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.

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.

scholarly journals Novel In Vitro Protein Fragment Complementation Assay Applicable to High-Throughput Screening in a 1536-Well Format

2009 ◽  
Vol 14 (8) ◽  
pp. 970-979 ◽  
Author(s):  
Junko Hashimoto ◽  
Taku Watanabe ◽  
Tatsuya Seki ◽  
Satoshi Karasawa ◽  
Miho Izumikawa ◽  
...  
Keyword(s):  
Natural Product ◽  
High Throughput ◽  
High Throughput Screening ◽  
Protein Fragment ◽  
Complementation Assay ◽  
Protein Fragment Complementation ◽  
Natural Product Library ◽  
Protein Fragment Complementation Assay ◽  
Vitro Protein

Protein-protein interactions (PPIs) play key roles in all cellular processes and hence are useful as potential targets for new drug development. To facilitate the screening of PPI inhibitors as anticancer drugs, the authors have developed a high-throughput screening (HTS) system using an in vitro protein fragment complementation assay (PCA) with monomeric Kusabira-Green fluorescent protein (mKG). The in vitro PCA system was established by the topological formation of a functional complex between 2 split inactive mKG fragments fused to target proteins, which fluoresces when 2 target proteins interact to allow complementation of the mKG fragments. Using this assay system, the authors screened inhibitors for TCF7/β-catenin, PAC1/PAC2, and PAC3 homodimer PPIs from 123,599 samples in their natural product library. Compound TB1 was identified as a specific inhibitor for PPI of PAC3 homodimer. TB1 strongly inhibited the PPI of PAC3 homodimer with an IC 50 value of 0.020 µM and did not inhibit PPI between TCF7/β-catenin and PAC1/PAC2 even at a concentration of 250 µM. The authors thus demonstrated that this in vitro PCA system applicable to HTS in a 1536-well format is capable of screening for PPI inhibitors from a huge natural product library. ( Journal of Biomolecular Screening 2009:970-979)

High throughput huaman pancreactic lipase screening of natural product library for lipase inhibition activity

Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
P Jiao ◽  
J Zhao ◽  
J Yeop Lee ◽  
J Tseng-Crank ◽  
B Corneliusen ◽  
...  
Keyword(s):  
Natural Product ◽  
High Throughput ◽  
Inhibition Activity ◽  
Natural Product Library ◽  
Lipase Screening ◽  
Lipase Inhibition

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

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 Sensitive ADAR editing reporter in cancer cells enables high-throughput screening of small molecule libraries

2018 ◽  
Vol 47 (4) ◽  
pp. e22-e22 ◽  
Author(s):  
Kajsa Fritzell ◽  
Li-Di Xu ◽  
Magdalena Otrocka ◽  
Claes Andréasson ◽  
Marie Öhman
Keyword(s):  
Cancer Cells ◽  
Small Molecule ◽  
High Throughput ◽  
High Throughput Screening ◽  
Small Molecule Libraries ◽  
Adar Editing

High throughput screening to identify new compounds with proapoptotic activity in resistant lung cancer cells

2015 ◽  
Vol 32 (3) ◽  
pp. 324
Author(s):  
P. Gilson ◽  
L. Vanwonterghem ◽  
F. Mahuteau ◽  
S. Piguel ◽  
J.L. Coll ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cancer Cells ◽  
High Throughput ◽  
High Throughput Screening ◽  
Lung Cancer Cells ◽  
New Compounds
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