Ligands for G-protein-coupled receptors (GPCRs) represent approximately 50% of currently marketed drugs. RGS proteins modulate heterotrimeric G proteins and, thus, GPCR signaling, by accelerating the intrinsic GTPase activity of the Gα subunit. Given the prevalence of GPCR targeted therapeutics and the role RGS proteins play in G protein signaling, some RGS proteins are emerging as targets in their own right. One such RGS protein is RGS17. Increased RGS17 expression in some prostate and lung cancers has been demonstrated to support cancer progression, while reduced expression of RGS17 can lead to development of chemotherapeutic resistance in ovarian cancer. High-throughput screening is a powerful tool for lead compound identification, and utilization of high-throughput technologies has led to the discovery of several RGS inhibitors, thus far. As screening technologies advance, the identification of novel lead compounds the subsequent development of targeted therapeutics appears promising.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3865709 | PMC |
| http://dx.doi.org/10.4155/fmc.13.91 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
promotes the progression of gastric cancer through the focal adhesion kinase/phosphatidyl-inositol-3-kinase/protein kinase B pathway and epithelial-mesenchymal transition.
World J Gastroenterol
January 2025
Department of General Surgery, Tianjin Medical University General Hospital, Tianjin Medical University, Tianjin 300052, China.
Background: Regulator of G protein signaling (RGS) proteins participate in tumor formation and metastasis by acting on the α-subunit of heterotrimeric G proteins. The specific effect of RGS, particularly , on the progression of gastric cancer (GC) is not yet clear.
Aim: To explore the role and underlying mechanisms of action of in GC development.
Hydralazine inhibits cysteamine dioxygenase to treat preeclampsia and senesce glioblastoma.
bioRxiv
December 2024
Department of Chemistry, University of Pennsylvania, Philadelphia, PA, USA.
The vasodilator hydralazine (HYZ) has been used clinically for ~ 70 years and remains on the World Health Organization's List of Essential Medicines as a therapy for preeclampsia. Despite its longstanding use and the concomitant progress toward a general understanding of vasodilation, the target and mechanism of HYZ have remained unknown. We show that HYZ selectively targets 2-aminoethanethiol dioxygenase (ADO) by chelating its metal cofactor and alkylating one of its ligands.
View Article and Find Full Text PDFG Protein Regulation by RGS Proteins in the Pathophysiology of Dilated Cardiomyopathy.
Am J Physiol Heart Circ Physiol
January 2025
Department of Physiology & Biophysics, Case Western Reserve University School of Medicine, Cleveland, OH, 44106.
Regulators of G protein signaling (RGS) proteins finetune signaling via heterotrimeric G proteins to maintain physiologic homeostasis in various organ systems of the human body including the brain, kidney, heart, and the vasculature. Impaired regulation of G protein signaling by RGS proteins is implicated in the pathogenesis of several human diseases including various forms of cardiomyopathy such as hypertrophic cardiomyopathy and dilated cardiomyopathy (DCM). Both genetic and non-genetic changes that impinge on G protein signaling in cardiomyocytes are implicated in the etiology of DCM, and there is accumulating evidence that such genetic and non-genetic changes affecting G protein signaling in cell types other than cardiomyocytes could serve as a DCM trigger in humans.
View Article and Find Full Text PDFRegulator of G protein signaling-1 facilitates ovarian cancer development by modulating NF-kB signal pathway.
Sci Rep
January 2025
Department of Obstetrics and Gynecology, Changhai Hospital, Naval Medical University, Shanghai, 200433, China.
Regulator of G protein signaling 1 (RGS1) is known to be highly expressed in various tumors, but its specific effects and regulatory mechanism in ovarian cancer (OC) progression are not well understood. To delve into the tumor biology, a predictive risk model for OC was developed, incorporating RGS1, PRKG2, CD24, and ABCB1, with RGS1 exhibiting the strongest correlation. The model's reliability and validity were confirmed through Kaplan-Meier analysis, receiver operating characteristic (ROC) curve, and principal component analysis (PCA).
View Article and Find Full Text PDFDownregulation of Gldc attenuates myocardial ischemia reperfusion injury in vitro by modulating Akt and NF-κB signalings.
Sci Rep
January 2025
Geriatric Center, Affiliated Hospital of Inner Mongolia Medical University, No.1 Tongdao North Street, Huimin District, Hohhot, 010050, China.
Article Synopsis
- Myocardial ischemia/reperfusion injury (MIRI) is a major complication after myocardial infarction, and the role of mitochondria-related genes in this process is not well understood.
- Researchers utilized specific datasets (GSE67308 and GSE61592) to identify genes associated with MIRI and found glycine decarboxylase (Gldc) to be significantly elevated in MIRI models.
- Experiments showed that reducing Gldc levels improved cell survival and reduced inflammation during hypoxia/reperfusion injury, indicating its potential as a diagnostic and therapeutic target for MIRI.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!