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51.
Chandra Bhushan Mishra Dimpy Sharma Amresh Prakash Namrata Kumari Nitin Kumar Pratibha Mehta Luthra 《Bioorganic & medicinal chemistry》2013,21(19):6077-6083
Novel 2-thioxothiazole derivatives (6–19) as potential adenosine A2A receptor (A2AR) antagonists were synthesized. The strong interaction of the compounds (6–19) with A2AR in docking study was confirmed by high binding affinity with human A2AR expressed in HEK293T cells using radioligand-binding assay. The compound 19 demonstrated very high selectivity for A2AR as compared to standard A2AR antagonist SCH58261. Decrease in A2AR-coupled release of endogenous cAMP in treated HEK293T cells demonstrated in vitro A2AR antagonist potential of the compound 19. Attenuation in haloperidol-induced impairment (catalepsy) in Swiss albino male mice pre-treated with compound 19 is evocative to explore its prospective in therapy of PD. 相似文献
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The present study explores the suitability of chemical reaction-based and diffusion-based kinetic models for defining the biosorption of Cu(II), Cd(II) and Pb(II) by Phormidium sp.-dominated mat. The time-course data of metal sorption by the test mat significantly (r2 = 0.932-0.999) fitted to the chemical reaction-based models namely pseudo-first-order, -second-order, and the general rate law. However, these models fail to accurately describe the kinetics of metal biosorption due either to prefixed order or unjustifiable change in rate constant and reaction order with varying concentrations of metal and biomass in the solution. The diffusion-based models, namely, the intra-particle diffusion model and the external mass transfer model fitted well to the time-course metal sorption data, thus suggesting involvement of both external and intra-particle diffusion processes in sorption of test metals by mat biomass. However, the Boyd kinetic expression clearly showed that the external mass transfer is the dominant process. 相似文献
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Tatsuya Maehigashi Seohyun Ahn Uk-Il Kim Jared Lindenberger Adrian Oo Pratibha C. Koneru Bijan Mahboubi Alan N. Engelman Mamuka Kvaratskhelia Kyungjin Kim Baek Kim 《PLoS pathogens》2021,17(7)
Allosteric integrase inhibitors (ALLINIs) are a class of experimental anti-HIV agents that target the noncatalytic sites of the viral integrase (IN) and interfere with the IN-viral RNA interaction during viral maturation. Here, we report a highly potent and safe pyrrolopyridine-based ALLINI, STP0404, displaying picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. X-ray structural and biochemical analyses revealed that STP0404 binds to the host LEDGF/p75 protein binding pocket of the IN dimer, which induces aberrant IN oligomerization and blocks the IN-RNA interaction. Consequently, STP0404 inhibits proper localization of HIV-1 RNA genomes in viral particles during viral maturation. Y99H and A128T mutations at the LEDGF/p75 binding pocket render resistance to STP0404. Extensive in vivo pharmacological and toxicity investigations demonstrate that STP0404 harbors outstanding therapeutic and safety properties. Overall, STP0404 is a potent and first-in-class ALLINI that targets LEDGF/p75 binding site and has advanced to a human trial. 相似文献
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Singh Ashish Tripathi Pratibha Yadawa Arun Kumar Singh Sarika 《Neurochemical research》2020,45(8):1731-1745
Neurochemical Research - Parkinson’s disease (PD) is a slow progressive, second most common neurodegenerative disease characterized by the loss of dopaminergic neurons from the nigrostriatal... 相似文献
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S. T. Chandel H. S. Gaur M. M. Alam 《Archives Of Phytopathology And Plant Protection》2013,46(3):195-200
The effects of puddling and water regimes on hydraulic conductivity (cm/day) of soil and on bulk density (mg/m 3 ) during rice culture, soil physical characteristics of the experimental field population densities of plant-parasitic nematodes have been studied. Puddling reduced the bulk density of soil and decreased the hydraulic conductivity in the upper layers but not in the deeper layers of soil aeration was reduced due to high moisture levels retained in the puddled soil. Population density of M. triticoryzae declined in puddled soil. The invasion of the roots by the second-generation infective juveniles was reduced. The population density of the root-knot nematodes was higher in the non-puddled soil especially in unsubmerged condition compared to puddled and submerged soil. However, if the seedlings were already infected before transplanting and submergence, the nematode could survive well and reproduce within the aerenchyma of the root. 相似文献
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Vaccinia virus infection induces dendritic cell maturation but inhibits antigen presentation by MHC class II 总被引:2,自引:0,他引:2
Yao Y Li P Singh P Thiele AT Wilkes DS Renukaradhya GJ Brutkiewicz RR Travers JB Luker GD Hong SC Blum JS Chang CH 《Cellular immunology》2007,246(2):92-102
Vaccinia virus (VV) infection is known to inhibit dendritic cells (DC) functions in vitro. Paradoxically, VV is also highly immunogenic and thus has been used as a vaccine. In the present study, we investigated the effects of an in vivo VV infection on DC function by focusing on early innate immunity. Our data indicated that DC are activated upon in vivo VV infection of mice. Splenic DC from VV-infected mice expressed elevated levels of MHC class I and co-stimulatory molecules on their cell surface and exhibited the enhanced potential to produce cytokines upon LPS stimulation. DC from VV-infected mice also expressed a high level of interferon-beta. However, a VV infection resulted in the down-regulation of MHC class II expression and the impairment of antigen presentation to CD4 T cells by DC. Thus, during the early stage of a VV infection, although DC are impaired in some of the critical antigen presentation functions, they can promote innate immune defenses against viral infection. 相似文献
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