New insights into the structure and function of class B1 GPCRs

BP Cary, X Zhang, J Cao, RM Johnson… - Endocrine …, 2023 - academic.oup.com
G protein–coupled receptors (GPCRs) are the largest family of cell surface receptors. Class
B1 GPCRs constitute a subfamily of 15 receptors that characteristically contain large …

[HTML][HTML] New insights into GPCR coupling and dimerisation from cryo-EM structures

A Gusach, J García-Nafría, CG Tate - Current Opinion in Structural Biology, 2023 - Elsevier
Over the past three years (2020–2022) more structures of GPCRs have been determined
than in the previous twenty years (2000–2019), primarily of GPCR complexes that are large …

Molecular recognition of morphine and fentanyl by the human μ-opioid receptor

Y Zhuang, Y Wang, B He, X He, XE Zhou, S Guo… - Cell, 2022 - cell.com
Morphine and fentanyl are among the most used opioid drugs that confer analgesia and
unwanted side effects through both G protein and arrestin signaling pathways of μ-opioid …

Structures of the entire human opioid receptor family

Y Wang, Y Zhuang, JF DiBerto, XE Zhou, GP Schmitz… - Cell, 2023 - cell.com
Opioids are effective analgesics, but their use is beset by serious side effects, including
addiction and respiratory depression, which contribute to the ongoing opioid crisis. The …

Autoregulation of GPCR signalling through the third intracellular loop

F Sadler, N Ma, M Ritt, Y Sharma, N Vaidehi… - Nature, 2023 - nature.com
The third intracellular loop (ICL3) of the G protein-coupled receptor (GPCR) fold is important
for the signal transduction process downstream of receptor activation,–. Despite this, the lack …

VMHvllCckar cells dynamically control female sexual behaviors over the reproductive cycle

L Yin, K Hashikawa, Y Hashikawa, T Osakada… - Neuron, 2022 - cell.com
Sexual behavior is fundamental for the survival of mammalian species and thus supported
by dedicated neural substrates. The ventrolateral part of ventromedial hypothalamus …

GPCRome-wide analysis of G-protein-coupling diversity using a computational biology approach

M Matic, P Miglionico, M Tatsumi, A Inoue… - Nature …, 2023 - nature.com
GPCRs are master regulators of cell signaling by transducing extracellular stimuli into the
cell via selective coupling to intracellular G-proteins. Here we present a computational …

A tool kit of highly selective and sensitive genetically encoded neuropeptide sensors

H Wang, T Qian, Y Zhao, Y Zhuo, C Wu, T Osakada… - Science, 2023 - science.org
Neuropeptides are key signaling molecules in the endocrine and nervous systems that
regulate many critical physiological processes. Understanding the functions of …

Specific binding of GPR174 by endogenous lysophosphatidylserine leads to high constitutive Gs signaling

Y Nie, Z Qiu, S Chen, Z Chen, X Song, Y Ma… - Nature …, 2023 - nature.com
Many orphan G protein-coupled receptors (GPCRs) remain understudied because their
endogenous ligands are unknown. Here, we show that a group of class A/rhodopsin-like …

Structural insights into ligand recognition and activation of the medium-chain fatty acid-sensing receptor GPR84

H Liu, Q Zhang, X He, M Jiang, S Wang, X Yan… - nature …, 2023 - nature.com
GPR84 is an orphan class AG protein-coupled receptor (GPCR) that is predominantly
expressed in immune cells and plays important roles in inflammation, fibrosis, and …