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Computing must become much more human centered--for example, by presenting personalized information to users and by respecting personal preferences when controlling multiple devices or invoking various services. Appropriate representation of the information's semantics and of the functionality of devices and services will be critical to such personalized computing. Symbolic artificial intelligence techniques provide the method of choice for the required semantic-representation and reasoning capabilities. 相似文献
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Nitroarenes as Antitubercular Agents: Stereoelectronic Modulation to Mitigate Mutagenicity 下载免费PDF全文
Dr. Sudhir Landge Dr. Vasanthi Ramachandran Dr. Anupriya Kumar Dr. João Neres Kannan Murugan Dr. Claire Sadler Dr. Mick D. Fellows Vaishali Humnabadkar Dr. Prakash Vachaspati Dr. Anandkumar Raichurkar Sreevalli Sharma Sudha Ravishankar Supreeth Guptha Dr. Vasan K. Sambandamurthy Dr. Tanjore S. Balganesh Dr. Bheemarao G. Ugarkar Dr. V. Balasubramanian Dr. Balachandra S. Bandodkar Dr. Manoranjan Panda 《ChemMedChem》2016,11(3):331-339
Nitroarenes are less preferred in drug discovery due to their potential to be mutagenic. However, several nitroarenes were shown to be promising antitubercular agents with specific modes of action, namely, nitroimidazoles and benzothiazinones. The nitro group in these compounds is activated through different mechanisms, both enzymatic and non‐enzymatic, in mycobacteria prior to binding to the target of interest. From a whole‐cell screening program, we identified a novel lead nitrobenzothiazole (BT) series that acts by inhibition of decaprenylphosphoryl‐β‐d ‐ribose 2′‐epimerase (DprE1) of Mycobacterium tuberculosis (Mtb). The lead was found to be mutagenic to start with. Our efforts to mitigate mutagenicity resulted in the identification of 6‐methyl‐7‐nitro‐5‐(trifluoromethyl)‐1,3‐benzothiazoles (cBTs), a novel class of antitubercular agents that are non‐mutagenic and exhibit an improved safety profile. The methyl group ortho to the nitro group decreases the electron affinity of the series, and is hence responsible for the non‐mutagenic nature of these compounds. Additionally, the co‐crystal structure of cBT in complex with Mtb DprE1 established the mode of binding. This investigation led to a new non‐mutagenic antitubercular agent and demonstrates that the mutagenic nature of nitroarenes can be solved by modulation of stereoelectronic properties. 相似文献
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The area of metaheuristics has grown immensely in the past two decades as a solution to real-world optimisation problems. They are able to perform well in situations where exact optimisation techniques fail to deliver satisfactory results. For complex optimisation problems (Nondeterministic polynomial time-hard problems), metaheuristic techniques are able to generate good quality solution in relatively much less time than traditional optimisation techniques. Metaheuristics find applications in a wide range of areas including finance, planning, scheduling and engineering design. This paper presents a review of various metaheuristic algorithms, their methodology, recent trends and applications. 相似文献
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ScGpi12 is a 304 amino residue long endoplasmic reticulum membrane protein, which participates in the de-N-acetylation of N-acetylglucosaminyl phosphatidylinositol to produce glucosaminyl phosphatidylinositol in the second step of GPI anchor biosynthesis pathway in Saccharomyces cerevisiae. ScGpi12 was cloned in a pMAL-c2x vector and expressed heterologously in Rosetta-gami (DE3) strain of E. coli. Affinity purification of the protein yielded low amounts of the MBP-tagged enzyme, which was active. To the best of our knowledge, this is the first successful purification of full-length Gpi12 enzyme, without the accompanying GroEL that was seen in other studies. The presence of the tag did not greatly alter the activity of the enzyme. ScGpi12 was optimally active in the pH range of 6.5–8.5 and at 30 °C. It was not sensitive to treatment with EDTA but was stimulated by multiple divalent cations. The divalent cation did not alter the pH profile of the enzyme, suggesting no role of the divalent metal in creating a nucleophile for catalysis. Divalent cations did, however, enhance the turnover number of the enzyme for its substrate, suggesting that they are probably required for the production of a catalytically competent active site by bringing the active site residues within optimum distance of the substrate for catalysis. 相似文献
