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151.
152.
A piece of lymph node containing polyclonally-activated lymphocytes when transplanted in the anterior eye chamber of mouse along with solid piece of fibrosarcoma from syngeneic Swiss mice, dramatically inhibited the tumour-induced-vasodilatation and neo-vascularization. If the tumour explants were incubated in vitro with activated lymphocytes prior to transplantation, such angiogenic reactions was significantly reduced. These explants were incapable of incorporating radioactive thymidine in vitro. Furthermore, the cytotoxic ability of activated lymphocytes towards 51Cr labelled tumour target cells was of significant level indicating the possible mechanism of immunological reactiveness of Con A-stimulated lymphocytes to 3'-methylcholanthrene-induced tumour cells of syngeneic origin. 相似文献
153.
Mayankbhai Patel Santhosh Palani Arijit Chakravarty Johnny Yang Wen Chyi Shyu Jerome T. Mettetal 《PloS one》2014,9(10)
Toxicity often limits the utility of oncology drugs, and optimization of dose schedule represents one option for mitigation of this toxicity. Here we explore the schedule-dependency of neutropenia, a common dose-limiting toxicity. To this end, we analyze previously published mathematical models of neutropenia to identify a pharmacokinetic (PK) predictor of the neutrophil nadir, and confirm this PK predictor in an in vivo experimental system. Specifically, we find total AUC and Cmax are poor predictors of the neutrophil nadir, while a PK measure based on the moving average of the drug concentration correlates highly with neutropenia. Further, we confirm this PK parameter for its ability to predict neutropenia in vivo following treatment with different doses and schedules. This work represents an attempt at mechanistically deriving a fundamental understanding of the underlying pharmacokinetic drivers of neutropenia, and provides insights that can be leveraged in a translational setting during schedule selection. 相似文献
154.
Anuradha Jha Anil Kumar R. K. Saxena M. Kamalvanshi Neha Chakravarty 《Indian journal of microbiology》2012,52(2):281-285
A study was conducted to identify suitable arbuscular mycorrhizal (AM) fungi for inoculation of Bambusa bambos and Dendrocalamus strictus at nursery stage for increasing growth and productivity. Twelve AM species, isolated from bamboo and other common trees of Bundelkhand were used for inoculations. In B. bambos, total dry weight and phosphorus (P) uptake were significantly increased by all studied fungi and shoot length was increased by eight AM inoculants. Maximum mycorrhizal dependency (MD) was recorded for Acaulospora scrobiculata (44.2%), followed by Glomus cerebriforme (41.6%) and G. intraradix (41.0%). In D. strictus, all tested AM inoculants significantly increased shoot length, dry shoot weight and P uptake, except Glomus 1. Dry root weight was significantly increased by only two inoculants namely, G. cerebriforme and G. etunicatum. Total dry weight was significantly increased by eight AM fungi. Maximum MD was recorded for G. cerebriforme (62.9%), followed by G. diaphanum (55.0%) and G. etunicatum (51.3%). Thus, the results showed that utilization of effective AM fungi can enhance the productivity of bamboo in the region. 相似文献
155.
Added-value is the additional information that a model carries with respect to the template structure used for model building. Thousands of single-template models, corresponding to proteins of known structure, were analyzed. The accuracy of structure-derived properties, such as residue accessibility, surface area, electrostatic potential, and others, was determined as a function of template:target sequence identity by comparing the models with their corresponding experimental structures. Added-value was determined by comparing the accuracy in models with that from templates. Geometry-dependent properties such as neighborhood of buried residues and accessible surface area showed low added-value. Properties that also depend on the protein sequence, such as presence of polar areas and electrostatic potential, showed high added-value. In general added-value increases when template:target sequence identity decreases, but it is also affected by alignment errors. This study justifies the use of models instead of the use of templates to estimate structure-derived properties of a target protein. 相似文献
156.
