This research, titled Fragment-Based Discovery of a Series of Allosteric-Binding Site Modulators of β‑Glucocerebrosidase, highlights the potential of fragment-based drug discovery (FBDD) and employs permeability assays with CacoReady and PreadyPort plates.
The article highlights the discovery of a series of azetidine derivatives, known as BGAz compounds, that exhibit potent bactericidal activity against both drug-sensitive Mycobacterium tuberculosis and multidrug-resistant TB strains.
In preclinical research, the choice of the appropriate well system format – whether it’s a transwell, non-transwell, or individual transwell – can significantly impact the outcome of experiments. Selecting the correct plate is crucial to working with permeability, toxicity, drug screening, or other assays.
OATP1B1 and OATP1B3 are two influx transporters of the SLCO gene family that are primarily expressed in the sinusoidal membrane of hepatocytes.
Understanding the role of these transporters in the clearance of new molecular entities (NME) is normally performed in-vitro at the early stages of drug development.