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Anupriya Ankolekar Markus Krtzsch Thanh Tran Denny Vrande
i 《Journal of Web Semantics》2008,6(1):70-75
A common perception is that there are two competing visions for the future evolution of the Web: the Semantic Web and Web 2.0. A closer look, though, reveals that the core technologies and concerns of these two approaches are complementary and that each field can and must draw from the other’s strengths. We believe that future Web applications will retain the Web 2.0 focus on community and usability, while drawing on Semantic Web infrastructure to facilitate mashup-like information sharing. However, there are several open issues that must be addressed before such applications can become commonplace. In this paper, we outline a semantic weblogs scenario that illustrates the potential for combining Web 2.0 and Semantic Web technologies, while highlighting the unresolved issues that impede its realization. Nevertheless, we believe that the scenario can be realized in the short-term. We point to recent progress made in resolving each of the issues as well as future research directions for each of the communities. 相似文献
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Gauri Shankar Shaw Dibyajyoti Biswal Anupriya B Indranil Banerjee Krishna Pramanik Arfat Anis 《Polymer-Plastics Technology and Engineering》2017,56(2):141-152
The current study delineates the development of novel gelatin–tamarind gum/carboxymethyl tamarind gum-based phase-separated films for probable skin tissue engineering applications. Polyethylene glycol was used as plasticizer. The films were characterized thoroughly using mechanical tester and impedance analyzer. Cell proliferation ability and drug release properties of the films were investigated. Mechanical studies indicated composition-dependent stress relaxation properties. Polysaccharide containing films supported better proliferation of human keratinocytes as compared to control. Drug-loaded films showed good antimicrobial properties against Escherichia coli. Analysis of the results indicated that the prepared films may be tried as matrices for skin tissue engineering. 相似文献
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Anupriya Anand Abimanyu Sugumaran Damodharan Narayanasamy 《IET nanobiotechnology / IET》2019,13(4):353
A brain tumour is amongst most devastating and challenging condition to overcome with suitable treatment as the drug has to cross the blood–brain barrier (BBB) with several physiological barriers like opsonisation by the reticuloendothelial system. Presently various techniques such as surgical, chemotherapeutic agents, and radiotherapy techniques have performed to extend the lifespan of patients diagnosed with glioblastoma, which did not maximise the overall survival of patients with a tumour. Nanotechnology is relied upon to diminish the requirement for intrusive methods for conveyance of therapeutics to the central nervous system. Colloidal nanocarriers sizing range 1–1000 nm have been utilised to cross BBB delivers the drug at cell levels with enhanced bioavailability and reduced toxicity. However, solid lipid nanoparticles (SLNs) are considered a highly flexible carrier for more successful remedially in brain tumour. The treatment of a brain tumour via SLNs is gaining greater potency due to its inimitable size and lipidic nature. This review focuses and represents the current strategies of SLNs in the brain tumour treatment with appropriate techniques adopted are highlighted. Based on this review, the authors concluded that SLNs embrace exclusive promising lipidic nanocarrier that could be utilised to target a brain tumour effectively.Inspec keywords: brain, cancer, nanoparticles, blood, molecular biophysics, tumours, nanomedicine, neurophysiology, radiation therapy, colloids, biomedical materials, drug delivery systems, nanofabrication, drugs, cellular biophysicsOther keywords: chemotherapeutic agents, radiotherapy techniques, central nervous system, colloidal nanocarriers sizing range 1–1000 nm, BBB, drug, solid lipid nanoparticles, brain tumour therapeutical uses, lipidic nature, brain tumour treatment, brain targeted delivery, anticancer drugs, prospective approach, blood–brain barrier, physiological barriers, reticuloendothelial system, surgical agents, lipidic nanocarrier, size 1.0 nm to 1000.0 nm 相似文献