High-throughput inhibitor screening
IDENTIFICATION OF HUMAN cAMP DEPENDENT PROTEIN KINASE CATALYTIC SUBUNIT INHIBITORS
... potential inhibitor of cAMP dependent protein kinase catalytic subunit, a high throughput virtual screening of zinc natural compounds database was ...
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Molecular docking and High throughput screening of potent inhibitor to gp46SU involved in ATLL through drug design studies
... domain inhibitor) satisfied almost all properties like drug toxicity value, drug score, lower logP values and Lipinski’s rule of ...potential inhibitor of gp46SU, and can be considered as a good drug ...
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Thiazolidinone CFTR inhibitor identified by high throughput screening blocks cholera toxin–induced intestinal fluid secretion
... The high-throughput screening assay was designed to identify CFTR inhibitors that interact directly with ...best inhibitor identified by screening of structural analogs was subject to ...
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Discovery of Cercosporamide, a Known Antifungal Natural Product, as a Selective Pkc1 Kinase Inhibitor through High-Throughput Screening
... Our goal in this effort was to discover novel Pkc1 inhibitors through an enzyme-based HTS to be developed into antifungal drugs. Thus, as antifungals, Pkc1 inhibitors must be active against the endogenous Pkc1 kinase ...
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A systematic approach to identify novel cancer drug targets using machine learning, inhibitor design and high-throughput screening
... low-throughput screening and/or low coverage of the human genome, limits their usefulness for genome-wide identification of drug ...performed high-throughput chemical compound screening ...
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High throughput chemical library screening identifies a novel p110-δ inhibitor that potentiates the anti-myeloma effect of bortezomib
... Despite the introduction of PIs and immunomodulatory agents into the clinic, MM remains incurable. While most patients initially respond to PIs, drug resistance emerges and represents the primary factor for treatment ...
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High-throughput virtual screening with e-pharmacophore and molecular simulations study in the designing of pancreatic lipase inhibitors
... e-pharmacophore screening was implemented on the natural ligand-molecule Zinc ...of screening displayed four varied ...potent inhibitor against the target receptor pancreatic lipase ...
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Development of automatic image analysis methods for high-throughput and high-content screening
... In order to validate the sensitivity of our algorithm for perturbation of the biological system, a pilot experiment was performed by pre-exposing the HepG2/GFP-p65 cells for 2 hours with increasing concentrations of an ...
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Energy-Optimized Pharmacophore Coupled Virtual Screening in the Discovery of Quorum Sensing Inhibitors of LasR Protein of Pseudomonas aeruginosa
... sensing inhibitor; VS, virtual screening; HTVS, high-throughput virtual screening; EF, enrichment factor; ROC, receiver operating characteristic; BEDROC, Boltzmann-enhanced ...
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Identification of Mannich Base as a Novel Inhibitor of Mycobacterium Tuberculosis Isocitrate by High-Throughput Screening
... a high-throughput screen (HTS) developed to screen active molecule from a mannich base compounds library for inhibition of ...HTS. Screening of a collection of 124 mannich base compounds resulted in ...
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Clinical application of high throughput molecular screening techniques for pharmacogenomics
... of high throughput diagnostic methods as part of clinically validated ...for high throughput mutation detection, including techniques able to monitor thousands of genetic variants for a single ...
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A high-throughput cellulase screening system based on droplet microfluidics
... obtained high enrichment factors of up to 300 when starting from low concentrations of positive cells, and we were able to sort to a purity of greater than ...a high-throughput screening ...
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An efficient high throughput metabotyping platform for screening of biomass willows
... Abstract: Future improvement of woody biomass crops such as willow and poplar relies on our ability to select for metabolic traits that sequester more atmospheric carbon into biomass, or into useful products to replace ...
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High-throughput screening of Mucoromycota fungi for production of low- and high-value lipids
... For each strain, three biological replicates were prepared. Biological replicates were represented by the spore sus- pensions prepared from separate agar plates. Exceptions were M. circinelloides strains with five ...
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High-throughput high-volume nuclear imaging for preclinical in vivo compound screening§
... In this study, workflows, methods and software have been developed to allow efficient high-volume compound screening of 25 proteins by SPECT/CT of a tumour xeno- graft mouse model. The main interest of this ...
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High-throughput system for screening of Monascus purpureus high-yield strain in pigment production
... the high correlation coefficient ...This high-throughput assay could be effectively used for the determination of Monascus pigment instead of traditional ...for high-aerobic microbe ...
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High throughput miniaturized screening of nanoparticle formation via inkjet printing
... Nevertheless, conventional methods need materials in the milligram scale, require days for the full removal of the solvent, face issues with scalability and batch-to-batch variability and frequently result in NPs with ...
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The QSARome of the receptorome : quantitative structure-activity relationship modeling of multiple ligand sets acting at multiple receptors
... Chapter 4 and 5 focus on the development of QSARome models for predicting chemical binding profiles instead of binding affinity to a specific target. Conventional QSAR studies, including previous works from our ...
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Familial Hypercholesterolemia: From Diagnosis to Treatment
... indicate high efficacy and safety for this option but According to the infrequency of liver donor and complexities of the transplant and post-transplant management this is not a popular choice for treatment ...
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Maximizing gain in high-throughput screening using conformal prediction
... from screening the training set and the predicted test subset gain, compared to the corresponding models based on physicochemical descriptors for the investi- gated datasets (Table ...
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