scholarly journals Deguelins, Natural Product Modulators of NF1-Defective Astrocytoma Cell Growth Identified by High-Throughput Screening of Partially Purified Natural Product Extracts

2015 ◽  
Vol 78 (11) ◽  
pp. 2776-2781 ◽  
Author(s):  
Curtis J. Henrich ◽  
Laura K. Cartner ◽  
Jennifer A. Wilson ◽  
Richard W. Fuller ◽  
Anthony E. Rizzo ◽  
...  
Keyword(s):  
Cell Growth ◽  
Natural Product ◽  
High Throughput ◽  
High Throughput Screening ◽  
Astrocytoma Cell

The Search for Novel Human Pancreatic α-Amylase Inhibitors: High-Throughput Screening of Terrestrial and Marine Natural Product Extracts

ChemBioChem ◽  
2008 ◽  
Vol 9 (3) ◽  
pp. 433-438 ◽  
Author(s):  
Chris A. Tarling ◽  
Kate Woods ◽  
Ran Zhang ◽  
Harry C. Brastianos ◽  
Gary D. Brayer ◽  
...  
Keyword(s):  
Natural Product ◽  
High Throughput ◽  
High Throughput Screening ◽  
Marine Natural Product ◽  
Amylase Inhibitors

scholarly journals Development of a Robust Cytopathic Effect-Based High-Throughput Screening Assay To Identify Novel Inhibitors of Dengue Virus

2012 ◽  
Vol 56 (6) ◽  
pp. 3399-3401 ◽  
Author(s):  
Kevin D. McCormick ◽  
Shufeng Liu ◽  
Jana L. Jacobs ◽  
Ernesto T. A. Marques ◽  
Nicolas Sluis-Cremer ◽  
...  
Keyword(s):  
Dengue Virus ◽  
Natural Product ◽  
High Throughput ◽  
High Throughput Screening ◽  
Cytopathic Effect ◽  
Complex Molecule ◽  
Denv Infection ◽  
Screening Assay ◽  
High Throughput Screening Assay ◽  
Natural Product Library

ABSTRACTWe have developed a robust cytopathic effect-based high-throughput screening assay to identify inhibitors of dengue virus (DENV) infection. Screening of a small natural product library yielded 11 hits. Four of these were found to be potent inhibitors of DENV, although serotype differences were noted. Taken together, these data suggest that screening of larger and more complex molecule libraries may result in the identification of more potent and specific DENV inhibitors.

Logistic Considerations to Deliver Natural Product Libraries for High-­Throughput Screening

2015 ◽  
pp. 91-104
Author(s):  
Ngoc Pham ◽  
Stephen Toms ◽  
David Camp ◽  
Ronald Quinn
Keyword(s):  
Natural Product ◽  
High Throughput ◽  
High Throughput Screening

scholarly journals A High Throughput Screen for Inhibitors of Fungal Cell Wall Synthesis

2002 ◽  
Vol 7 (4) ◽  
pp. 359-366 ◽  
Author(s):  
Jonathan M. Evans ◽  
Phillip G. Zaworski ◽  
Christian N. Parker
Keyword(s):  
Cell Wall ◽  
Cell Growth ◽  
High Throughput ◽  
High Throughput Screening ◽  
Osmotic Shock ◽  
Fungal Cell Wall ◽  
Cell Wall Synthesis ◽  
Fungal Cell ◽  
Unique Nature ◽  
Pharmacologically Active

Fungal cell wall synthesis is essential for viability, requiring the activity of genes involved in environmental sensing, precursor synthesis, transport, secretion, and assembly. This multitude of potential targets, the availability of known agents targeting this pathway, and the unique nature of fungal cell wall synthesis make this pathway an appealing target for drug discovery. Here we describe the adaptation of an assay monitoring cell wall synthesis for high-throughput screening. The assay requires fungal cell growth, in the presence of the test compound, for 3 h before the cells are subjected to osmotic shock in the presence of a dye that stains DNA. Miniaturization of the assay to a 384-well plate format and removing a mechanical transfer led to subtle changes in the assay characteristics. Validation of the assay with a library of known pharmacologically active agents has identified a number of different classes of compounds that are active in this assay, causing aberrant cell wall morphology and in many cases the inhibition of fungal cell growth.

scholarly journals High-Throughput Screening Platform for Natural Product–Based Drug Discovery Against 3 Neglected Tropical Diseases

