. Recent studies have revealed newmechanisms and new functions of 14-3-3, giving us more insights on this fascinating and complex family of proteins.Of all the seven isoforms, 14-3-3σ seems to be directly involved in human cancer. 14-3-3σ itself is subject to regulationby p53 upon DNA damage and by epigenetic deregulation. Gene silencing of 14-3-3σ by CpG methylation has beenfound in many human cancer types. This suggests that therapy-targeting 14-3-3σ may be beneficial for future cancertreatment.
基金supported by the Intercollegiate Key Scientific Research Projects of Henan Province(15A150018)~~
文摘An efficient Cu catalyzed selective arylation/annulation cascade reaction of 2-alkynylanilines with diaryliodonium salts was developed.This reaction was selective to N-arylation instead of C-arylation,which provides a simple synthetic method for N-aryl indoles.
文摘A new crystalline form of carboxypeptidase A (CPA) complexes withan inactivator was obtained by the method of hanging drop vapor diffusion. The inacti-’vator, 2-benzyl-3-iodo-propanoic acid (BIPA ), binds covalently to an active siteresidue Glu-27O of CPA. The complex was crystallized in space group P212121 with a= 48. 8 A, b=66. 9 A, c= 96. 0 A. The complex structure was determined by molecu-lar replacement using the native CPA crystal structure as the search model. The finalcrystallographic residual is 0. 152. Except for the modification of Glu-270, the inactiva-tor exhibits normal binding mode compared with other ligand complexes of CPA. Inthe final different electron density maps (2Fo-Fc, Fo-Fc), the density of the iodo ioncould not be found while the conserved molecule remains coordinated to Zn2+ as in thenative CPA. Comparisons of complex of CPA-BIPA with the native CPA and theCPA/D-Phe complex are presented. The mechanism of inactivation of CPA was dis-cussed.
基金supported by the National Natural Science Foundation of China(21462017)China Posdoctoral Science Foundation Funded Project(2014M560649)+2 种基金the Scientific Research Fund of Hunan Provincial Education Department(13B094)the Fund of Science and Technology Innovation and Entrepreneur for Hunan Young Talentsthe Project Sponsored by the Scientific Research Foundation for the Returned Overseas Chinese Scholars,State Education Ministry for the financial and infrastructural assistance
文摘A simple and direct route for double C–C bond formation by copper-catalyzed Meerwein carboarylation process has been developed. In the presence of Cu I(5 mol%), tert-butyl nitrite and anilines, a wide variety of N-arylacrylamides underwent tandem Meerwein arylation/C–H cyclization to produce pharmaceutically important 3-benzyl-3-alkyloxindole in moderate to good yield.
