International Union of Basic and Clinical Pharmacology. CX. Classification of receptors for 5-hydroxytryptamine; pharmacology and function

NM Barnes, GP Ahern, C Becamel, J Bockaert… - Pharmacological …, 2021 - ASPET
5-HT receptors expressed throughout the human body are targets for established
therapeutics and various drugs in development. Their diversity of structure and function …

DREADDs for neuroscientists

BL Roth - Neuron, 2016 - cell.com
To understand brain function, it is essential that we discover how cellular signaling specifies
normal and pathological brain function. In this regard, chemogenetic technologies represent …

Structure-based discovery of nonhallucinogenic psychedelic analogs

D Cao, J Yu, H Wang, Z Luo, X Liu, L He, J Qi, L Fan… - Science, 2022 - science.org
Drugs that target the human serotonin 2A receptor (5-HT2AR) are used to treat
neuropsychiatric diseases; however, many have hallucinogenic effects, hampering their use …

Structural insights into the lipid and ligand regulation of serotonin receptors

P Xu, S Huang, H Zhang, C Mao, XE Zhou, X Cheng… - Nature, 2021 - nature.com
Abstract Serotonin, or 5-hydroxytryptamine (5-HT), is an important neurotransmitter, that
activates the largest subtype family of G-protein-coupled receptors. Drugs that target 5 …

ProLIF: a library to encode molecular interactions as fingerprints

C Bouysset, S Fiorucci - Journal of cheminformatics, 2021 - Springer
Interaction fingerprints are vector representations that summarize the three-dimensional
nature of interactions in molecular complexes, typically formed between a protein and a …

[HTML][HTML] Tumor cell-derived exosomes home to their cells of origin and can be used as Trojan horses to deliver cancer drugs

L Qiao, S Hu, K Huang, T Su, Z Li, A Vandergriff… - Theranostics, 2020 - ncbi.nlm.nih.gov
Cancer is the second leading cause of death worldwide and patients are in urgent need of
therapies that can effectively target cancer with minimal off-target side effects. Exosomes are …

Indole-3-lactic acid associated with Bifidobacterium-dominated microbiota significantly decreases inflammation in intestinal epithelial cells

AM Ehrlich, AR Pacheco, BM Henrick, D Taft, G Xu… - BMC microbiology, 2020 - Springer
Background Bifidobacterium longum subsp. infantis (B. infantis) is a commensal bacterium
that colonizes the gastrointestinal tract of breast-fed infants. B. infantis can efficiently utilize …

How ligands illuminate GPCR molecular pharmacology

D Wacker, RC Stevens, BL Roth - Cell, 2017 - cell.com
G protein-coupled receptors (GPCRs), which are modulated by a variety of endogenous and
synthetic ligands, represent the largest family of druggable targets in the human genome …

GPCR dynamics: structures in motion

NR Latorraca, AJ Venkatakrishnan, RO Dror - Chemical reviews, 2017 - ACS Publications
The function of G protein-coupled receptors (GPCRs) which represent the largest class of
both human membrane proteins and drug targets depends critically on their ability to …

[HTML][HTML] Crystal structure of an LSD-bound human serotonin receptor

D Wacker, S Wang, JD McCorvy, RM Betz… - Cell, 2017 - cell.com
The prototypical hallucinogen LSD acts via serotonin receptors, and here we describe the
crystal structure of LSD in complex with the human serotonin receptor 5-HT 2B. The complex …