Results 21 to 30 of about 665 (203)

Determination of Pseudokinase-ligand Interaction by a Fluorescence-based Thermal Shift Assay

Bio-Protocol, 2014
This protocol describes a robust technique for the measurement of pseudokinase-ligand interaction by a fluorescence-based Thermal Shift Assay (TSA).
Isabelle Lucet, Joanne Hildebrand, Peter Czabotar, Jian-Guo Zhang, Nicos Nicola, John Silke, Jeffrey Babon, James Murphy   +7 more
doaj   +1 more source

Thermal Proteome Profiling to Identify Protein-ligand Interactions in the Apicomplexan Parasite Toxoplasma gondii

Bio-Protocol, 2021
Toxoplasma gondii is a single-celled eukaryotic parasite that chronically infects a quarter of the global population. In recent years, phenotypic screens have identified compounds that block parasite replication.
Alice Herneisen, Sebastian Lourido
doaj   +1 more source

Optimization of protein samples for NMR using thermal shift assays [PDF]

Journal of Biomolecular NMR, 2016
Maintaining a stable fold for recombinant proteins is challenging, especially when working with highly purified and concentrated samples at temperatures >20 °C. Therefore, it is worthwhile to screen for different buffer components that can stabilize protein samples.
Sandra Kozak, Lukas Lercher, Megha N. Karanth, Rob Meijers, Teresa Carlomagno, Stephane Boivin   +5 more
openaire   +3 more sources

High-Throughput Cellular Thermal Shift Assays in Research and Drug Discovery [PDF]

SLAS Discovery, 2020
Thermal shift assays (TSAs) can reveal changes in protein structure, due to a resultant change in protein thermal stability. Since proteins are often stabilized upon binding of ligand molecules, these assays can provide a readout for protein target engagement.
Mark J. Henderson, Marc A. Holbert, Anton Simeonov, Lorena A. Kallal   +3 more
openaire   +2 more sources

Real-Time Cellular Thermal Shift Assay to Monitor Target Engagement

ACS Chemical Biology, 2022
Determining a molecule's mechanism of action is paramount during chemical probe development and drug discovery. The cellular thermal shift assay (CETSA) is a valuable tool to confirm target engagement in cells for a small molecule that demonstrates a pharmacological effect.
Tino W. Sanchez, Michael H. Ronzetti, Ashley E. Owens, Maria Antony, Ty Voss, Eric Wallgren, Daniel Talley, Krishna Balakrishnan, Sebastian E. Leyes Porello, Ganesha Rai, Juan J. Marugan, Samuel G. Michael, Bolormaa Baljinnyam, Noel Southall, Anton Simeonov, Mark J. Henderson   +15 more
openaire   +2 more sources

Thermal Shift Assay for Small GTPase Stability Screening: Evaluation and Suitability

International Journal of Molecular Sciences, 2022
Thermal unfolding methods are commonly used as a predictive technique by tracking the protein’s physical properties. Inherent protein thermal stability and unfolding profiles of biotherapeutics can help to screen or study potential drugs and to find stabilizing or destabilizing conditions.
Kopra, Kari, Valtonen, Salla, Mahran, Randa, Kapp, Jonas N, Hassan, Nazia, Gillette, William, Dennis, Bryce, Li, Lianbo, Westover, Kenneth D, Plückthun, Andreas, Härmä, Harri   +10 more
openaire   +2 more sources

Gentiopicroside targets PAQR3 to activate the PI3K/AKT signaling pathway and ameliorate disordered glucose and lipid metabolism

Acta Pharmaceutica Sinica B, 2022
The obstruction of post-insulin receptor signaling is the main mechanism of insulin-resistant diabetes. Progestin and adipoQ receptor 3 (PAQR3), a key regulator of inflammation and metabolism, can negatively regulate the PI3K/AKT signaling pathway. Here,
Haiming Xiao, Xiaohong Sun, Zeyuan Lin, Yan Yang, Meng Zhang, Zhanchi Xu, Peiqing Liu, Zhongqiu Liu, Heqing Huang   +8 more
doaj   +1 more source

Detection of thermal shift in cellular Keap1 by protein-protein interaction inhibitors using immunoblot- and fluorescence microplate-based assays

STAR Protocols, 2022
Summary: Pharmacologic inhibition of the protein-protein interaction (PPI) interface of the Keap1:Nrf2 complex, which leads to Nrf2 activation and cytoprotective gene expression, offers a promising strategy for disease prevention and treatment.
Sharadha Dayalan Naidu, Dina Dikovskaya, Terry W. Moore, Albena T. Dinkova-Kostova   +3 more
doaj   +1 more source

Synthesis and biological evaluation of thiazole derivatives as LbSOD inhibitors

Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Leishmaniasis is considered as one of the major neglected tropical diseases due to its magnitude and wide geographic distribution. Leishmania braziliensis, responsible for cutaneous leishmaniasis, is the most prevalent species in Brazil.
Camila C. Bitencourt Brito, Hélder Vinicius Carneiro da Silva, Daci José Brondani, Antonio Rodolfo de Faria, Rafael Matos Ximenes, Ivanildo Mangueira da Silva, Julianna F. C. de Albuquerque, Marcelo Santos Castilho   +7 more
doaj   +1 more source

Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement

Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Testing of an expanded, 800-compound set of analogues of the earlier described Strecker-type α-aminonitriles (selected from publicly available Enamine Ltd.
Mikhail Krasavin, Stanislav Kalinin, Sergey Zozulya, Anastasia Griniukova, Petro Borysko, Andrea Angeli, Claudiu T. Supuran   +6 more
doaj   +1 more source