The emergence of superbugs that are resistant to last-resort antibiotics poses a serious
threat to human health, and we are in a “race against time to develop new antibiotics.” New …

The human cannabinoid 2 GPCR (hCB2) is a prime therapeutic target. To define potential
cysteine-related binding motifs critical to hCB2-ligand interaction, a library of hCB2 cysteine …

Pyrazole derivatives, as a class of heterocyclic compounds, possess unique chemical
structures that confer them with a broad spectrum of pharmacological activities. They have …

The nitrogen-bearing heterocycle pyridine in its several analogous forms occupies an
important position as a precious source of clinically useful agents in the field of medicinal …

Heterocycles are a cornerstone of fragment-based drug discovery (FBDD) due to their
prevalence in biologically active compounds. However, novel heterocyclic fragments are …

Background: Pyrazoline scaffold is a key structural motif found among pharmaceutically
active molecules including synthetic and natural products. The molecules with pyrazoline …

The transport of drug molecules is mainly determined by the distribution of influx and efflux
transporters for which they are substrates. To enable tissue targeting, we sought to develop …

ABL2 (also known as ARG (ABL related gene)) is closely related to the well-studied Abelson
kinase cABL. ABL2 is involved in human neoplastic diseases and is deregulated in solid …

Imidazopyridazines are fused heterocycles, like purines, with a pyridazine ring replacing the
pyrimidine ring in purines. Imidazopyridazines have been primarily studied for their kinase …

We recently established the mechanism-based inactivation (MBI) of cytochrome P450 3A
(CYP3A) by the fibroblast growth factor receptor (FGFR) inhibitors erdafitinib and infigratinib …