International Union of Basic and Clinical Pharmacology. XCV. Recent advances in the understanding of the pharmacology and biological roles of relaxin family …
ML Halls, RAD Bathgate, SW Sutton… - Pharmacological …, 2015 - ASPET
Relaxin, insulin-like peptide 3 (INSL3), relaxin-3, and INSL5 are the cognate ligands for the
relaxin family peptide (RXFP) receptors 1–4, respectively. RXFP1 activates pleiotropic …
relaxin family peptide (RXFP) receptors 1–4, respectively. RXFP1 activates pleiotropic …
β-arrestin signalling and bias in hormone-responsive GPCRs
G protein-coupled receptors (GPCRs) play crucial roles in the ability of target organs to
respond to hormonal cues. GPCRs' activation mechanisms have long been considered as a …
respond to hormonal cues. GPCRs' activation mechanisms have long been considered as a …
[HTML][HTML] A single-chain derivative of the relaxin hormone is a functionally selective agonist of the G protein-coupled receptor, RXFP1
Human gene-2 relaxin (H2 relaxin) is a pleiotropic hormone with powerful vasodilatory and
anti-fibrotic properties which has led to its clinical evaluation and provisional FDA approval …
anti-fibrotic properties which has led to its clinical evaluation and provisional FDA approval …
[HTML][HTML] ML290 is a biased allosteric agonist at the relaxin receptor RXFP1
Activation of the relaxin receptor RXFP1 has been associated with improved survival in
acute heart failure. ML290 is a small molecule RXFP1 agonist with simple structure, long …
acute heart failure. ML290 is a small molecule RXFP1 agonist with simple structure, long …
Development of a single-chain peptide agonist of the relaxin-3 receptor using hydrocarbon stapling
K Hojo, MA Hossain, J Tailhades… - Journal of medicinal …, 2016 - ACS Publications
Structure–activity studies of the insulin superfamily member, relaxin-3, have shown that its G
protein-coupled receptor (RXFP3) binding site is contained within its central B-chain α-helix …
protein-coupled receptor (RXFP3) binding site is contained within its central B-chain α-helix …
Mechanisms of biased agonism by Gαi/o-biased stapled peptide agonists of the relaxin-3 receptor
T Jayakody, A Inoue, S Kannan, G Nakamura… - Science …, 2024 - science.org
The neuropeptide relaxin-3 is composed of an A chain and a B chain held together by
disulfide bonds, and it modulates functions such as anxiety and food intake by binding to …
disulfide bonds, and it modulates functions such as anxiety and food intake by binding to …
Central relaxin-3 receptor (RXFP3) activation increases ERK phosphorylation in septal cholinergic neurons and impairs spatial working memory
H Albert-Gascó, Á García-Avilés, S Moustafa… - Brain Structure and …, 2017 - Springer
The medial septum/diagonal band (MS/DB) is a relay region connecting the hypothalamus
and brainstem with the hippocampus, and both the MS/DB and dorsal/ventral hippocampus …
and brainstem with the hippocampus, and both the MS/DB and dorsal/ventral hippocampus …
Development of a synthetic relaxin-3/INSL5 chimeric peptide ligand for NanoBiT complementation binding assays
H Wu, BL Hoare, TNG Handley, MA Hossain… - Biochemical …, 2024 - Elsevier
INSL5 and relaxin-3 are relaxin family peptides with important roles in gut and brain
function, respectively. They mediate their actions through the class A GPCRs RXFP4 and …
function, respectively. They mediate their actions through the class A GPCRs RXFP4 and …
Indole-containing amidinohydrazones as nonpeptide, dual RXFP3/4 agonists: synthesis, structure–activity relationship, and molecular modeling studies
The central relaxin-3/RXFP3 system plays important roles in stress responses, feeding, and
motivation for reward. However, exploration of its therapeutic applications has been …
motivation for reward. However, exploration of its therapeutic applications has been …
Central relaxin-3 receptor (RXFP3) activation impairs social recognition and modulates ERK-phosphorylation in specific GABAergic amygdala neurons
H Albert-Gasco, S Sanchez-Sarasua, S Ma… - Brain Structure and …, 2019 - Springer
In mammals, the extended amygdala is a neural hub for social and emotional information
processing. In the rat, the extended amygdala receives inhibitory GABAergic projections …
processing. In the rat, the extended amygdala receives inhibitory GABAergic projections …