Dopamine receptor subtypes, physiology and pharmacology: new ligands and concepts in schizophrenia

JC Martel, S Gatti McArthur - Frontiers in pharmacology, 2020 - frontiersin.org
Dopamine receptors are widely distributed within the brain where they play critical
modulator roles on motor functions, motivation and drive, as well as cognition. The …

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 …

Improved green and red GRAB sensors for monitoring dopaminergic activity in vivo

Y Zhuo, B Luo, X Yi, H Dong, X Miao, J Wan… - Nature …, 2024 - nature.com
Dopamine (DA) plays multiple roles in a wide range of physiological and pathological
processes via a large network of dopaminergic projections. To dissect the spatiotemporal …

Next-generation GRAB sensors for monitoring dopaminergic activity in vivo

F Sun, J Zhou, B Dai, T Qian, J Zeng, X Li, Y Zhuo… - Nature …, 2020 - nature.com
Dopamine (DA) plays a critical role in the brain, and the ability to directly measure
dopaminergic activity is essential for understanding its physiological functions. We therefore …

GPCR activation mechanisms across classes and macro/microscales

AS Hauser, AJ Kooistra, C Munk… - Nature structural & …, 2021 - nature.com
Two-thirds of human hormones and one-third of clinical drugs activate~ 350 G-protein-
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …

A genetically encoded fluorescent sensor enables rapid and specific detection of dopamine in flies, fish, and mice

F Sun, J Zeng, M Jing, J Zhou, J Feng, SF Owen, Y Luo… - Cell, 2018 - cell.com
Dopamine (DA) is a central monoamine neurotransmitter involved in many physiological
and pathological processes. A longstanding yet largely unmet goal is to measure DA …

[HTML][HTML] Structural insights into the human D1 and D2 dopamine receptor signaling complexes

Y Zhuang, P Xu, C Mao, L Wang, B Krumm, XE Zhou… - Cell, 2021 - cell.com
Summary The D1-and D2-dopamine receptors (D1R and D2R), which signal through G s
and G i, respectively, represent the principal stimulatory and inhibitory dopamine receptors …

Structure of the D2 dopamine receptor bound to the atypical antipsychotic drug risperidone

S Wang, T Che, A Levit, BK Shoichet, D Wacker… - Nature, 2018 - nature.com
Dopamine is a neurotransmitter that has been implicated in processes as diverse as reward,
addiction, control of coordinated movement, metabolism and hormonal secretion …

[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 …

A survey of the role of noncovalent sulfur interactions in drug design

BR Beno, KS Yeung, MD Bartberger… - Journal of medicinal …, 2015 - ACS Publications
Electron deficient, bivalent sulfur atoms have two areas of positive electrostatic potential, a
consequence of the low-lying σ* orbitals of the C–S bond that are available for interaction …