Autotaxin is the enzyme responsible for the production of lysophosphatidic acid (LPA) from
lysophosphatidyl choline (LPC), and it is up-regulated in many inflammatory conditions, …

Penetration by an object through a dense granular medium (for example, by a finger pushing
slowly into the sand on a beach) presents an interesting physics problem 1 that is closely …

Glecaprevir was identified as a potent HCV NS3/4A protease inhibitor, and an enabling
synthesis was required to support the preclinical evaluation and subsequent Phase I clinical trials…

The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also
known as RORγt) is a promising target for the treatment of autoimmune diseases. A small …

The work described herein demonstrates the utility of structure-based drug design (SBDD) in
shifting the binding mode of an HTS hit from a DFG-in to a DFG-out binding mode resulting …

A concise stereoselective approach to the spirobicyclic imine fragment of pinnatoxins and
pteriatoxins is described. The approach relies on a tandem reaction sequence involving …

The preceding article described the development of the large-scale synthetic route to
macrocycle 3 of glecaprevir (1), a potent HCV protease inhibitor. This article describes the …

Fatty acid amide hydrolase (FAAH) is an integral membrane serine hydrolase responsible
for the degradation of fatty acid amide signaling molecules such as endocannabinoid …

Hematopoietic prostaglandin D synthase (HPGDS) is primarly expressed in mast cells,
antigen-presenting cells, and Th-2 cells. HPGDS converts PGH 2 into PGD 2 , a mediator thought …

Glecaprevir was identified as a potent hepatitis C virus (HCV) protease inhibitor, and a large-scale
synthesis was required to support the late-stage clinical trials and subsequent …