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排序方式: 共有2563条查询结果,搜索用时 15 毫秒
1.
《International Journal of Hydrogen Energy》2022,47(67):29172-29183
To improve the safety of wet dust removal systems for processing magnesium-based alloys, a new method is proposed for preventing hydrogen generation. In this paper, hydrogen generation by Mg–Zn alloy dust was inhibited with six common metal corrosion inhibitors. The results showed that sodium dodecylbenzene sulfonate was the best hydrogen inhibitor, while CeCl3 enhanced hydrogen precipitation. The film-forming stability of sodium dodecylbenzene sulfonate was tested with different contents, temperatures, Cl? concentrations and perturbation rates. The results showed that this inhibitor formed stable protective films on the surfaces of Mg–Zn alloy particles, and adsorption followed the Langmuir adsorption model. 相似文献
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Nikhil K. Tulsian Valerie Jia-En Sin Hwee-Ling Koh Ganesh S. Anand 《International journal of molecular sciences》2021,22(10)
Phosphodiesterases (PDEs) hydrolyze cyclic nucleotides to modulate multiple signaling events in cells. PDEs are recognized to actively associate with cyclic nucleotide receptors (protein kinases, PKs) in larger macromolecular assemblies referred to as signalosomes. Complexation of PDEs with PKs generates an expanded active site that enhances PDE activity. This facilitates signalosome-associated PDEs to preferentially catalyze active hydrolysis of cyclic nucleotides bound to PKs and aid in signal termination. PDEs are important drug targets, and current strategies for inhibitor discovery are based entirely on targeting conserved PDE catalytic domains. This often results in inhibitors with cross-reactivity amongst closely related PDEs and attendant unwanted side effects. Here, our approach targeted PDE–PK complexes as they would occur in signalosomes, thereby offering greater specificity. Our developed fluorescence polarization assay was adapted to identify inhibitors that block cyclic nucleotide pockets in PDE–PK complexes in one mode and disrupt protein-protein interactions between PDEs and PKs in a second mode. We tested this approach with three different systems—cAMP-specific PDE8–PKAR, cGMP-specific PDE5–PKG, and dual-specificity RegA–RD complexes—and ranked inhibitors according to their inhibition potency. Targeting PDE–PK complexes offers biochemical tools for describing the exquisite specificity of cyclic nucleotide signaling networks in cells. 相似文献
4.
Dr. Tommaso Felicetti Prof. Giuseppe Manfroni Prof. Violetta Cecchetti Dr. Rolando Cannalire 《ChemMedChem》2020,15(24):2391-2419
Infections by flaviviruses, such as Dengue, West Nile, Yellow Fever and Zika viruses, represent a growing risk for global health. There are vaccines only for few flaviviruses while no effective treatments are available. Flaviviruses share epidemiological, structural, and ecologic features and often different viruses can co-infect the same host. Therefore, the identification of broad-spectrum inhibitors is highly desirable either for known flaviviruses or for viruses that likely will emerge in the future. Strategies targeting both virus and host factors have been pursued to identify broad-spectrum antiflaviviral agents. In this review, we describe the most promising and best characterized targets and their relative broad-spectrum inhibitors, identified by drug repurposing/libraries screenings and by focused medicinal chemistry campaigns. Finally, we discuss about future strategies to identify new broad-spectrum antiflavivirus agents. 相似文献
5.
Dr. Feng Wang. Dr. Shan Li Taiping Gan Dr. Gordon M. Stott Dr. Andrew Flint Dr. Tsui-Fen Chou 《ChemMedChem》2020,15(8):685-694
Abstract : A major challenge of targeted cancer therapy is the selection for drug-resistant mutations in tumor cells leading to loss of treatment effectiveness. p97/VCP is central regulator of protein homeostasis and a promising anticancer target because of its vital role in cell growth and survival. One ATP-competitive p97 inhibitor, CB-5083, has entered clinical trials. Selective pressure on HCT116 cells dosed with CB-5083 identified five different resistant mutants. Identification of p97 inhibitors with different mechanisms of action would offer the potential to overcome this class of resistance mutations. Our results demonstrate that two CB-5083 resistant p97 mutants, N660 K and T688 A, were also resistant to several other ATP-competitive p97 inhibitors, whereas inhibition by two allosteric p97 inhibitors NMS-873 and UPCDC-30245 were unaffected by these mutations. We also established a CB-5083 resistant cell line that harbors a new p97 double mutation (D649 A/T688 A). While CB-5083, NMS-873, and UPCDC-30245 all effectively inhibited proliferation of the parental HCT116 cell line, NMS-873 and UPCDC-30245 were 30-fold more potent in inhibiting the CB-5083 resistant D649 A/T688 A double mutant than CB-5083. Our results suggest that allosteric p97 inhibitors are promising alternatives when resistance to ATP-competitive p97 inhibitors arises during anticancer treatment. 相似文献
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Nina ukanovi Slobodan Obradovi Marija Zdravkovi Sinia uraevi Maja Stojkovi Tomislav Tosti Neboja Jasni Jelena orevi Zoran Todorovi 《International journal of molecular sciences》2021,22(6)
Lipids play an essential role in platelet functions. It is known that polyunsaturated fatty acids play a role in increasing platelet reactivity and that the prothrombotic phenotype plays a crucial role in the occurrence of major adverse cardiovascular events. The ongoing increase in cardiovascular diseases’ incidence emphasizes the importance of research linking lipids and platelet function. In particular, the rebound phenomenon that accompanies discontinuation of clopidogrel in patients receiving dual antiplatelet therapy has been associated with changes in the lipid profile. Our many years of research underline the importance of reduced HDL values for the risk of such a rebound effect and the occurrence of thromboembolic events. Lipids are otherwise a heterogeneous group of molecules, and their signaling molecules are not deposited but formed “on-demand” in the cell. On the other hand, exosomes transmit lipid signals between cells, and the profile of such changes can be monitored by lipidomics. Changes in the lipid profile are organ-specific and may indicate new drug action targets. 相似文献
8.
