Structural Understanding of Peptide-Bound G Protein-Coupled Receptors: Peptide–Target Interactions

Y Shi, Y Chen, L Deng, K Du, S Lu… - Journal of Medicinal …, 2023 - ACS Publications
The activation of G protein-coupled receptors (GPCRs) is triggered by ligand binding to their
orthosteric sites, which induces ligand-specific conformational changes. Agonists and …

Neuropeptide substance P: a promising regulator of wound healing in diabetic foot ulcers

J Chen, P Ye, R Gu, H Zhu, W He, X Mu, X Wu… - Biochemical …, 2023 - Elsevier
In the past, neuropeptide substance P (SP) was predominantly recognized as a
neuroinflammatory factor, while its potent healing activity was overlooked. This paper aims …

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 …

The role of G protein conformation in receptor–G protein selectivity

W Jang, S Lu, X Xu, G Wu, NA Lambert - Nature chemical biology, 2023 - nature.com
G protein-coupled receptors (GPCRs) selectively activate at least one of the four families of
heterotrimeric G proteins, but the mechanism of coupling selectivity remains unclear …

Structural basis of antibody inhibition and chemokine activation of the human CC chemokine receptor 8

D Sun, Y Sun, E Janezic, T Zhou, M Johnson… - Nature …, 2023 - nature.com
The CC motif chemokine receptor 8 (CCR8) is a class A G-protein coupled receptor that has
emerged as a promising therapeutic target in cancer. Targeting CCR8 with an antibody has …

Improving resolution and resolvability of single-particle cryoEM structures using Gaussian mixture models

M Chen, MF Schmid, W Chiu - Nature methods, 2024 - nature.com
Cryogenic electron microscopy is widely used in structural biology, but its resolution is often
limited by the dynamics of the macromolecule. Here we developed a refinement protocol …

Structures of human gastrin-releasing peptide receptors bound to antagonist and agonist for cancer and itch therapy

S Peng, Y Zhan, D Zhang, L Ren… - Proceedings of the …, 2023 - National Acad Sciences
Gastrin releasing peptide receptor (GRPR), a member of the bombesin (BBN) G protein-
coupled receptors, is aberrantly overexpressed in several malignant tumors, including those …

Structural insights into neurokinin 3 receptor activation by endogenous and analogue peptide agonists

W Sun, F Yang, H Zhang, Q Yuan, S Ling, Y Wang… - Cell Discovery, 2023 - nature.com
Abstract Neurokinin 3 receptor (NK3R) is a tachykinin receptor essential for the
hypothalamic-pituitary-gonadal axis. The endogenous peptide agonist neurokinin B (NKB) …

Molecular basis for the selective G protein signaling of somatostatin receptors

S Chen, X Teng, S Zheng - Nature Chemical Biology, 2023 - nature.com
G protein-coupled receptors (GPCRs) modulate every aspect of physiological functions
mainly through activating heterotrimeric G proteins. A majority of GPCRs promiscuously …

Structural insights into the activation of somatostatin receptor 2 by cyclic SST analogues

Q Bo, F Yang, Y Li, X Meng, H Zhang, Y Zhou, S Ling… - Cell Discovery, 2022 - nature.com
The endogenous cyclic tetradecapeptide SST14 was reported to stimulate all five
somatostatin receptors (SSTR1–5) for hormone release, neurotransmission, cell growth …