The topic of this chapter, transient receptor potential ankyrin 1 (TRPA1), is a calcium-
permeable nonselective cation channel that is a member of the TRP family expressed on …

The majority of bioactive molecules act on membrane proteins or intracellular targets and
therefore needs to partition into or cross biological membranes. Natural products often …

Fluorinated prolines play an important role in peptide studies, protein engineering,
medicinal chemistry, drug discovery, and agrochemistry. Since the first synthesis of 4 …

Transient receptor potential ankyrin 1 (TRPA1) is a nonselective calcium ion channel highly
expressed in the primary sensory neurons, functioning as a polymodal sensor for …

In this work, an amorphous solid dispersion (ASD) formulation was systematically developed
to simultaneously enhance bioavailability and mitigate the mechanical instability risk of the …

Parkinson's disease is the second most prevalent progressive neurodegenerative disorder
characterized by the loss of dopaminergic neurons in the substantia nigra. Loss-of-function …

Transient receptor potential ankyrin 1 (TRPA1) channel, as a nonselective ligand-gated
cation channel robustly in dorsal root ganglion sensory neurons, is implicated in sensing …

In mammalian cells, all-trans farnesol, a 15-carbon isoprenol, is a product of the mevalonate
pathway. It is the natural substrate of alcohol dehydrogenase and a substrate for CYP2E1 …

A growing number of G-protein-coupled receptor (GPCR) structures reveal novel
transmembrane lipid-exposed allosteric sites. Ligands must first partition into the …

We report a fit-for-purpose, stereocontrolled, and chromatography-free first-generation
manufacturing process for GDC-6599 (1), a TRPA1 inhibitor, to enable first-in-human clinical …