ArticleCell2022
State-selective modulation of heterotrimeric Gαs signaling with macrocyclic peptides.
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In one paragraph
Article in Cell, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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30citing papers in PubMed
–field-weighted citation impact
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
30 citing papers in PubMed.
- Inhibitory probes for spatiotemporal analysis of GαNature chemical biology · 2026Article
- Advances in Cyclic Peptides Targeting G Protein-Coupled Receptors.Chembiochem : a European journal of chemical biology · 2026Review
- Small-molecule modulation of β-arrestins.Nature · 2026Article
- De novo GNAS-Gsα variant (p.Thr55Ala) with constitutive gain-of-function effects on AVPR2 and PTH1R signalings.Journal of human genetics · 2026Article
- Phage Display Driven Identification and Computational Mapping of Macrocyclic Peptides Targeting RhoA G17V.Biochemistry · 2026Article
- Direct Selection of Functional De Novo Macrocycles for Activation of On-Cellulo Insulin Receptor.Angewandte Chemie (International ed. in English) · 2026Article
- Macrophage Gsα promotes NLRP3 stability and its intervention attenuates abdominal aortic aneurysm in male mice.Nature communications · 2026Article
- Fibrous dysplasia/McCune-Albright syndrome: state-of-the-art advances, pathogenesis, and basic/translational research.Orphanet journal of rare diseases · 2025Review
- Cyclic peptide inhibitors function as molecular glues to stabilize Gq/11 heterotrimers.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Contract to kill: GNAS mutation.Molecular cancer · 2025Review
- Discovering covalent cyclic peptide inhibitors of peptidyl arginine deiminase 4 (PADI4) using mRNA-display with a genetically encoded electrophilic warhead.Communications chemistry · 2024Article
- Optimized Construction of a Yeast SICLOPPS Library for UnbiasedBiochemistry · 2024Article
- Tackling Undruggable Targets with Designer Peptidomimetics and Synthetic Biologics.Chemical reviews · 2024Review
- Selection of Nucleotide-Encoded Mass Libraries of Macrocyclic Peptides for Inaccessible Drug Targets.Chemical reviews · 2024Review
- Molecular and Clinicopathologic Impact of GNAS Variants Across Solid Tumors.Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2024Article
- Going Rogue: Mechanisms, Regulation, and Roles of Mutationally Activated GMolecular pharmacology · 2024Review
- Stabilization of interdomain closure by a G protein inhibitor.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- A neurodevelopmental disorder mutation locks G proteins in the transitory pre-activated state.Nature communications · 2024Article
- Chemoproteomics Identifies State-Dependent and Proteoform-Selective Caspase-2 Inhibitors.Journal of the American Chemical Society · 2024Article
- Gsα Regulates Macrophage Foam Cell Formation During Atherosclerosis.Circulation research · 2024Article
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Authors and funding
10 authors.
Shizhong A DaiDepartment of Cellular and Molecular Pharmacology, University of California, San Francisco, San Francisco, CA 94158, USA; Howard Hughes Medical Institute, Chevy Chase, MD 20815, USA.
Qi HuDepartment of Cellular and Molecular Pharmacology, University of California, San Francisco, San Francisco, CA 94158, USA; Howard Hughes Medical Institute, Chevy Chase, MD 20815, USA.
Rong GaoDepartment of Chemistry, Graduate School of Science, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Emily E BlytheDepartment of Cellular and Molecular Pharmacology, University of California, San Francisco, San Francisco, CA 94158, USA; Department of Psychiatry, University of California, San Francisco, San Francisco, CA 94158, USA.
Kouki K TouharaDepartment of Physiology, University of California, San Francisco, San Francisco, CA 94158, USA.
Hayden PeacockDepartment of Chemistry, Graduate School of Science, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Ziyang ZhangDepartment of Cellular and Molecular Pharmacology, University of California, San Francisco, San Francisco, CA 94158, USA; Howard Hughes Medical Institute, Chevy Chase, MD 20815, USA.
Mark von ZastrowDepartment of Cellular and Molecular Pharmacology, University of California, San Francisco, San Francisco, CA 94158, USA; Department of Psychiatry, University of California, San Francisco, San Francisco, CA 94158, USA.
Hiroaki SugaDepartment of Chemistry, Graduate School of Science, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan. Electronic address: hsuga@chem.s.u-tokyo.ac.jp.
Kevan M ShokatDepartment of Cellular and Molecular Pharmacology, University of California, San Francisco, San Francisco, CA 94158, USA; Howard Hughes Medical Institute, Chevy Chase, MD 20815, USA. Electronic address: kevan.shokat@ucsf.edu.
Funding
PROTEINS REGULATING ENDOCYTOSIS OF OPIOID RECEPTORSR01DA012864 · NIDA · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI Mark E Von Zastrow · 2000 to 2026
$7.9MMembrane Trafficking of Opioid and Adrenergic ReceptorsR01DA010711 · NIDA · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VONZASTROW, MARK E · 2014 to 2023
$4.6MMEMBRANE TRAFFICKING OF OPIOID RECEPTORSR37DA010711 · NIDA · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VONZASTROW, MARK E · 2004 to 2013
$3.1MImproving the efficacy of mTOR inhibitionR01CA221969 · NCI · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI FAN, QI WEN, SHOKAT, KEVAN M. · 2018 to 2022
$2.9MInhibitors of the G protein GNAS which drives pancreatic tumorigenesisR01CA244550 · NCI · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI SHOKAT, KEVAN M. · 2020 to 2024
$2.0MGPR88 localization to primary cilia and its impact on striatal cAMP signalingR01MH120212 · NIMH · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VONZASTROW, MARK E · 2019 to 2023
$2.0MMEMBRANE TRAFFICKING OF OPIOID RECEPTORSR29DA010711 · NIDA · UNIVERSITY OF CALIFORNIA SAN FRANCISCO · PI VON ZASTROW, MARK E. · 1997 to 2003
$413kEffects of GPCR trafficking on the spatiotemporal control of signalingF32CA260118 · NCI · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI BLYTHE, EMILY ELIZABETH · 2021 to 2023
$189kHoward Hughes Medical InstituteNCI NIH HHS F32 CA260118NCI NIH HHS R01 CA221969NCI NIH HHS R01 CA244550NIDA NIH HHS R01 DA010711NIDA NIH HHS R01 DA012864NIDA NIH HHS R29 DA010711NIDA NIH HHS R37 DA010711NIMH NIH HHS R01 MH120212
Abstract
The G protein-coupled receptor cascade leading to production of the second messenger cAMP is replete with pharmacologically targetable proteins, with the exception of the Gα subunit, Gαs. GTPases remain largely undruggable given the difficulty of displacing high-affinity guanine nucleotides and the lack of other drug binding sites. We explored a chemical library of 10
Indexed as
PeptidesReceptors, G-Protein-CoupledGTP PhosphohydrolasesGuanine NucleotidesNucleotidesPeptides, CyclicGTP PhosphohydrolasesGuanine NucleotidesNucleotidesPeptidesPeptides, CyclicReceptors, G-Protein-CoupledcAMPchemical probecyclic peptidedrug discoveryGIRKG proteinGTPaseGαsinhibitorprotein crystal structure
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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.