Heterotrimeric G proteins are known to function as messengers in numerous signal transduction pathways.The nullmutation of RGA(rice heterotrimeric G protein α subunit),which encodes the α subunit of heterotrimeric G...Heterotrimeric G proteins are known to function as messengers in numerous signal transduction pathways.The nullmutation of RGA(rice heterotrimeric G protein α subunit),which encodes the α subunit of heterotrimeric G proteinin rice,causes severe dwarfism and reduced responsiveness to gibberellic acid in rice.However,less is known aboutheterotrimeric G protein in brassinosteroid(BR)signaling,one of the well-understood phytohormone pathways.In thepresent study,we used root elongation inhibition assay,lamina inclination assay and coleoptile elongation analysis todemonstrated reduced sensitivity of dl mutant plants(caused by the null mutation of RGA)to 24-epibrassinolide(24-epiBL),which belongs to brassinosteroids and plays a wide variety of roles in plant growth and development.Moreover,RGA transcript level was decreased in 24-epiBL-treated seedlings in a dose-dependent manner.Our results show thatRGA is involved in rice brassinosteroid response,which may be beneficial to elucidate the molecular mechanisms of Gprotein signaling and provide a novel perspective to understand BR signaling in higher plants.展开更多
Proteolysis targeting chimeras（PROTACs） are bispecific molecules containing a target protein binder and a ubiquitin ligase binder connected by a linker. Recently, some heterobifunctional small molecule bromodomain-c...Proteolysis targeting chimeras（PROTACs） are bispecific molecules containing a target protein binder and a ubiquitin ligase binder connected by a linker. Recently, some heterobifunctional small molecule bromodomain-containing protein 4（BRD4） degraders based on the concept of PROTACs were designed to induce the degradation of BRD4 protein. Herein, we synthesized a new class of PROTAC BRD4 degraders. One of the most promising compound 22f exhibited robust potency of BRD4 inhibition with IC50 value of （9.4±0.6） nmol/L. Furthermore, com- pound 22f potently inhibited cell proliferation in BRD4-sensitive cell lines RS4;11 with IC50 value of （27.6±1.6） nmol/L and capable of inducing degradation of BRD4 protein at 0.5-1.0 μmol/L in the RS4;11 cells. These data establish that compound 22f is a potent and efficacious BRD4 degrader.展开更多
The effect of Gd content on microstructure and magnetic properties of sintered Nd33.03-xGdxFe65.65B1.32 （x=0-2） was studied in this paper to improve the thermal stability of NdFeB and to reduce the raw material cost...The effect of Gd content on microstructure and magnetic properties of sintered Nd33.03-xGdxFe65.65B1.32 （x=0-2） was studied in this paper to improve the thermal stability of NdFeB and to reduce the raw material cost. The results showed that better magnet performance could be obtained by adding Gd （0-1.5 wt.%） with partial substitution of Nd in Nd33.03-xGdxFe65.65B1.32. It was also found that the Nd33.03-xGdxFe65.65B1.32 magnets showed the best performance when Gd addition increased to 1.0 wt.%. The temperature coefficient Br （α） could be improved from -0.15%/oC to -0.063%/oC （maximum work temperature 120 oC） and the Curie temperature could be improved from 315 oC to 323 oC because the Gd2Fe14B had positive temperature coefficient Br （α） and higher Curie temperature than that of Nd2Fe14B. The coercivity could be improved from 10.2 to 11.48 kOe and the microstructure was close to ideal microstructure. The magnetic performance decreased sharply by adding Gd （above 2 wt.%） with partial substitution of Nd in Nd33.03-xGdxFe65.65B1.32 because the Gd element concen-trated in the grain boundaries.展开更多
基金This project was supported by the Major State Basic Research Program of China （2005CB 120806）, National Natural Science Foundation of China for Distinguished Young Scholars （30525026） and the State Transgenic Plant Project （JY04-A-01）
文摘Heterotrimeric G proteins are known to function as messengers in numerous signal transduction pathways.The nullmutation of RGA(rice heterotrimeric G protein α subunit),which encodes the α subunit of heterotrimeric G proteinin rice,causes severe dwarfism and reduced responsiveness to gibberellic acid in rice.However,less is known aboutheterotrimeric G protein in brassinosteroid(BR)signaling,one of the well-understood phytohormone pathways.In thepresent study,we used root elongation inhibition assay,lamina inclination assay and coleoptile elongation analysis todemonstrated reduced sensitivity of dl mutant plants(caused by the null mutation of RGA)to 24-epibrassinolide(24-epiBL),which belongs to brassinosteroids and plays a wide variety of roles in plant growth and development.Moreover,RGA transcript level was decreased in 24-epiBL-treated seedlings in a dose-dependent manner.Our results show thatRGA is involved in rice brassinosteroid response,which may be beneficial to elucidate the molecular mechanisms of Gprotein signaling and provide a novel perspective to understand BR signaling in higher plants.
文摘Proteolysis targeting chimeras（PROTACs） are bispecific molecules containing a target protein binder and a ubiquitin ligase binder connected by a linker. Recently, some heterobifunctional small molecule bromodomain-containing protein 4（BRD4） degraders based on the concept of PROTACs were designed to induce the degradation of BRD4 protein. Herein, we synthesized a new class of PROTAC BRD4 degraders. One of the most promising compound 22f exhibited robust potency of BRD4 inhibition with IC50 value of （9.4±0.6） nmol/L. Furthermore, com- pound 22f potently inhibited cell proliferation in BRD4-sensitive cell lines RS4;11 with IC50 value of （27.6±1.6） nmol/L and capable of inducing degradation of BRD4 protein at 0.5-1.0 μmol/L in the RS4;11 cells. These data establish that compound 22f is a potent and efficacious BRD4 degrader.
基金Project supported by Application of Rare Earth Project of Ministry of Industry and Information Technology of the People's Republic of China (2010 No.1)
文摘The effect of Gd content on microstructure and magnetic properties of sintered Nd33.03-xGdxFe65.65B1.32 （x=0-2） was studied in this paper to improve the thermal stability of NdFeB and to reduce the raw material cost. The results showed that better magnet performance could be obtained by adding Gd （0-1.5 wt.%） with partial substitution of Nd in Nd33.03-xGdxFe65.65B1.32. It was also found that the Nd33.03-xGdxFe65.65B1.32 magnets showed the best performance when Gd addition increased to 1.0 wt.%. The temperature coefficient Br （α） could be improved from -0.15%/oC to -0.063%/oC （maximum work temperature 120 oC） and the Curie temperature could be improved from 315 oC to 323 oC because the Gd2Fe14B had positive temperature coefficient Br （α） and higher Curie temperature than that of Nd2Fe14B. The coercivity could be improved from 10.2 to 11.48 kOe and the microstructure was close to ideal microstructure. The magnetic performance decreased sharply by adding Gd （above 2 wt.%） with partial substitution of Nd in Nd33.03-xGdxFe65.65B1.32 because the Gd element concen-trated in the grain boundaries.
