Dopamine (DA) is a critical neurotransmitter in the mammalian central nervous system
(CNS). The cerebral dopaminergic system is implicated in the pathophysiology of several …

Morphine is an alkaloid from the opium poppy used to treat pain. The potentially lethal side
effects of morphine and related opioids—which include fatal respiratory depression—are …

A major challenge in cancer therapy is tumor drug resistance. To overcome it, it is essential
to understand the mechanisms and identify the molecules involved, so that they can be …

Using stabilized “soft” nucleophiles in copper-catalyzed allylic substitutions is highly
desirable but remains an unsolved challenge for the last 40 years. In this work, a general …

Starting from dopamine receptor ligand BP897, an interactive drug discovery process
leading to heterocyclic bioisosteres is demonstrated. The four step strategy involved a …

G protein–coupled receptors (GPCRs), including dopamine receptors, represent a group of
important pharmacological targets. An increased formation of dopamine receptor D2 …

Crystal structures of G protein-coupled receptor (GPCR) ligand complexes allow a rational
design of novel molecular probes and drugs. Here we report the structure-guided design …

Structural studies on G protein-coupled receptors (GPCRs) provide important insights into
the architecture and function of these important drug targets. However, the crystallization of …

The high affinity dopamine D4 receptor ligand APH199 and derivatives thereof exhibit bias
toward the Gi signaling pathway over β-arrestin recruitment compared to quinpirole. Based …

Dimerization of terminal alkynes is a very practical and straightforward approach to
conjugated enynes-important building blocks for synthetic organic chemistry and key units …