Structural Insights into Molecular Recognition and Receptor Activation in Chemokine–Chemokine Receptor Complexes

L Urvas, E Kellenberger - Journal of Medicinal Chemistry, 2023 - ACS Publications
The chemokine system is a key player in the functioning of the immune system and a sought-
after target for drug candidates. The number of experimental structures of chemokines in …

Structural basis of GPCR coupling to distinct signal transducers: implications for biased signaling

M Seyedabadi, M Gharghabi, EV Gurevich… - Trends in biochemical …, 2022 - cell.com
Three classes of G-protein-coupled receptor (GPCR) partners–G proteins, GPCR kinases,
and arrestins–preferentially bind active GPCRs. Our analysis suggests that the structures of …

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 …

Structural insights into CXCR4 modulation and oligomerization

K Saotome, LL McGoldrick, JH Ho, TF Ramlall… - Nature Structural & …, 2024 - nature.com
Activation of the chemokine receptor CXCR4 by its chemokine ligand CXCL12 regulates
diverse cellular processes. Previously reported crystal structures of CXCR4 revealed the …

Biased allosteric activation of ketone body receptor HCAR2 suppresses inflammation

C Zhao, H Wang, Y Liu, L Cheng, B Wang, X Tian, H Fu… - Molecular Cell, 2023 - cell.com
Summary Hydroxycarboxylic acid receptor 2 (HCAR2), modulated by endogenous ketone
body β-hydroxybutyrate and exogenous niacin, is a promising therapeutic target for …

Mechanism of activation and biased signaling in complement receptor C5aR1

Y Feng, C Zhao, Y Deng, H Wang, L Ma, S Liu, X Tian… - Cell Research, 2023 - nature.com
The complement system plays an important role in the innate immune response to invading
pathogens. The complement fragment C5a is one of its important effector components and …

Revealing the signaling of complement receptors C3aR and C5aR1 by anaphylatoxins

Y Wang, W Liu, Y Xu, X He, Q Yuan, P Luo… - Nature Chemical …, 2023 - nature.com
The complement receptors C3aR and C5aR1, whose signaling is selectively activated by
anaphylatoxins C3a and C5a, are important regulators of both innate and adaptive immune …

Prospect of acromegaly therapy: molecular mechanism of clinical drugs octreotide and paltusotine

J Zhao, H Fu, J Yu, W Hong, X Tian, J Qi, S Sun… - Nature …, 2023 - nature.com
Abstract Somatostatin receptor 2 (SSTR2) is highly expressed in neuroendocrine tumors
and represents as a therapeutic target. Several peptide analogs mimicking the endogenous …

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 …

Control of Gαq signaling dynamics and GPCR cross-talk by GRKs

G Xiang, A Acosta-Ruiz, A Radoux-Mergault… - Science …, 2022 - science.org
Numerous processes contribute to the regulation of G protein–coupled receptors (GPCRs),
but relatively little is known about rapid mechanisms that control signaling on the seconds …