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 …
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 …
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 …
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
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 …
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
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 …
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
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 …
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 …
coupled receptors, is aberrantly overexpressed in several malignant tumors, including those …
Structural insights into neurokinin 3 receptor activation by endogenous and analogue peptide agonists
Abstract Neurokinin 3 receptor (NK3R) is a tachykinin receptor essential for the
hypothalamic-pituitary-gonadal axis. The endogenous peptide agonist neurokinin B (NKB) …
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 …
mainly through activating heterotrimeric G proteins. A majority of GPCRs promiscuously …
Structural insights into the activation of somatostatin receptor 2 by cyclic SST analogues
The endogenous cyclic tetradecapeptide SST14 was reported to stimulate all five
somatostatin receptors (SSTR1–5) for hormone release, neurotransmission, cell growth …
somatostatin receptors (SSTR1–5) for hormone release, neurotransmission, cell growth …