J. A. Javitch

The in vitro functional profiles of fentanyl and nitazene analogs at the μ-opioid receptor - high efficacy is dangerous regardless of signaling bias

This study evaluates the in vitro functional profiles of fentanyl and nitazene analogs at the μ-opioid receptor, finding that high intrinsic efficacy in Gi signaling correlates with increased risk of intoxication, regardless of signaling bias.

Impact of membrane lipid polyunsaturation on dopamine D2 receptor ligand binding and signaling

This study shows that n-3 PUFAs enhance D2R ligand binding and signaling, suggesting they act as allosteric modulators of the receptor.

Novel Class of Psychedelic Iboga Alkaloids Disrupts Opioid Addiction States

This paper introduces a new class of iboga alkaloids, oxa-iboga, which show therapeutic efficacy in opioid use disorder without cardiac risks, as demonstrated in rat models.

A novel mitragynine analog with low efficacy mu-opioid receptor agonism displays antinociception with attenuated adverse effects

The paper develops a novel mitragynine analog with reduced mu-opioid receptor efficacy and adverse effects, showing antinociception without respiratory depression or hyperlocomotion.

A novel luminescence-based β-arrestin membrane recruitment assay for unmodified GPCRs

This paper introduces a luminescence-based assay to measure arrestin recruitment to unmodified GPCRs, avoiding C-terminal modifications.

Role of transmembrane helix 6 in substrate recognition of the amino acid transporter MhsT

The paper investigates how the flexibility of a GMG motif in TM6 of MhsT enables substrate recognition of different amino acid sizes by shaping the binding site.

Distinct antagonist-bound inactive states underlie the divergence in the structures of the dopamine D2 and D3 receptors

The paper identifies distinct antagonist-bound inactive states in dopamine D2 and D3 receptors, showing conformational diversity with implications for drug discovery.

The allosteric mechanism of substrate-specific transport in SLC6 is mediated by a volumetric sensor

The paper identifies an allosteric mechanism involving residues F259 and I359 that modulates Na+ release and substrate transport in SLC6 family proteins.