Goods and bads of the endocannabinoid system as a therapeutic target: Lessons learned after 30 years

M Maccarrone, V Di Marzo, J Gertsch, U Grether… - Pharmacological …, 2023 - ASPET
The cannabis derivative marijuana is the most widely used recreational drug in the Western
world and is consumed by an estimated 83 million individuals (∼ 3% of the world …

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 …

The current state of peptide drug discovery: back to the future?

A Henninot, JC Collins, JM Nuss - Journal of medicinal chemistry, 2018 - ACS Publications
Over the past decade, peptide drug discovery has experienced a revival of interest and
scientific momentum, as the pharmaceutical industry has come to appreciate the role that …

Phase-plate cryo-EM structure of a class B GPCR–G-protein complex

YL Liang, M Khoshouei, M Radjainia, Y Zhang… - Nature, 2017 - nature.com
Class B G-protein-coupled receptors are major targets for the treatment of chronic diseases,
such as osteoporosis, diabetes and obesity. Here we report the structure of a full-length …

[HTML][HTML] Psychedelic-inspired drug discovery using an engineered biosensor

C Dong, C Ly, LE Dunlap, MV Vargas, J Sun… - Cell, 2021 - cell.com
Ligands can induce G protein-coupled receptors (GPCRs) to adopt a myriad of
conformations, many of which play critical roles in determining the activation of specific …

Allosteric regulation of IGF2BP1 as a novel strategy for the activation of tumor immune microenvironment

Y Liu, Q Guo, H Yang, XW Zhang, N Feng… - ACS central …, 2022 - ACS Publications
Tumor immune microenvironment (TIME) regulators are promising cancer
immunotherapeutic targets. IGF2BP1, as a crucial N 6-methyladenosine (m6A) reader …

The diverse roles of arrestin scaffolds in G protein–coupled receptor signaling

YK Peterson, LM Luttrell - Pharmacological reviews, 2017 - ASPET
The visual/β-arrestins, a small family of proteins originally described for their role in the
desensitization and intracellular trafficking of G protein–coupled receptors (GPCRs), have …

The physiology, signaling, and pharmacology of dopamine receptors

JM Beaulieu, RR Gainetdinov - Pharmacological reviews, 2011 - ASPET
G protein-coupled dopamine receptors (D1, D2, D3, D4, and D5) mediate all of the
physiological functions of the catecholaminergic neurotransmitter dopamine, ranging from …

How were new medicines discovered?

DC Swinney, J Anthony - Nature reviews Drug discovery, 2011 - nature.com
Preclinical strategies that are used to identify potential drug candidates include target-based
screening, phenotypic screening, modification of natural substances and biologic-based …

Glucagon-like peptide-1 and its class BG protein–coupled receptors: a long march to therapeutic successes

C De Graaf, D Donnelly, D Wootten, J Lau… - Pharmacological …, 2016 - ASPET
The glucagon-like peptide (GLP)-1 receptor (GLP-1R) is a class BG protein–coupled
receptor (GPCR) that mediates the action of GLP-1, a peptide hormone secreted from three …