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排序方式: 共有1303条查询结果,搜索用时 31 毫秒
1.
Prof. Andrea Baier Dr. Anne Kokel Dr. William Horton Ewa Gizińska Dr. Garima Pandey Prof. Ryszard Szyszka Prof. Béla Török Prof. Marianna Török 《ChemMedChem》2021,16(12):1927-1932
A set of novel hydrazone derivatives were synthesized and analyzed for their biological activities. The compounds were tested for their inhibitory effect on the phosphorylating activity of the protein kinase CK2, and their antioxidant activity was also determined in three commonly used assays. The hydrazones were evaluated for their radical scavenging against the DPPH, ABTS and peroxyl radicals. Several compounds have been identified as good antioxidants as well as potent protein kinase CK2 inhibitors. Most hydrazones containing a 4-N(CH3)2 residue or perfluorinated phenyl rings showed high activity in the radical-scavenging assays and possess nanomolar IC50 values in the kinase assays. 相似文献
2.
对赤红球菌的组氨酸激酶基因进行密码子优化,将优化后的组氨酸激酶基因(rhks)构建重组表达质粒pGEX-4T-2-rhks。将此质粒导入到大肠杆菌BL21(DE3)中进行异源表达。在25 ℃和1 mmol/L异丙基-β-D-硫代吡喃半乳糖苷诱导条件下,组氨酸激酶融合蛋白(GST-RHK)获得成功表达,并具有催化活性。经谷胱甘肽琼脂糖亲和层析纯化,获得电泳纯的GST-RHK,其中纯化倍数为3.1,得率为19.5%。该蛋白大小约为72.75 kDa,Km、Vmax和Kcat值分别为20.92 μmol/L、0.17 μmol/(L·min)和1.4 min-1。野生型赤红球菌、组氨酸激酶基因增强株sdrhkE和组氨酸激酶基因敲减株sdrhkD在分别含有苯酚、甲苯、氯苯、异辛烷4 种有机溶剂的培养基中培养,菌株sdrhkD的生长情况都优于野生型赤红球菌,菌株sdrhkE的生长情况都低于野生型赤红球菌。本研究为进一步揭示赤红球菌SD3中组氨酸激酶涉及的信号转导途径与赤红球菌有机溶剂耐受性的关联机制提供一定参考依据。 相似文献
3.
Alice Maurer Prof. Dr. Florian P. Seebeck 《Chembiochem : a European journal of chemical biology》2020,21(20):2908-2911
Ergothioneine has emerged as a crucial cytoprotectant in the pathogenic lifestyle of Mycobacterium tuberculosis. Production of this antioxidant from primary metabolites may be regulated by phosphorylation of Thr213 in the active site of the methyltransferase EgtD. The structure of mycobacterial EgtD suggests that this post-translational modification would require a large-scale change in conformation to make the active-site residue accessible to a protein kinase. In this report, we show that, under in vitro conditions, EgtD is not a substrate of protein kinase PknD. 相似文献
4.
Dr. Hui Qiu Richard Caldwell Dr. Lesley Liu-Bujalski Dr. Andreas Goutopoulos Reinaldo Jones Justin Potnick Dr. Brian Sherer Dr. Andrew Bender Dr. Roland Grenningloh Dr. Daigen Xu Dr. Anna Gardberg Dr. Igor Mochalkin Dr. Theresa Johnson Dr. Ariele Viacava Follis Jared Head Dr. Federica Morandi 《ChemMedChem》2019,14(2):217-223
Bruton's tyrosine kinase (Btk) is an attractive target for the treatment of a wide array of B-cell malignancies and autoimmune diseases. Small-molecule covalent irreversible Btk inhibitors targeting Cys481 have been developed for the treatment of such diseases. In clinical trials, probe molecules are required in occupancy studies to measure the level of engagement of the protein by these covalent irreversible inhibitors. The result of this pharmacodynamic (PD) activity provides guidance for appropriate dosage selection to optimize inhibition of the drug target and correlation of target inhibition with disease treatment efficacy. This information is crucial for successful evaluation of drug candidates in clinical trials. Based on the pyridine carboxamide scaffold of a novel solvent-accessible pocket (SAP) series of covalent irreversible Btk inhibitors, we successfully developed a potent and selective affinity-based biotinylated probe 12 (2-[(4-{4-[5-(1-{5-[(3aS,4S,6aR)-2-oxo-hexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanamido}-3,6,9,12-tetraoxapentadecan-15-amido)pentanoyl]piperazine-1-carbonyl}phenyl)amino]-6-[1-(prop-2-enoyl)piperidin-4-yl]pyridine-3-carboxamide). Compound 12 has been used in Btk occupancy assays for preclinical studies to determine the therapeutic efficacy of Btk inhibition in two mouse lupus models driven by TLR7 activation and type I interferon. 相似文献
5.
6.
Ha-Nul Lee Joo-Hee Choi Ji-Yeon Park Jae-Hun Ahn Da Eun Jang Jae Gun Shim Jong-Hwan Park Young-Min Kim 《Food science and biotechnology》2021,30(4):583
Vegetable soup (VS), a plant-based functional food, has been used as a traditional folk medicine and is attracting attention for its ability to enhance the immune response. β-Glucan, a well-established and effective immunomodulator, has synergistic effects when used in combination with some bioactive compounds. In the present study, we aimed to evaluate the synergistic immunomodulatory effects of the combination of VS and β-glucan on macrophage-mediated immune responses. β-Glucan was demonstrated to synergistically enhance the VS-stimulated immune response, including the production of interleukin-6, tumor necrosis factor-α, and nitric oxide, mainly through the mitogen-activated protein kinase pathway in macrophages. In addition, this combination has the potential for further development in functional foods with immune-enhancing activity.Supplementary InformationThe online version contains supplementary material available at 10.1007/s10068-021-00888-x. 相似文献
7.
The role of arginine vasopressin (AVP) in the nongenomic transfer of paternal behavior from fathers to offspring was examined in Peromyscus. Male California mice (P. californicus) exposed to fewer retrievals by white-footed mouse (P. leucopus) foster parents displayed fewer retrievals of biological offspring. In contrast, white-footed mice were retrieved equally rarely by California mouse foster parents and by biological parents and displayed no changes in pup retrieval behavior. AVP-immunoreactive staining in the bed nucleus of the stria terminalis may predict paternal behavior because it correlated positively with retrievals and with a score consisting of huddling, grooming, and time inside the nest. The authors discuss AVP as a possible mechanism by which early experience shapes adult paternal behavior. (PsycINFO Database Record (c) 2010 APA, all rights reserved) 相似文献
8.
Johan M. Thevelein 《Yeast (Chichester, England)》1994,10(13):1753-1790
9.
We present an analysis of a stochastic model of the vascular endothelial growth factor (VEGF) receptor. This analysis addresses the contribution of ligand-binding-induced oligomerization, activation of src-homology 2 domain-carrying kinases and receptor internalization in the overall behaviour of the VEGF/VEGF receptor (VEGFR) system. The analysis is based upon a generalization of a Wentzel-Kramers-Brillouin (WKB) approximation of the solution of the corresponding master equation. We predict that tumour-mediated overexpression of VEGFRs in the endothelial cells (ECs) of tumour-engulfed vessels leads to an increased sensitivity of the ECs to low concentrations of VEGF, thus endowing the tumour with increased resistance to anti-angiogenic treatment. 相似文献
10.