Unlabelled: The human relaxin peptide family consists of seven cystine-rich peptides, four of which are known to signal through relaxin family peptide receptors, RXFP1-4. As these peptides play a vital role physiologically and in various diseases, they are of considerable importance for drug discovery and development. Detailed structure-activity relationship (SAR) studies towards understanding the role of important residues in each of these peptides have been reported over the years and utilized for the design of antagonists and minimized agonist variants. This review summarizes the current knowledge of the SAR of human relaxin 2 (H2 relaxin), human relaxin 3 (H3 relaxin), human insulin-like peptide 3 (INSL3) and human insulin-like peptide 5 (INSL5).
Linked Articles: This article is part of a themed section on Recent Progress in the Understanding of Relaxin Family Peptides and their Receptors. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v174.10/issuetoc.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5406294 | PMC |
http://dx.doi.org/10.1111/bph.13684 | DOI Listing |
J Reprod Dev
December 2024
Laboratory of Theriogenology, Graduate School of Veterinary Science, Osaka Metropolitan University, Osaka 598-8531, Japan.
The objective of this study was to examine the relationship between the insulin-like peptide 3 (INSL3) receptor (RXFP2) expression levels on spermatozoa and INSL3 concentrations in the seminal plasma of fresh semen from beef bulls with different levels of sperm morphological normality. Ejaculates (n = 44) were collected from 21 yearling Japanese Black beef bulls and categorized into three groups based on the levels of sperm morphological normality: High (normal morphology ≥ 80%; n = 23), Mid (< 80% & ≥ 65%; n = 10) and Low (< 65%; n = 11). Immunofluorescence was used to determine the localization and expression levels of RXFP2 in spermatozoa.
View Article and Find Full Text PDFBiochem Pharmacol
December 2024
Department of Human Anatomy and Cell Science, Winnipeg, MB, Canada; Department of Pathology, University of Manitoba, Rady Faculty of Health Sciences, Max Rady College of Medicine, Winnipeg, MB, Canada; CancerCare Manitoba, Winnipeg, MB, Canada; Children's Hospital Research Institute of Manitoba (CHRIM), Winnipeg, MB, Canada. Electronic address:
Glioblastoma (GB) is the most prevalent and aggressive primary brain tumor with fatal outcome due to a lack of effective treatments. We previously identified C1q-tumor necrosis factor-related protein 8 (CTRP8), a new member of the adiponectin family, as a novel agonist of the relaxin family peptide receptor 1 (RXFP1) and showed that the CTRP8-RXFP1 ligand-receptor system facilitates increased invasiveness and chemoresistance in GB cells. In the present study, we have investigated the role of the CTRP8-RXFP1 signaling axis in glioma progression using an orthotopic mouse model xenografted with human U251 glioma cells stably expressing CTRP8 and RXFP1.
View Article and Find Full Text PDFBiochem Pharmacol
December 2024
Faculty of Health, School of Medicine, Institute for Mental and Physical Health and Clinical Translation (IMPACT), Deakin University, Waurn Ponds, Victoria 3216, Australia.
The relaxin-family peptide 3 receptor (RXFP3) and its native ligand, relaxin-3, are expressed in specific populations of brain neurons, and research on this system has focused on its role in the central nervous system. However, some studies have indicated that relaxin-3 and RXFP3 are also expressed in peripheral organs, including the gut. In this study, we characterised the identity of RXFP3-expressing cells in the gastrointestinal tract, using RXFP3-Cre/tdTomato reporter mice.
View Article and Find Full Text PDFExpert Opin Investig Drugs
December 2024
Cardiology, Liverpool University Hospitals NHS Foundation Trust, Liverpool, UK.
Introduction: Acute failure is a critical condition, encompassed by the sudden or progressive onset of symptoms or signs of congestion. The treatment strategies available are mainly supportive and do not improve mortality or long-term outcomes. Therefore, there is a need for alternative novel treatment strategies.
View Article and Find Full Text PDFMedicine (Baltimore)
November 2024
Department of Emergency, Shenzhen Nanshan People's Hospital, Shenzhen, Guangdong Province, China.
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!