Molecular basis of opioid receptor signaling

T Che, BL Roth - Cell, 2023 - cell.com
Opioids are used for pain management despite the side effects that contribute to the opioid
crisis. The pursuit of non-addictive opioid analgesics remains unattained due to the …

[HTML][HTML] The neuroimmune response during stress: A physiological perspective

H Haykin, A Rolls - Immunity, 2021 - cell.com
Stress is an essential adaptive response that enables the organism to cope with challenges
and restore homeostasis. Different stressors require distinctive corrective responses in …

[HTML][HTML] LGR5 expressing skin fibroblasts define a major cellular hub perturbed in scleroderma

C Gur, SY Wang, F Sheban, M Zada, B Li, F Kharouf… - Cell, 2022 - cell.com
Systemic sclerosis (scleroderma, SSc) is an incurable autoimmune disease with high
morbidity and mortality rates. Here, we conducted a population-scale single-cell genomic …

[HTML][HTML] GPCR kinase knockout cells reveal the impact of individual GRKs on arrestin binding and GPCR regulation

J Drube, RS Haider, ESF Matthees, M Reichel… - Nature …, 2022 - nature.com
G protein-coupled receptors (GPCRs) activate G proteins and undergo a complex regulation
by interaction with GPCR kinases (GRKs) and the formation of receptor–arrestin complexes …

[HTML][HTML] How Carvedilol activates β2-adrenoceptors

T Benkel, M Zimmermann, J Zeiner, S Bravo… - Nature …, 2022 - nature.com
Carvedilol is among the most effective β-blockers for improving survival after myocardial
infarction. Yet the mechanisms by which carvedilol achieves this superior clinical profile are …

Structures of atypical chemokine receptor 3 reveal the basis for its promiscuity and signaling bias

YC Yen, CT Schafer, M Gustavsson, SA Eberle… - Science …, 2022 - science.org
Both CXC chemokine receptor 4 (CXCR4) and atypical chemokine receptor 3 (ACKR3) are
activated by the chemokine CXCL12 yet evoke distinct cellular responses. CXCR4 is a …

Community guidelines for GPCR ligand bias: IUPHAR review 32

P Kolb, T Kenakin, SPH Alexander… - British journal of …, 2022 - Wiley Online Library
GPCRs modulate a plethora of physiological processes and mediate the effects of one‐third
of FDA‐approved drugs. Depending on which ligand activates a receptor, it can engage …

Clinical potential of adrenomedullin signaling in the cardiovascular system

L Bálint, NP Nelson-Maney, Y Tian, SD Serafin… - Circulation …, 2023 - Am Heart Assoc
Numerous clinical studies have revealed the utility of circulating AM (adrenomedullin) or MR-
proAM (mid-regional proAM 45-92) as an effective prognostic and diagnostic biomarker for a …

Pharmacological characterization and radiolabeling of VUF15485, a high-affinity small-molecule agonist for the atypical chemokine receptor ACKR3

AM Zarca, I Adlere, CP Viciano, M Arimont-Segura… - Molecular …, 2024 - ASPET
Atypical chemokine receptor 3 (ACKR3), formerly referred to as CXCR7, is considered to be
an interesting drug target. In this study, we report on the synthesis, pharmacological …

The CXCL12/CXCR4/ACKR3 axis in the tumor microenvironment: signaling, crosstalk, and therapeutic targeting

MJ Smit, G Schlecht-Louf, M Neves… - Annual review of …, 2021 - annualreviews.org
Elevated expression of the chemokine receptors CXCR4 and ACKR3 and of their cognate
ligand CXCL12 is detected in a wide range of tumors and the tumor microenvironment …