Common and biased signaling pathways of the chemokine receptor CCR7 elicited by its ligands CCL19 and CCL21 in leukocytes

MA Hauser, DF Legler - Journal of Leucocyte Biology, 2016 - academic.oup.com
Chemokines are pivotal regulators of cell migration during continuous immune surveillance,
inflammation, homeostasis, and development. Chemokine binding to their 7-transmembrane …

Structure-based design of a novel third-generation antipsychotic drug lead with potential antidepressant properties

Z Chen, L Fan, H Wang, J Yu, D Lu, J Qi, F Nie… - Nature …, 2022 - nature.com
Partial agonist activity at the dopamine D2 receptor (DRD2) is a key feature of third-
generation antipsychotics (TGAs). However, TGAs also act as antagonists or weak partial …

Omega‐3 PUFA profoundly affect neural, physiological, and behavioural competences–Implications for systemic changes in trophic interactions

M Pilecky, L Závorka, MT Arts, MJ Kainz - Biological Reviews, 2021 - Wiley Online Library
In recent decades, much conceptual thinking in trophic ecology has been guided by theories
of nutrient limitation and the flow of elements, such as carbon and nitrogen, within and …

An online resource for GPCR structure determination and analysis

C Munk, E Mutt, V Isberg, LF Nikolajsen, JM Bibbe… - Nature …, 2019 - nature.com
G-protein-coupled receptors (GPCRs) transduce physiological and sensory stimuli into
appropriate cellular responses and mediate the actions of one-third of drugs. GPCR …

Functional selectivity profiling of the angiotensin II type 1 receptor using pathway-wide BRET signaling sensors

Y Namkung, C LeGouill, S Kumar, Y Cao… - Science …, 2018 - science.org
G protein–coupled receptors (GPCRs) are important therapeutic targets that exhibit
functional selectivity (biased signaling), in which different ligands or receptor variants elicit …

Determination of the melanocortin-4 receptor structure identifies Ca2+ as a cofactor for ligand binding

J Yu, LE Gimenez, CC Hernandez, Y Wu, AH Wein… - Science, 2020 - science.org
The melanocortin-4 receptor (MC4R) is involved in energy homeostasis and is an important
drug target for syndromic obesity. We report the structure of the antagonist SHU9119-bound …

Elucidating the active δ-opioid receptor crystal structure with peptide and small-molecule agonists

T Claff, J Yu, V Blais, N Patel, C Martin, L Wu… - Science …, 2019 - science.org
Selective activation of the δ-opioid receptor (DOP) has great potential for the treatment of
chronic pain, benefitting from ancillary anxiolytic and antidepressant-like effects. Moreover …

Activation mechanism of endothelin ETB receptor by endothelin-1

W Shihoya, T Nishizawa, A Okuta, K Tani, N Dohmae… - Nature, 2016 - nature.com
Abstract Endothelin, a 21-amino-acid peptide, participates in various physiological
processes, such as regulation of vascular tone, humoral homeostasis, neural crest cell …

Unifying family A GPCR theories of activation

BG Tehan, A Bortolato, FE Blaney, MP Weir… - Pharmacology & …, 2014 - Elsevier
Several new pairs of active and inactive GPCR structures have recently been solved
enabling detailed structural insight into the activation process, not only of rhodopsin but now …

The endocannabinoid system as a target in cancer diseases: are we there yet?

E Moreno, M Cavic, A Krivokuca, V Casadó… - Frontiers in …, 2019 - frontiersin.org
The endocannabinoid system (ECS) has been placed in the anti-cancer spotlight in the last
decade. The immense data load published on its dual role in both tumorigenesis and …