Theory and applications of differential scanning fluorimetry in early-stage drug discovery
K Gao, R Oerlemans, MR Groves - Biophysical reviews, 2020 - Springer
Differential scanning fluorimetry (DSF) is an accessible, rapid, and economical biophysical
technique that has seen many applications over the years, ranging from protein folding state …
technique that has seen many applications over the years, ranging from protein folding state …
Human protein tyrosine phosphatase 1B (PTP1B): from structure to clinical inhibitor perspectives
R Liu, C Mathieu, J Berthelet, W Zhang… - International Journal of …, 2022 - mdpi.com
Phosphorylation is an essential process in biological events and is considered critical for
biological functions. In tissues, protein phosphorylation mainly occurs on tyrosine (Tyr) …
biological functions. In tissues, protein phosphorylation mainly occurs on tyrosine (Tyr) …
The cellular thermal shift assay for evaluating drug target interactions in cells
R Jafari, H Almqvist, H Axelsson, M Ignatushchenko… - Nature protocols, 2014 - nature.com
Thermal shift assays are used to study thermal stabilization of proteins upon ligand binding.
Such assays have been used extensively on purified proteins in the drug discovery industry …
Such assays have been used extensively on purified proteins in the drug discovery industry …
Analysis of protein stability and ligand interactions by thermal shift assay
K Huynh, CL Partch - Current protocols in protein science, 2015 - Wiley Online Library
Purification of recombinant proteins for biochemical assays and structural studies is time‐
consuming and presents inherent difficulties that depend on the optimization of protein …
consuming and presents inherent difficulties that depend on the optimization of protein …
Monitoring drug target engagement in cells and tissues using the cellular thermal shift assay
The efficacy of therapeutics is dependent on a drug binding to its cognate target.
Optimization of target engagement by drugs in cells is often challenging, because drug …
Optimization of target engagement by drugs in cells is often challenging, because drug …
[HTML][HTML] Structural basis for small molecule targeting of the programmed death ligand 1 (PD-L1)
KM Zak, P Grudnik, K Guzik, BJ Zieba, B Musielak… - Oncotarget, 2016 - ncbi.nlm.nih.gov
Abstract Targeting the PD-1/PD-L1 immunologic checkpoint with monoclonal antibodies has
provided unprecedented results in cancer treatment in the recent years. Development of …
provided unprecedented results in cancer treatment in the recent years. Development of …
Discovery of MK-1454: a potent cyclic dinucleotide stimulator of interferon genes agonist for the treatment of cancer
W Chang, MD Altman, CA Lesburg… - Journal of Medicinal …, 2022 - ACS Publications
Stereochemically and structurally complex cyclic dinucleotide-based stimulator of interferon
genes (STING) agonists were designed and synthesized to access a previously unexplored …
genes (STING) agonists were designed and synthesized to access a previously unexplored …
The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability
Differential scanning fluorimetry (DSF) is a rapid and inexpensive screening method to
identify low-molecular-weight ligands that bind and stabilize purified proteins. The …
identify low-molecular-weight ligands that bind and stabilize purified proteins. The …
Reconsidering anion inhibitors in the general context of drug design studies of modulators of activity of the classical enzyme carbonic anhydrase
Inorganic anions inhibit the metalloenzyme carbonic anhydrase (CA, EC 4.2. 1.1) generally
by coordinating to the active site metal ion. Cyanate was reported as a non-coordinating CA …
by coordinating to the active site metal ion. Cyanate was reported as a non-coordinating CA …
The cellular thermal shift assay: a novel biophysical assay for in situ drug target engagement and mechanistic biomarker studies
D Martinez Molina, P Nordlund - Annual review of …, 2016 - annualreviews.org
A drug must engage its intended target to achieve its therapeutic effect. However,
conclusively measuring target engagement (TE) in situ is challenging. This complicates …
conclusively measuring target engagement (TE) in situ is challenging. This complicates …