Dr. Elena Petit Dr. Lluís Bosch Prof. Anna M. Costa Ignacio Rodríguez-Izquierdo Dr. Daniel Sepúlveda-Crespo Prof. M. Angeles Muñoz-Fernández Prof. Jaume Vilarrasa 《ChemMedChem》2021,16(14):2217-2222
Amides from indole-3-glyoxylic acid and 4-benzoyl-2-methylpiperazine, which are related to entry inhibitors developed by Bristol-Myers Squibb (BMS), have been synthesized with aliphatic chains located at the C7 position of the indole ring. These spacers contain an azido group suitable for the well-known Cu(I)-catalyzed (3+2)-cycloaddition or an activated triple bond for the nucleophilic addition of thiols under physiological conditions. Reaction with polyols (β-cyclodextrin and hyperbranched polyglycerol) decorated with complementary click partners has afforded polyol-BMS-like conjugates that are not cytotoxic (TZM.bl cells) and retain the activity against R5-HIV-1NLAD8 isolates. Thus, potential vaginal microbicides based on entry inhibitors, which can be called of 4th generation, are reported here for the first time. 相似文献
9.
Roberta Bastos Vasques Marjory Moreira Levy Matheus Souza Rodrigues Francisco Wagner de Queiroz Almeida Neto Leonardo Paes da Silva Gustavo Leitão Vaz Álvaro Augusto Oliveira Magalhães Pedro de Lima-Neto Walney Silva Araújo 《工业材料与腐蚀》2021,72(8):1417-1432
Phosphate ester was investigated as a corrosion inhibitor for AISI 1018 carbon steel in carbon dioxide-saturated chloride solutions at different temperatures and pressures. The corrosion tests were realized by electrochemical techniques, weight loss measurements, bubble tests, and a high-pressure/high-temperature autoclave system. The corrosion tests demonstrated that the investigated molecule is an excellent corrosion inhibitor. The inhibiting effect is even bigger at high pressure and temperature than at atmospheric pressure and room temperature. The thermodynamic parameters were calculated and determined to obey the Langmuir isotherm. Polarization studies revealed that the evaluated inhibitor is a mixed type. 相似文献
10.
Dr. Avisek Mahapa Gopal Ch Samanta Dr. Krishnagopal Maiti Prof. Dipankar Chatterji Prof. Narayanaswamy Jayaraman 《Chembiochem : a European journal of chemical biology》2019,20(15):1966-1976
Lipomannan and lipoarabinomannan are integral components of the mycobacterial cell wall. Earlier studies demonstrated that synthetic arabinan and arabinomannan glycolipids acted as inhibitors of mycobacterial growth, in addition to exhibiting inhibitory activities of mycobacterial biofilm. Herein, it is demonstrated that synthetic mannan glycolipids are better inhibitors of mycobacterial growth, whereas lipoarabinomannan has a higher inhibition efficiency to biofilm. Syntheses of mannan glycolipids with a graded number of mannan moieties and an arabinomannan glycolipid are conducted by chemical methods and subsequent mycobacterial growth and biofilm inhibition studies are conducted on Mycobacterium smegmatis. Growth inhibition of (73±3) % is observed with a mannose trisaccharide containing a glycolipid, whereas this glycolipid did not promote biofilm inhibition activity better than that of arabinomannan glycolipid. The antibiotic supplementation activities of glycolipids on growth and biofilm inhibitions are evaluated. Increases in growth and biofilm inhibitions are observed if the antibiotic is supplemented with glycolipids, which leads to a significant reduction of inhibition concentrations of the antibiotic. 相似文献