[HTML][HTML] New insights into GPCR coupling and dimerisation from cryo-EM structures
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 …
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 …
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 …
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
Photoactivatable neuropeptides offer a robust stimulus–response relationship that can drive
mechanistic studies into the physiological mechanisms of neuropeptidergic transmission …
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 …
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
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 …
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 …
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 …
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
Ticks are blood-feeding arthropods that require heme for their successful reproduction.
During feeding they also acquire pathogens that are subsequently transmitted to humans …
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 …
physiological functions. Some GPCRs have their activity affected by the presence of …