scholarly journals Click-Chemistry Based High Throughput Screening Platform for Modulators of Ras Palmitoylation

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
Lakshmi Ganesan ◽  
Peyton Shieh ◽  
Carolyn R. Bertozzi ◽  
Ilya Levental
Keyword(s):  
Click Chemistry ◽  
High Throughput ◽  
High Throughput Screening ◽  
Screening Platform

High-Throughput Screening Platform for Nanoparticle-Mediated Alterations of DNA Repair Capacity

ACS Nano ◽  
2021 ◽  
Author(s):  
Sneh M. Toprani ◽  
Dimitrios Bitounis ◽  
Qiansheng Huang ◽  
Nathalia Oliveira ◽  
Kee Woei Ng ◽  
...  
Keyword(s):  
Dna Repair ◽  
High Throughput ◽  
High Throughput Screening ◽  
Repair Capacity ◽  
Dna Repair Capacity ◽  
Screening Platform

Time-Resolved Luminescent High-Throughput Screening Platform for Lysosomotropic Compounds in Living Cells

ACS Sensors ◽  
2020 ◽  
Author(s):  
Ke-Jia Wu ◽  
Chun Wu ◽  
Feng Chen ◽  
Sha-Sha Cheng ◽  
Dik-Lung Ma ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Living Cells ◽  
Time Resolved ◽  
Screening Platform

Rapid build-up of high-throughput screening microarrays with biochemistry gradients via light-induced thiol–ene “click” chemistry

2021 ◽  
Vol 9 (13) ◽  
pp. 3032-3037
Author(s):  
Hongye Hao ◽  
Junjie Huang ◽  
Ping Liu ◽  
Yunfan Xue ◽  
Jing Wang ◽  
...  
Keyword(s):  
Click Chemistry ◽  
High Throughput ◽  
High Throughput Screening ◽  
Cell Behaviors

Microarrays with biochemistry gradients were rapidly fabricated via light-induced thiol–ene “click” chemistry and showed great applicability in cell behaviors screening.

scholarly journals A High-Throughput Approach To Identify Compounds That Impair Envelope Integrity in Escherichia coli

2016 ◽  
Vol 60 (10) ◽  
pp. 5995-6002 ◽  
Author(s):  
Kristin R. Baker ◽  
Bimal Jana ◽  
Henrik Franzyk ◽  
Luca Guardabassi
Keyword(s):  
Escherichia Coli ◽  
High Throughput ◽  
High Throughput Screening ◽  
Gram Negative Bacteria ◽  
Chromogenic Substrate ◽  
Intrinsic Resistance ◽  
Gram Negative ◽  
Content Type ◽  
E Coli ◽  
Screening Platform

ABSTRACTThe envelope of Gram-negative bacteria constitutes an impenetrable barrier to numerous classes of antimicrobials. This intrinsic resistance, coupled with acquired multidrug resistance, has drastically limited the treatment options against Gram-negative pathogens. The aim of the present study was to develop and validate an assay for identifying compounds that increase envelope permeability, thereby conferring antimicrobial susceptibility by weakening of the cell envelope barrier in Gram-negative bacteria. A high-throughput whole-cell screening platform was developed to measureEscherichia colienvelope permeability to a β-galactosidase chromogenic substrate. The signal produced by cytoplasmic β-galactosidase-dependent cleavage of the chromogenic substrate was used to determine the degree of envelope permeabilization. The assay was optimized by using known envelope-permeabilizing compounds andE. coligene deletion mutants with impaired envelope integrity. As a proof of concept, a compound library comprising 36 peptides and 45 peptidomimetics was screened, leading to identification of two peptides that substantially increased envelope permeability. Compound 79 reduced significantly (from 8- to 125-fold) the MICs of erythromycin, fusidic acid, novobiocin and rifampin and displayed synergy (fractional inhibitory concentration index, <0.2) with these antibiotics by checkerboard assays in two genetically distinctE. colistrains, including the high-risk multidrug-resistant, CTX-M-15-producing sequence type 131 clone. Notably, in the presence of 0.25 μM of this peptide, both strains were susceptible to rifampin according to the resistance breakpoints (R> 0.5 μg/ml) for Gram-positive bacterial pathogens. The high-throughput screening platform developed in this study can be applied to accelerate the discovery of antimicrobial helper drug candidates and targets that enhance the delivery of existing antibiotics by impairing envelope integrity in Gram-negative bacteria.

scholarly journals A click chemistry-based microRNA maturation assay optimized for high-throughput screening

2016 ◽  
Vol 52 (53) ◽  
pp. 8267-8270 ◽  
Author(s):  
Daniel A. Lorenz ◽  
Amanda L. Garner
Keyword(s):  
Click Chemistry ◽  
High Throughput ◽  
High Throughput Screening ◽  
Diels Alder ◽  
Inverse Electron Demand ◽  
Electron Demand

A catalytic enzyme-linked click chemistry assay (cat-ELCCA) for Dicer-catalyzed pre-microRNA maturation was optimized to employ inverse-electron demand Diels–Alder (IEDDA) chemistry affording high-throughput screening capability.

scholarly journals A Novel High-Throughput Screening Platform Identifies Itaconate Derivatives from Marine Penicillium antarcticum as Inhibitors of Mesenchymal Stem Cell Differentiation

Marine Drugs ◽  
2020 ◽  
Vol 18 (4) ◽  
pp. 192
Author(s):  
Pietro Marchese ◽  
Nipun Mahajan ◽  
Enda O’Connell ◽  
Howard Fearnhead ◽  
Maria Tuohy ◽  
...  
Keyword(s):  
Stem Cell ◽  
Cell Differentiation ◽  
Small Molecules ◽  
High Throughput ◽  
High Throughput Screening ◽  
Chondrogenic Differentiation ◽  
Stem Cell Differentiation ◽  
Ectopic Calcification ◽  
Tissue Calcification ◽  
Screening Platform

Worldwide diffused diseases such as osteoarthritis, atherosclerosis or chronic kidney disease are associated with a tissue calcification process which may involve unexpected local stem cell differentiation. Current pharmacological treatments for such musculoskeletal conditions are weakly effective, sometimes extremely expensive and often absent. The potential to develop new therapies is represented by the discovery of small molecules modulating resident progenitor cell differentiation to prevent aberrant tissue calcification. The marine environment is a rich reserve of compounds with pharmaceutical potential and many novel molecules are isolated from macro and microorganisms annually. The potential of small molecules synthetized by marine filamentous fungi to influence the osteogenic and chondrogenic differentiation of human mesenchymal stem/stromal cells (hMSCs) was investigated using a novel, high-throughput automated screening platform. Metabolites synthetized by the marine-derived fungus Penicillium antarcticum were evaluated on the platform. Itaconic acid derivatives were identified as inhibitors of calcium elaboration into the matrix of osteogenically differentiated hMSCs and also inhibited hMSC chondrogenic differentiation, highlighting their capacity to impair ectopic calcification. Bioactive small molecule discovery is critical to address ectopic tissue calcification and the use of biologically relevant assays to identify naturally occurring metabolites from marine sources represents a strategy that can contribute to this effort.

Development of a High-Throughput Screening Platform to Study the Adsorption of Antigens onto Aluminum-Containing Adjuvants

2015 ◽  
Vol 104 (2) ◽  
pp. 557-565 ◽  
Author(s):  
Vanessa Jully ◽  
Nicolas Moniotte ◽  
Frédéric Mathot ◽  
Dominique Lemoine ◽  
Véronique Préat
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Screening Platform
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