The μ and δ types of opioid receptors form heteromers that exhibit pharmacological and
functional properties distinct from those of homomeric receptors. To characterize these …

STRONGHOLDS FOR DRUG DISCOVERY Historically, natural products (NPs) have played
a key role in the development of chemotherapy, 1, 2 and to this very day numerous marketed …

This issue of Molecular Pharmacology is dedicated to Dr. Avram Goldstein, the journal's
founding editor and one of the leaders in the development of modern pharmacology. This …

The growing availability of novel structures for several G protein-coupled receptors (GPCRs)
has provided new opportunities for structure-based drug design of ligands against this …

Opioids are effective analgesics, but their use is beset by serious side effects, including
addiction and respiratory depression, which contribute to the ongoing opioid crisis. The …

Opiates have been the most widely investigated class of natural products. 1 The two most
prominent opiates, morphine and codeine, have had a long history of use and abuse …

Despite the increasing number of GPCR structures and recent advances in peptide design,
the development of efficient technologies allowing rational design of high-affinity peptide …

The recent progress in crystallography of G-protein coupled receptors opens an
unprecedented venue for structure-based GPCR drug discovery. To test efficiency of the …

The κ opioid agonists are analgesics that seem to be free of undesired morphine-like effects.
Their dysphoric actions observed with the κ agonist cyclazocine are thought to be mediated …

Bifunctional μ-and δ-opioid receptor (OR) ligands are potential therapeutic alternatives, with
diminished side effects, to alkaloid opiate analgesics. We solved the structure of human δ …