Owing to their inherent three-dimensionality and structural novelty, spiro scaffolds have
been increasingly utilized in drug discovery. In this brief review, we highlight selected …

G-protein-coupled receptors (GPCRs) have been tractable drug targets for decades with
over one-third of currently marketed drugs targeting GPCRs. Of these, the class A GPCR …

The discovery of allosteric modulators of G protein-coupled receptors (GPCRs) provides a
promising new strategy with potential for developing novel treatments for a variety of central …

Allosteric modulation of G protein-coupled receptors (GPCRs) is nowadays a hot topic in
medicinal chemistry. Allosteric modulators, ie, compounds which bind in a receptor site …

Parkinson&aposs disease (PD) is t he second most common form of neurodegenerative
disorders that results from the progressive loss of dopaminergic neurons in the midbrain …

Herein, we present an overview of the historic development of drugs for the treatment of
Parkinson's disease as well as prospective novel treatment forms based on targeting the …

A variety of stable, small-molecule peptidomimetic ligands have been developed to
elucidate the mechanism by which the neuropeptide Pro-Leu-Gly-NH 2 (PLG) modulates …

We have synthesized a curcumin derivative, 4-{5-(4-hydroxy-3-methoxy-phenyl)-2-[3-(4-
hydroxy-3-methoxy-phenyl)-acryloyl]-3-oxo-penta-1, 4-dienyl}-piperidine-1-carboxylic acid …

The activity of G protein-coupled receptors (GPCRs) is intricately regulated by a range of
intracellular proteins, including G protein-coupled kinases (GRKs) and arrestins …

Terms such as “nondruggable GPCRs” describe a unique group of GPCRs having strong
biological hypothesis validation, but for which medicinal chemistry efforts based on …