Results 61 to 70 of about 137,634 (294)

High-throughput screening assay used in pharmacognosy: Selection, optimization and validation of methods of enzymatic inhibition by UV-visible spectrophotometry [PDF]

Journal of Pharmacy & Pharmacognosy Research, 2014
In research laboratories of both organic synthesis and extraction of natural products, every day a lot of products that can potentially introduce some biological activity are obtained.
Graciela Granados-Guzmán, Noemí Waksman de Torres, Rocío Castro-Ríos, Ricardo Salazar-Aranda   +3 more
doaj  

Organoid drug screening in cancer: advances in high-throughput platforms and clinical applications [PDF]

Organoid
Patient-derived tumor organoids represent the most physiologically relevant 3-dimensional (3D) cancer models, preserving tumor heterogeneity and native tissue architecture.
Jiho Lee, Hyun Ju Kang, Jin-Ku Lee
doaj   +1 more source

Optimization of Spectrophotometric and Fluorometric Assays Using Alternative Substrates for the High-Throughput Screening of Lipase Activity

Journal of Chemistry, 2021
The effects of reaction conditions on the spectrophotometric and fluorometric assays using alternative substrates (p-nitrophenyl palmitate and 4-methylumbelliferyl oleate) were investigated to optimize them for the high-throughput screening of lipase ...
Jun-Young Park, Jisu Ha, Yoonseok Choi, Pahn-Shick Chang, Kyung-Min Park   +4 more
doaj   +1 more source

Modulation of Homer1 EVH1 domain internal dynamics by putative autism‐associated mutations

FEBS Letters, EarlyView.
The putative autism‐associated M65I and S97L variants of the EVH1 domain of the postsynaptic scaffold protein Homer1 do not exhibit substantial changes in their overall structure or partner binding. Both of them, but especially the M65I variant, show altered internal dynamics relative to the wild‐type domain on the μs‐ms timescale, indicated by the ...
Fanni Farkas, Brigitta Maruzs, Zsófia E. Kálmán, Tomas Klumpler, Gyula Batta, Bálint Péterfia, Zoltán Gáspári   +6 more
wiley   +1 more source

In vitro high throughput screening of compounds for favorable metabolic properties in drug discovery

, 2001
Drug metabolism can have profound effects on the pharmacological and toxicological profile of therapeutic agents. In the pharmaceutical industry, many in vitro techniques are in place or under development to screen and optimize compounds for favorable ...
Masimirembwa, CM, Andersson, TB, Thompson, R   +2 more
core   +1 more source

High-throughput mass spectrometry based assays for detection of reactive compounds

Green Analytical Chemistry
High-throughput screening (HTS) is a foundational approach in small molecule drug discovery, but false positives due to reactive compounds can waste resources and hinder progress. Nuisance assays are therefore required to identify such compounds; however,
Fan Pu, Sangeeta Pandey, Qi Sun, Kristine E. Frank, Chaohong Sun, Jon D. Williams, Sujatha M. Gopalakrishnan, Nathaniel L. Elsen   +7 more
doaj   +1 more source

Network divergence analysis identifies adaptive gene modules and two orthogonal vulnerability axes in pancreatic cancer

Molecular Oncology, EarlyView.
Tumors contain diverse cellular states whose behavior is shaped by context‐dependent gene coordination. By comparing gene–gene relationships across biological contexts, we identify adaptive transcriptional modules that reorganize into distinct vulnerability axes.
Brian Nelson, Lyanne Delgado‐Coka, Natalia Marchenko, Luisa F. Escobar‐Hoyos, Kenneth R. Shroyer, Alisa Yurovsky, Trey Ideker, Gábor Balázsi, Thomas MacCarthy, Scott Powers   +9 more
wiley   +1 more source

Gametocyte-specific and all-blood-stage transmission-blocking chemotypes discovered from high throughput screening on Plasmodium falciparum gametocytes

Communications Biology, 2022
High-throughput screening of 120,000 compounds followed by counter-screening and validation assays reveals candidate antimalarial drugs that kill Plasmodium falciparum sexual and asexual blood stages blocking parasite transmission through mosquito.
Giacomo Paonessa, Giulia Siciliano, Rita Graziani, Cristiana Lalli, Ottavia Cecchetti, Cristina Alli, Roberto La Valle, Alessia Petrocchi, Alessio Sferrazza, Monica Bisbocci, Mario Falchi, Carlo Toniatti, Alberto Bresciani, Pietro Alano   +13 more
doaj   +1 more source

EDNRB‐dependent endothelin signaling reduces proliferation and promotes proneural‐to‐mesenchymal transition in gliomas

Molecular Oncology, EarlyView.
Glioma cells mainly express the endothelin receptor EDNRB, while EDNRA is restricted to a perivascular tumor subpopulation. Endothelin signaling reduces glioma cell proliferation while promoting migration and a proneural‐to‐mesenchymal transition associated with poor prognosis. This pathway activates Ca2+, K+, ERK, and STAT3 signalings and is regulated
Donovan Pineau, Leonor Garcia, Hugo Arnold, Antonija Hanžek, Maialen Arrieta, Laurent R Gauthier, Christine Granotier‐Beckers, François D Boussin, Amaury Herbet, Marie Hautière, Valentin Asei‐Ceschino, Clémentin Jacques, Laura Brard, Thomas Harnois, Valérie Coronas, Bruno Constantin, Aurélien Chatelier, Jean Chemin, Serge Urbach, Martial Seveno, Szimonetta Hideg, Chantal Ripoll, Kasandra Aguilar‐Cázarez, Min Zheng, Guo‐Hao Huang, Sheng‐Qing Lv, Lei Zhang, Philippe Rondard, Laurent Prezeau, Jean‐Philippe Pin, Hugues Duffau, Luc Bauchet, Valérie Rigau, Franck Denat, Charles Truillet, Didier Boquet, Jean‐Philippe Hugnot   +36 more
wiley   +1 more source

Artificial tissue binding models : development and comparative evaluation of high - throughput lipophilicity assays and their use for PET tracer optimization [PDF]

, 2015
The purpose of this thesis was to increase the efficiency of the Positron Emission Tomography (PET) tracer development process. Since many neuroimaging agents fail due to undesirably high non-specific binding (NSB) to brain tissue, we aimed at estimating
Assmus, Frauke
core   +1 more source