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 …

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) …

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 …

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 …

Monitoring drug target engagement in cells and tissues using the cellular thermal shift assay

DM Molina, R Jafari, M Ignatushchenko, T Seki… - Science, 2013 - science.org
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 …

[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 …

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 …

The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability

FH Niesen, H Berglund, M Vedadi - Nature protocols, 2007 - nature.com
Differential scanning fluorimetry (DSF) is a rapid and inexpensive screening method to
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

A Nocentini, A Angeli, F Carta, JY Winum… - Journal of Enzyme …, 2021 - Taylor & Francis
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 …

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 …