ArticleProceedings of the National Academy of Sciences of the United States of America1998
Gsalpha-selective G protein antagonists.
Article in Proceedings of the National Academy of Sciences of the United States of America, 1998. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 68 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
68 citing papers in PubMed, 136 citations in OpenAlex.
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- Imeglimin suppresses glucagon secretion and induces a loss of α cell identity.Cell reports. Medicine · 2025Article
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- Functional crosstalk of sucrose and G protein signaling in maize thermotolerance by modulating osmoregulation system.Protoplasma · 2025Article
- Shigella infection is facilitated by interaction of human enteric α-defensin 5 with colonic epithelial receptor P2Y11.Nature microbiology · 2025Article
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- Progesterone induces meiosis through two obligate co-receptors with PLA2 activity.bioRxiv : the preprint server for biology · 2024Article
- Structural insights into the human P2X1 receptor and ligand interactions.Nature communications · 2024Article
- The bacterial metabolite, lithocholic acid, has antineoplastic effects in pancreatic adenocarcinoma.Cell death discovery · 2024Article
- Gsα Regulates Macrophage Foam Cell Formation During Atherosclerosis.Circulation research · 2024Article
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- A Rare Skeletal Disorder, Fibrous Dysplasia: A Review of Its Pathogenesis and Therapeutic Prospects.International journal of molecular sciences · 2023Review
- Cell death signaling inExperimental biology and medicine (Maywood, N.J.) · 2023Article
- G protein-biased GPR3 signaling ameliorates amyloid pathology in a preclinical Alzheimer's disease mouse model.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Discovery of anti-inflammatory physiological peptides that promote tissue repair by reinforcing epithelial barrier formation.Science advances · 2021Article
- Activation of PTH1R alleviates epididymitis and orchitis through Gq and β-arrestin-1 pathways.Proceedings of the National Academy of Sciences of the United States of America · 2021Article
- Mechanical and chemical activation of GPR68 probed with a genetically encoded fluorescent reporter.Journal of cell science · 2021Article
8 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Suramin acts as a G protein inhibitor because it inhibits the rate-limiting step in activation of the Galpha subunit, i.e., the exchange of GDP for GTP. Here, we have searched for analogues that are selective for Gsalpha. Two compounds have been identified: NF449 (4,4',4",4'"-[carbonyl-bis[imino-5,1,3-benzenetriyl bis-(carbonylimino)]]tetrakis-(benzene-1,3-disulfonate) and NF503 (4, 4'-[carbonylbis[imino-3,1-phenylene-(2, 5-benzimidazolylene)carbonylimino]]bis-benzenesulfonate). These compounds (i) suppress the association rate of guanosine 5'-[gamma-thio]triphosphate ([35S]GTP[gammaS]) binding to Gsalpha-s but not to Gialpha-1, (ii) inhibit stimulation of adenylyl cyclase activity in S49 cyc- membranes (deficient in endogenous Gsalpha) by exogenously added Gsalpha-s, and (iii) block the coupling of beta-adrenergic receptors to Gs with half-maximum effects in the low micromolar range. In contrast to suramin, which is not selective, NF503 and NF449 disrupt the interaction of the A1-adenosine receptor with its cognate G proteins (Gi/Go) at concentrations that are >30-fold higher than those required for uncoupling of beta-adrenergic receptor/Gs tandems; similarly, the angiotensin II type-1 receptor (a prototypical Gq-coupled receptor) is barely affected by the compounds. Thus, NF503 and NF449 fulfill essential criteria for Gsalpha-selective antagonists. The observations demonstrate the feasibility of subtype-selective G protein inhibition.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.