[HTML][HTML] New insights into GPCR coupling and dimerisation from cryo-EM structures

A Gusach, J García-Nafría, CG Tate - Current Opinion in Structural Biology, 2023 - Elsevier
Over the past three years (2020–2022) more structures of GPCRs have been determined
than in the previous twenty years (2000–2019), primarily of GPCR complexes that are large …

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 …

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 …

A biomimetic C-terminal extension strategy for photocaging amidated neuropeptides

AE Layden, X Ma, CA Johnson, XJ He… - Journal of the …, 2023 - ACS Publications
Photoactivatable neuropeptides offer a robust stimulus–response relationship that can drive
mechanistic studies into the physiological mechanisms of neuropeptidergic transmission …

Structural basis for the activation and ligand recognition of the human oxytocin receptor

Y Waltenspühl, J Ehrenmann, S Vacca, C Thom… - Nature …, 2022 - nature.com
The small cyclic neuropeptide hormone oxytocin (OT) and its cognate receptor play a central
role in the regulation of social behaviour and sexual reproduction. Here we report the single …

Neurokinin-1 receptor (NK-1R) antagonists as a new strategy to overcome cancer resistance

M García-Aranda, T Téllez, L McKenna, M Redondo - Cancers, 2022 - mdpi.com
Simple Summary Improving the response, quality of life and survival of oncologic patients
through the design and application of the most appropriate treatment for each case is a great …

The repurposing of non-peptide neurokinin-1 receptor antagonists as antitumor drugs: An urgent challenge for aprepitant

R Coveñas, FD Rodríguez, P Robinson… - International journal of …, 2023 - mdpi.com
The substance P (SP)/neurokinin-1 receptor (NK-1R) system is involved in cancer
progression. NK-1R, activated by SP, promotes tumor cell proliferation and migration …

Peptidergic systems and cancer: Focus on tachykinin and calcitonin/calcitonin gene-related peptide families

ML Sánchez, FD Rodríguez, R Coveñas - Cancers, 2023 - mdpi.com
Simple Summary Neurokinins A and B, adrenomedullin, adrenomedullin 2, amylin, and
calcitonin gene-related peptide are essential in different tumors. These peptides are …

A fluorescently-tagged tick kinin neuropeptide triggers peristalsis and labels tick midgut muscles

JR Hernandez, C **ong, PV Pietrantonio - Scientific Reports, 2024 - nature.com
Ticks are blood-feeding arthropods that require heme for their successful reproduction.
During feeding they also acquire pathogens that are subsequently transmitted to humans …

Interactions of cholesterol molecules with GPCRs in different states: A comparative analysis of GPCRs' structures

CJ Moreau, G Audic, L Lemel… - … et Biophysica Acta (BBA …, 2023 - Elsevier
GPCRs form a very large family of transmembrane proteins involved in a wide range of
physiological functions. Some GPCRs have their activity affected by the presence of …