Bryan L. Roth
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View article: Nanobody-drug conjugates for targeting specific GPCR pairs
Nanobody-drug conjugates for targeting specific GPCR pairs Open
Bitopic ligands that engage two distinct binding sites offer exciting opportunities for finely tuned control of G protein-coupled receptor signaling. A recent study in PLOS Biology employed click chemistry to generate novel nanobody-small …
View article: Psychedelic compounds directly excite 5-HT2A layer V medial prefrontal cortex neurons through 5-HT2A Gq activation
Psychedelic compounds directly excite 5-HT2A layer V medial prefrontal cortex neurons through 5-HT2A Gq activation Open
Psilocybin, and its active metabolite psilocin, have seen renewed interest due to studies suggesting potential therapeutic utility. 5-Hydroxytryptamine2A receptors (5-HT2ARs) are primary mediators of the psychoactive effects of psychedelic…
View article: 5-Hydroxytryptamine receptors in GtoPdb v.2025.3
5-Hydroxytryptamine receptors in GtoPdb v.2025.3 Open
5-HT receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on 5-HT receptors [201] and subsequently revised [183]) are, with the exception of the ionotropic 5-HT3 class, GPCRs where the endogenous agonist is 5-hydroxytryptamine. …
View article: Differential effects of sodium on agonist-induced conformational transitions and signaling at μ and κ opioid receptors
Differential effects of sodium on agonist-induced conformational transitions and signaling at μ and κ opioid receptors Open
Sodium ions are classically conceptualized as negative allosteric modulators for G protein coupled receptors (GPCRs), although there have been reports of either positive allosteric modulation or no effect of sodium on GPCR function. Here w…
View article: Making Sense of Psychedelics in the CNS
Making Sense of Psychedelics in the CNS Open
For centuries, ancient lineages have consumed psychedelic compounds from natural sources. In the modern era, scientists have since harnessed the power of computational tools, cellular assays, and behavioral metrics to study how these compo…
View article: Intracellular GPCR modulators enable precision pharmacology
Intracellular GPCR modulators enable precision pharmacology Open
G-protein-coupled receptors (GPCRs) have proven to be the most successful target class for drug discovery but their complicated signal transduction pathways cause difficulties for drug development. Recently, ligands have been identified th…
View article: 5-Hydroxytryptamine receptors in GtoPdb v.2025.1
5-Hydroxytryptamine receptors in GtoPdb v.2025.1 Open
5-HT receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on 5-HT receptors [200] and subsequently revised [182]) are, with the exception of the ionotropic 5-HT3 class, GPCRs where the endogenous agonist is 5-hydroxytryptamine. …
View article: <i>De novo</i> design of miniprotein agonists and antagonists targeting G protein-coupled receptors
<i>De novo</i> design of miniprotein agonists and antagonists targeting G protein-coupled receptors Open
G protein-coupled receptors (GPCRs) play key roles in physiology and are central targets for drug discovery and development, yet the design of protein agonists and antagonists has been challenging as GPCRs are integral membrane proteins an…
View article: The structural diversity of psychedelic drug actions revealed
The structural diversity of psychedelic drug actions revealed Open
There is currently a resurgence in exploring the utility of classical psychedelics to treat depression, addiction, anxiety disorders, cluster headaches, and many other neuropsychiatric disorders. A biological target of these compounds, and…
View article: A proximity proteomics pipeline with improved reproducibility and throughput
A proximity proteomics pipeline with improved reproducibility and throughput Open
Proximity labeling (PL) via biotinylation coupled with mass spectrometry (MS) captures spatial proteomes in cells. Large-scale processing requires a workflow minimizing hands-on time and enhancing quantitative reproducibility. We introduce…
View article: Structures of the σ2 receptor enable docking for bioactive ligand discovery
Structures of the σ2 receptor enable docking for bioactive ligand discovery Open
The σ2 receptor has attracted intense interest in cancer imaging1, psychiatric disease2, neuropathic pain3–5 and other areas of biology6,7. Here we determined the crystal structure of this receptor in complex with the clinical candidate ro…