Permeability assays are important for understanding how molecules cross biological barriers, assessing both their ability to cross and the mechanisms involved. While drugs are often absorbed by passive diffusion, some molecules can also be substrates for membrane proteins or transporters.
The permeability assay protocol for Caco-2 cells serves as a cornerstone in understanding and predicting the intestinal absorption of pharmaceutical agents.
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.
In a recent publication in the Journal of Medicinal Chemistry, a collaborative research led by the scientist Dr. H. Day, in conjunction with a consortium of researchers, explored the development of allosteric inhibitors targeting SH2 domain-containing protein tyrosine phosphatase-2 (SHP2) for cancer therapy.
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.
