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排序方式: 共有1642条查询结果,搜索用时 31 毫秒
1.
Dr. Anders Højgaard Hansen Henriette B. Christensen Dr. Sunil K. Pandey Dr. Eugenia Sergeev Alice Valentini Julia Dunlop Domonkos Dedeo Simone Fratta Dr. Brian D. Hudson Prof. Graeme Milligan Prof. Trond Ulven Prof. Elisabeth Rexen Ulven 《ChemMedChem》2021,16(21):3326-3341
Free fatty acid receptor 2 (FFA2) is a sensor for short-chain fatty acids that has been identified as an interesting potential drug target for treatment of metabolic and inflammatory diseases. Although several ligand series are known for the receptor, there is still a need for improved compounds. One of the most potent and frequently used antagonists is the amide-substituted phenylbutanoic acid known as CATPB ( 1 ). We here report the structure-activity relationship exploration of this compound, leading to the identification of homologues with increased potency. The preferred compound 37 (TUG-1958) was found, besides improved potency, to have high solubility and favorable pharmacokinetic properties. 相似文献
2.
Design Automation for Embedded Systems - Moving object tracking is a computation-intensive operation that requires accelerating hardware solution. In this work, a high-performance design for mean... 相似文献
3.
Dr. Santosh Shivakumaraswamy Nivedita Pandey Dr. Lionel Ballut Dr. Sébastien Violot Prof. Dr. Nushin Aghajari Prof. Dr. Hemalatha Balaram 《Chembiochem : a European journal of chemical biology》2020,21(19):2805-2817
GMP synthetase catalyses the conversion of XMP to GMP through a series of reactions that include hydrolysis of Gln to generate ammonia in the glutamine amidotransferase (GATase) domain, activation of XMP to adenyl-XMP intermediate in the ATP pyrophosphatase (ATPPase) domain and reaction of ammonia with the intermediate to generate GMP. The functioning of GMP synthetases entails bidirectional domain crosstalk, which leads to allosteric activation of the GATase domain, synchronization of catalytic events and tunnelling of ammonia. Herein, we have taken recourse to the analysis of structures of GMP synthetases, site-directed mutagenesis and steady-state and transient kinetics on the Plasmodium falciparum enzyme to decipher the molecular basis of catalysis in the ATPPase domain and domain crosstalk. Our results suggest an arrangement at the interdomain interface, of helices with residues that play roles in ATPPase catalysis as well as domain crosstalk enabling the coupling of ATPPase catalysis with GATase activation. Overall, the study enhances our understanding of GMP synthetases, which are drug targets in many infectious pathogens. 相似文献
4.
Manoj Karakoti Ritu Jangra Sandeep Pandey Pawan Singh Dhapola Sunil Dhali Suman Mahendia Pramod K Singh Nanda Gopal Sahoo 《International Journal of Applied Ceramic Technology》2020,17(4):1899-1908
This study deals with the utility of mini spray dryer process to improve the dispersibility, of graphene oxide(GO) and its application for high-performance supercapacitor. Initially, the neutral solution of GO was obtained using the modified Hummer's method. After this, the prepared GO solution was processed by mini spray dryer to obtain a more purified, lighter, and dispersed form of GO which is named as spray dryer processed GO (SPGO). The SPGO thus obtained showed excellent dispersibility behavior with various solvents, which is not found in case of conventional oven drying. Furthermore, utility of SPGO and its reduced form (r-SPGO) for supercapacitor applications have been investigated. Results obtained from the cyclic voltammetry(CV) analysis, impedance, and charge-discharge behavior of supercapacitor fabricated using r-SPGO shows enhanced features. Therefore, the simple spray dried GO and its reduced form, that is, r-SPGO can be utilized as a potential candidate for the supercapacitor application. Herein, as synthesized SPGO exhibited the specific capacitance of 12.07 and 37.6 F/g with PVA-H3PO4 and 1 mol/L H3PO4, respectively, at a scan rate of 5 mV/s. On the other hand, reduced form of SPGO, that is, r-SPGO showed the specific capacitance of 27.16 and 230 F/g with PVA-H3PO4 and 1 mol/L H3PO4, respectively. 相似文献
5.
Shunqing Zhang Dr. Ravindra R. Cheruku Dr. Mykhaylo Dukh Walter Tabaczynski Dr. Nayan J. Patel Dr. William H. White III Joseph R. Missert Dr. Joseph A. Spernyak Dr. Ravindra K. Pandey 《ChemMedChem》2020,15(21):2058-2070
3-(1’-Hexyloxyethyl)-3-devinyl-pyropheophorbide-a (HPPH or Photochlor), a tumor-avid chlorophyll-a derivative currently undergoing human clinical trials, was conjugated at various peripheral positions (position-17 or 20) of HPPH with either Gd(III)-aminobenzyl-DTPA (Gd(III) DTPA) or Gd(III)-aminoethylamido-DOTA (Gd(III) DOTA). The corresponding conjugates were evaluated for in vitro PDT efficacy, T1, T2 relaxivities, in vivo fluorescence, and MR imaging under similar treatment parameters. Among these analogs, the water-soluble Gd(III)-aminoethylamido-DOTA linked at position-17 of HPPH, i. e., HPPH-17-Gd(III) DOTA, demonstrated strong potential for tumor imaging by both MR and fluorescence, while maintaining the PDT efficacy in BALB/c mice bearing Colon-26 tumors (7/10 mice were tumor free on day 60). In contrast to Gd(III) DTPA (Magnevist) and Gd(III) DOTA (Dotarem), the HPPH-Gd(III) DOTA retains in the tumor for a long period of time (24 to 48 h) and provides an option of fluorescence-guided cancer therapy. Thus, a single agent can be used for cancer-imaging and therapy. However, further detailed pharmacokinetic, pharmacodynamic, and toxicological studies of the conjugate are required before initiating Phase I human clinical trials. 相似文献
6.
Sanjeev Kumar Pandey S. L. Patil Praveen V. Pol S. B. Phadke 《International Journal of Electronics》2020,107(10):1682-1703
ABSTRACT In this paper, two control schemes for boost converters affected by uncertainties in input voltage and load are proposed. The boost converter dynamics is redefined in terms of new state variables to facilitate the use of a disturbance observer that can estimate matched and unmatched disturbances. A sliding surface, which is new in the context of boost converters, is proposed to enable tracking and regulation of output voltage without requiring measurement of input voltage and load current. The stability of the overall system including the disturbance observer, the sliding variable and the output is proved. The performance of the schemes is assessed for regulation of output voltage and tracking of reference voltage by simulation as well as experimentation in which various types of uncertainties and various types of reference voltages are considered. 相似文献
7.
Pandey Mahendra Kumar Parmar Girish Gupta Rajeev Sikander Afzal 《Microsystem Technologies》2019,25(8):3071-3081
Microsystem Technologies - Due to fast technological development, human beings generally depend upon computer and other digital equipments in different areas of concern/applications. Therefore,... 相似文献
8.
Pandey Mamta Litoriya Ratnesh Pandey Prateek 《Wireless Personal Communications》2019,107(4):1687-1708
Wireless Personal Communications - Increased dominance of mobile applications (henceforth, app) over conventional software applications is quite apparent; however, there is a lack of structured... 相似文献
9.
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
10.
Dhiman Gaurav Soni Mukesh Pandey Hari Mohan Slowik Adam Kaur Harsimran 《Engineering with Computers》2021,37(4):3017-3035
Engineering with Computers - A novel hybrid many-objective evolutionary algorithm called Reference Vector Guided Evolutionary Algorithm based on hypervolume indicator (H-RVEA) is proposed in this... 相似文献