2014 ◽  
Vol 20 (1) ◽  
pp. 82-91 ◽  
Author(s):  
F. Annang ◽  
G. Pérez-Moreno ◽  
R. García-Hernández ◽  
C. Cordon-Obras ◽  
J. Martín ◽  
...  
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Natural Product ◽  
High Throughput ◽  
High Throughput Screening ◽  
Neglected Tropical Diseases ◽  
Chemical Diversity ◽  
Tropical Diseases ◽  
Isolation And Characterization ◽  
Microbial Extracts

African trypanosomiasis, leishmaniasis, and Chagas disease are 3 neglected tropical diseases for which current therapeutic interventions are inadequate or toxic. There is an urgent need to find new lead compounds against these diseases. Most drug discovery strategies rely on high-throughput screening (HTS) of synthetic chemical libraries using phenotypic and target-based approaches. Combinatorial chemistry libraries contain hundreds of thousands of compounds; however, they lack the structural diversity required to find entirely novel chemotypes. Natural products, in contrast, are a highly underexplored pool of unique chemical diversity that can serve as excellent templates for the synthesis of novel, biologically active molecules. We report here a validated HTS platform for the screening of microbial extracts against the 3 diseases. We have used this platform in a pilot project to screen a subset (5976) of microbial extracts from the MEDINA Natural Products library. Tandem liquid chromatography–mass spectrometry showed that 48 extracts contain potentially new compounds that are currently undergoing de-replication for future isolation and characterization. Known active components included actinomycin D, bafilomycin B1, chromomycin A3, echinomycin, hygrolidin, and nonactins, among others. The report here is, to our knowledge, the first HTS of microbial natural product extracts against the above-mentioned kinetoplastid parasites.

scholarly journals NCI Program for Natural Product Discovery: A Publicly-Accessible Library of Natural Product Fractions for High-Throughput Screening

2018 ◽  
Vol 13 (9) ◽  
pp. 2484-2497 ◽  
Author(s):  
Christopher C. Thornburg ◽  
John R. Britt ◽  
Jason R. Evans ◽  
Rhone K. Akee ◽  
James A. Whitt ◽  
...  
Keyword(s):  
Natural Product ◽  
High Throughput ◽  
High Throughput Screening ◽  
Natural Product Discovery

Abstract A174: High‐throughput screening for natural product inhibitors of human tyrosyl‐DNA‐phosphodiesterase (Tdp‐1)

2009 ◽  
Author(s):  
Alun Bermingham ◽  
Edmund Price ◽  
Christophe Marchand ◽  
Yves Pommier ◽  
Katya Goncharova ◽  
...  
Keyword(s):  
Natural Product ◽  
High Throughput ◽  
High Throughput Screening

scholarly journals Development and Implementation of an HTS-Compatible Assay for the Discovery of Selective Small-Molecule Ligands for Pre-microRNAs

2017 ◽  
Vol 23 (1) ◽  
pp. 47-54 ◽  
Author(s):  
Daniel A. Lorenz ◽  
Steve Vander Roest ◽  
Martha J. Larsen ◽  
Amanda L. Garner
Keyword(s):  
Small Molecules ◽  
Natural Product ◽  
Small Molecule ◽  
High Throughput ◽  
High Throughput Screening ◽  
Two Dimensional ◽  
Small Molecule Ligands ◽  
Gene Regulatory ◽  
Regulatory Rnas ◽  
Target Rna

microRNAs (miRNAs) are small gene regulatory RNAs, and their expression has been found to be dysregulated in a number of human diseases. To facilitate the discovery of small molecules capable of selectively modulating the activity of a specific miRNA, we have utilized new high-throughput screening technology targeting Dicer-mediated pre-miRNA maturation. Pilot screening of ~50,000 small molecules and ~33,000 natural product extract libraries against pre-miR-21 processing indicated the potential of our assay for this goal, yielding a campaign Z′ factor of 0.52 and an average plate signal-to-background (S/B) ratio of 13. Using two-dimensional screening against a second pre-miRNA, pre-let-7d, we evaluated the selectivity of confirmed hits. The results presented demonstrate how high-throughput screening can be used to identify selective small molecules for a target RNA.

scholarly journals Discovery of selective cystathionine β-synthase inhibitors by high-throughput screening with a fluorescent thiol probe

MedChemComm ◽  
2017 ◽  
Vol 8 (1) ◽  
pp. 198-201 ◽  
Author(s):  
Weining Niu ◽  
Ping Wu ◽  
Fei Chen ◽  
Jun Wang ◽  
Xiaoya Shang ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Natural Product ◽  
High Throughput ◽  
High Throughput Screening ◽  
Natural Product Library

Screening of a natural product library identified several selective cystathionine β-synthase inhibitors, which suppressed the proliferation of HT29 cancer cells.

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