Results 1 to 10 of about 615 (167)

Capsaicin Targets tNOX (ENOX2) to Inhibit G1 Cyclin/CDK Complex, as Assessed by the Cellular Thermal Shift Assay (CETSA)

Cells, 2019
Capsaicin (8-methyl-N-vanillyl-6-noneamide), which is an active component in red chili peppers, is used as a chemopreventive agent that shows favorable cytotoxicity against cancer cells.
Atikul Islam, Ally J. Su, Zih-Ming Zeng, Pin Ju Chueh, Ming-Hung Lin   +4 more
doaj   +3 more sources

A superior loading control for the cellular thermal shift assay

Scientific Reports, 2022
The cellular thermal shift assay (CETSA), as a method to determine protein–ligand interaction and cellular protein modification, has rapidly become routine laboratory practice. However, current options to determine that (1) sample was loaded in each lane
Alexandré Delport, Raymond Hewer
doaj   +1 more source

A multifunctional cross-validation high-throughput screening protocol enabling the discovery of new SHP2 inhibitors

Acta Pharmaceutica Sinica B, 2021
The protein tyrosine phosphatase Src homology phosphotyrosyl phosphatase 2 (SHP2) is implicated in various cancers, and targeting SHP2 has become a promising therapeutic approach.
Yihui Song, Min Zhao, Yahong Wu, Bin Yu, Hong-Min Liu   +4 more
doaj   +1 more source

EDTA aggregates induce SYPRO orange-based fluorescence in thermal shift assay. [PDF]

PLoS ONE, 2017
Ethylenediaminetetraacetic acid (EDTA) is widely used in the life sciences as chelating ligand of metal ions. However, formation of supramolecular EDTA aggregates at pH > 8 has been reported, which may lead to artifactual assay results. When applied as a
Tobias Kroeger, Benedikt Frieg, Tao Zhang, Finn K Hansen, Andreas Marmann, Peter Proksch, Luitgard Nagel-Steger, Georg Groth, Sander H J Smits, Holger Gohlke   +9 more
doaj   +1 more source

The iterative application of a large chemical space in the drug discovery process

Журнал органічної та фармацевтичної хімії, 2021
Aim. To demonstrate the advantages of large-scale virtual libraries generated using chemical protocols previously validated in primary steps of the drug discovery process. Results and discussion.
Olena V. Savych, Anastasia V. Gryniukova, Diana O. Alieksieieva, Igor M. Dziuba, Petro O. Borysko, Dmytro V. Dudenko, Volodymyr S. Brovarets, Yurii S. Moroz   +7 more
doaj   +1 more source

New Chemotypes for the Inhibition of (p)ppGpp Synthesis in the Quest for New Antimicrobial Compounds

Molecules, 2022
Antimicrobial resistance (AMR) poses a serious threat to our society from both the medical and economic point of view, while the antibiotic discovery pipeline has been dwindling over the last decades.
Crescenzo Coppa, Luca Sorrentino, Monica Civera, Marco Minneci, Francesca Vasile, Sara Sattin   +5 more
doaj   +1 more source

Characterization of ligand-induced thermal stability of the human organic cation transporter 2 (OCT2)

Frontiers in Pharmacology, 2023
Introduction: The human organic cation transporter 2 (OCT2) is involved in the transport of endogenous quaternary amines and positively charged drugs across the basolateral membrane of proximal tubular cells.
Max Maane, Fangrui Xiu, Fangrui Xiu, Peter Bellstedt, Gerd A. Kullak-Ublick, Michele Visentin   +5 more
doaj   +1 more source

Norlobaridone Inhibits Quorum Sensing-Dependent Biofilm Formation and Some Virulence Factors in Pseudomonas aeruginosa by Disrupting Its Transcriptional Activator Protein LasR Dimerization

Biomolecules, 2023
In the present study, norlobaridone (NBD) was isolated from Parmotrema and then evaluated as a new potent quorum sensing (QS) inhibitor against Pseudomonas aeruginosa biofilm development. This phenolic natural product was found to reduce P.
Raya Soltane, Ahlam Alasiri, Mostafa N. Taha, Rehab H. Abd El-Aleam, Kawthar Saad Alghamdi, Mosad A. Ghareeb, Doaa El-Ghareeb Keshek, Susana M. Cardoso, Ahmed M. Sayed   +8 more
doaj   +1 more source

Inhibiting PHGDH with NCT-503 reroutes glucose-derived carbons into the TCA cycle, independently of its on-target effect

Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
The small-molecule inhibitor of phosphoglycerate dehydrogenase, NCT-503, reduces incorporation of glucose-derived carbons into serine in vitro.
Birte Arlt, Guido Mastrobuoni, Jasmin Wuenschel, Kathy Astrahantseff, Angelika Eggert, Stefan Kempa, Hedwig E. Deubzer   +6 more
doaj   +1 more source

An open source plant kinase chemogenomics set

Plant Direct, 2022
One hundred twenty‐nine protein kinases, selected to represent the diversity of the rice (Oryza sativa) kinome, were cloned and tested for expression in Escherichia coli.
Maria Florencia Ercoli, Priscila Zonzini Ramos, Rashmi Jain, Joseph Pilotte, Oliver Xiaoou Dong, Ty Thompson, Carrow I. Wells, Jonathan M. Elkins, Aled M. Edwards, Rafael M. Couñago, David H. Drewry, Pamela C. Ronald   +11 more
doaj   +1 more source