Bhuniya D Umrani D Dave B Salunke D Kukreja G Gundu J Naykodi M Shaikh NS Shitole P Kurhade S De S Majumdar S Reddy SB Tambe S Shejul Y Chugh A Palle VP Mookhtiar KA Cully D Vacca J Chakravarty PK Nargund RP Wright SD Graziano MP Singh SB Roy S Cai TQ 《Bioorganic & medicinal chemistry letters》2011,21(12):3596-3602
GPR91, a 7TM G-Protein-Coupled Receptor, has been recently deorphanized with succinic acid as its endogenous ligand. Current literature indicates that GPR91 plays role in various pathophysiology including renal hypertension, autoimmune disease and retinal angiogenesis. Starting from a small molecule high-throughput screening hit 1 (hGPR91 IC50: 0.8 μM)—originally synthesized in Merck for Bradykinin B1 Receptor (BK1R) program, systematic structure-activity relationship study led us to discover potent and selective hGPR91 antagonists e.g. 2c, 4c, and 5g (IC50: 7-35 nM; >1000 fold selective against hGPR99, a closest related GPCR; >100 fold selective in Drug Matrix screening). This initial work also led to identification of two structurally distinct and orally bio-available lead compounds: 5g (%F: 26) and 7e (IC50: 180 nM; >100 fold selective against hGPR99; %F: 87). A rat pharmacodynamic assay was developed to characterize the antagonists in vivo using succinate induced increase in blood pressure. Using two representative antagonists, 2c and 4c, the GPR91 target engagement was subsequently demonstrated using the designed pharmacodynamic assay. 相似文献
157.
Praveen Kumar V Gajendra Reddy R Vo DD Chakravarty S Chandrasekhar S Grée R 《Bioorganic & medicinal chemistry letters》2012,22(3):1439-1444
A versatile synthetic route is reported towards the preparation of new analogues for potent neurotrophic agent biaryl-type lignan honokiol. A focused 24-membered library of derivatives containing five different groups at 5'-position of honokiol has been prepared in fair to good overall yields. Compared to the natural product, or to analogues with a short alkyl chain in this position, these new derivatives have lost most of the neurotrophic activity. 相似文献
158.
Electron microscopic study of the regeneration in vitro of rat peritoneal mast cells after histamine secretion 总被引:2,自引:0,他引:2
Ellen Holm Nielsen Peter Bytzer Jørgen Clausen Nirmal Chakravarty 《Cell and tissue research》1981,216(3):635-645
Summary Regeneration of rat mast cells was studied by TEM from 10 s to 48 h after secretion of histamine induced by compound 48/80. During the first 2 h, small intracellular cavities, formed during compound exocytosis and containing non-membrane-bound remnants of the granules, tended to coalesce, and after 2 h of incubation regeneration started. After 6 h, all the cavities had fused into one large central cavity which contained the remnants of the granules and remained open to the exterior during the entire period. The plasma membrane microfolds which disappeared just after secretion were reformed during regeneration. They were apparently involved in endocytotic-like activity and coated vesicles also appeared beneath the plasmalemma (membrane recycling?). The fate of the granule remnants in the cavity is unknown, as regeneration was not completed after 48 h which is the longest survival time obtained so far in ultrastructural studies of mast cell regeneration in vitro. 相似文献
159.
160.
Anna Hadarovich Devlina Chakravarty Alexander V. Tuzikov Nir BenTal Petras J. Kundrotas Ilya A. Vakser 《Protein science : a publication of the Protein Society》2021,30(2):381
Structures of proteins and protein–protein complexes are determined by the same physical principles and thus share a number of similarities. At the same time, there could be differences because in order to function, proteins interact with other molecules, undergo conformations changes, and so forth, which might impose different restraints on the tertiary versus quaternary structures. This study focuses on structural properties of protein–protein interfaces in comparison with the protein core, based on the wealth of currently available structural data and new structure‐based approaches. The results showed that physicochemical characteristics, such as amino acid composition, residue–residue contact preferences, and hydrophilicity/hydrophobicity distributions, are similar in protein core and protein–protein interfaces. On the other hand, characteristics that reflect the evolutionary pressure, such as structural composition and packing, are largely different. The results provide important insight into fundamental properties of protein structure and function. At the same time, the results contribute to better understanding of the ways to dock proteins. Recent progress in predicting structures of individual proteins follows the advancement of deep learning techniques and new approaches to residue coevolution data. Protein core could potentially provide large amounts of data for application of the deep learning to docking. However, our results showed that the core motifs are significantly different from those at protein–protein interfaces, and thus may not be directly useful for docking. At the same time, such difference may help to overcome a major obstacle in application of the coevolutionary data to docking—discrimination of the intramolecular information not directly relevant to docking. 相似文献