The voltage-gated sodium channel Na V 1.7 is a genetically validated pain target under
investigation for the development of analgesics. A therapeutic with a less frequent dosing …

Drug discovery research on new pain targets with human genetic validation, including the
voltage-gated sodium channel Na V 1.7, is being pursued to address the unmet medical need …

Abstract Intramolecular Diels-Alder reactions of a series of substrates with 4-
triisopropylsilyloxy-2H-thiopyran as the diene and a dienophile attached to each of the four …

The identification of nonopioid alternatives to treat chronic pain has received a great deal of
interest in recent years. Recently, the engineering of a series of Nav1.7 inhibitory peptide-…

On présente une étude des réactions DAIM des dérivés du 4-[tris(2-méthyléthyl)silyl]oxy-2H-thiopyrane
avec des diénophiles potentiels attachés en positions C-2, C-3, C-5 et C-6. On n'…

The novel solution phase synthesis of an array of biologically relevant pyrazoloquinazolinones
in a simple microwave driven, one pot procedure is described. Transformations are …

Using fragment-based screening of a focused fragment library, 2-aminoquinoline 1 was
identified as an initial hit for BACE1. Further SAR development was supported by X-ray …

… A Notch luciferase reporter gene assay (in which a luciferase construct was inserted
under the control of the Notch promoter, in TE-671 cells and Luciferase luminescence was …

1. Large White male turkeys from a heavy commercial male-line were fed on 16 diets containing
4 concentrations of calcium (6, 10, 14 and 18 g/kg) and available phosphorus (3, 5, 7, 9 …

Small molecules and antibodies each have advantages and limitations as therapeutics.
Here, we present for the first time to our knowledge, the structure-guided design of “chemibodies…