The mode of action of the Protein tyrosine phosphatase 1B inhibitor Ertiprotafib.
PLoS ONE, 2020 Protein tyrosine phosphatase 1B (PTP1B) is a validated therapeutic target for the treatment of diabetes and obesity. Ertiprotafib is a PTP1B inhibitor that reached the clinical trial stage for the treatment of diabetes.
Ganesan Senthil Kumar +2 more
doaj +2 more sources
PLoS ONE, 2012 Most proteins have not evolved for maximal thermal stability. Some are only marginally stable, as for example, the DNA-binding domains of p53 and its homologs, whose kinetic and thermodynamic stabilities are strongly correlated.
Tobias Brandt +3 more
doaj +1 more source
Conformationally responsive dyes enable protein-adaptive differential scanning fluorimetry
, 2023 Abstract Flexible in vitro methods alter the course of biological discoveries. Differential Scanning Fluorimetry (DSF) is a particularly versatile technique which reports protein thermal unfolding via fluorogenic dye.
Taiasean Wu +13 more
openaire +2 more sources
High-Throughput Differential Scanning Fluorimetry of GFP-Tagged Proteins
, 2019 Differential scanning fluorimetry is useful for a wide variety of applications including characterization of protein function, structure-activity relationships, drug screening, and optimization of buffer conditions for protein purification, enzyme activity, and crystallization.
Sorenson, Alanna E. +1 more
openaire +3 more sources
DMAN: a Java tool for analysis of multi-well differential scanning fluorimetry experiments [PDF]
Bioinformatics, 2011 Abstract Summary: Differential scanning fluorimetry (DSF) is a rapid technique that can be used in structural biology to study protein–ligand interactions. We have developed DMAN, a novel tool to analyse multi-well plate data obtained in DSF experiments. DMAN is easy to install and provides a user-friendly interface.
Conan K. Wang +3 more
openaire +5 more sources
In Depth Analysis of Kinase Cross Screening Data to Identify CAMKK2 Inhibitory Scaffolds
Molecules, 2020 The calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2) activates CAMK1, CAMK4, AMPK, and AKT, leading to numerous physiological responses. The deregulation of CAMKK2 is linked to several diseases, suggesting the utility of CAMKK2 inhibitors ...
Sean N. O’Byrne +11 more
doaj +1 more source
Temperature and pH-Dependent Behaviors of mAb Drugs: A Case Study for Trastuzumab
Scientia Pharmaceutica, 2022 The distortions in the high-order structure of therapeutic monoclonal antibodies (mAbs) under different environmental conditions acutely affect mAb stability, resulting in altered safety, efficacy, and shelf-life profiles.
Fatma Sert +6 more
doaj +1 more source
A beginner’s guide to differential scanning fluorimetry
The BiochemistDifferential scanning fluorimetry (DSF) is a technique used to determine a protein’s stability. In a typical DSF experiment, a purified protein is heated in the presence of a fluorescent dye and the resulting temperature vs fluorescence plot is used to calculate its apparent melting temperature.
Charvat, Annemarie F +2 more
openaire +2 more sources
The use of differential scanning fluorimetry in the rational design of plastic antibodies for protein targets [PDF]
The Analyst, 2016 Predicted interactions between acrylic monomers and proteins, and melting profiles using DSF in the rational design of MIP-NPs for proteins.
Ashley, J. +2 more
openaire +4 more sources
Differential Scanning Fluorimetry provides high throughput data on silk protein transitions. [PDF]
Sci Rep, 2014 Here we present a set of measurements using Differential Scanning Fluorimetry (DSF) as an inexpensive, high throughput screening method to investigate the folding of silk protein molecules as they abandon their first native melt conformation, dehydrate and denature into their final solid filament conformation.
Vollrath F +4 more
europepmc +6 more sources