A5022925390- Mass Spectrometry Techniques and Applications
- Diabetes Treatment and Management
- Biosimilars and Bioanalytical Methods
- Innovative Microfluidic and Catalytic Techniques Innovation
- Biotechnology and Related Fields
- Pharmaceutical Economics and Policy
- Cell Image Analysis Techniques
- Receptor Mechanisms and Signaling
- Neuropeptides and Animal Physiology
Sanofi (Germany)
2019-2022
The therapeutic success of peptidic GLP-1 receptor agonists for treatment type 2 diabetes mellitus (T2DM) motivated our search orally bioavailable small molecules that can activate the (GLP-1R) as a well-validated target T2DM. Here, discovery and characterization potent selective positive allosteric modulator (PAM) GLP-1R based on 3,4,5,6-tetrahydro-1H-1,5-epiminoazocino[4,5-b]indole scaffold is reported. Optimization this series from HTS was supported by ligand binding model. Biological in...
Acoustic droplet ejection mass spectrometry (ADE-MS) has recently emerged as a promising label-free, MS-based readout method for high throughput screening (HTS) campaigns in early pharmaceutical drug discovery, since it enables high-speed analysis directly from 384- or 1536-well plates. In this manuscript we describe our characterization of an ADE-MS based sample content enzymatic assay mutant isocitrate dehydrogenase 1 (IDH1) R132H with strong focus on development. IDH1 become very...