Reversible, allosteric small-molecule inhibitors of regulator of G protein signaling proteins (Q34128004)

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:20571077%20AND%20SRC:MED&resulttype=core&format=json

6 February 2020

title

Reversible, allosteric small-molecule inhibitors of regulator of G protein signaling proteins (English)

1 reference

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6 February 2020

1 reference

3

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6 February 2020

Stephen M. Husbands

6

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6 February 2020

Richard Neubig

7

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6 February 2020

author name string

Levi L Blazer

1

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6 February 2020

David L Roman

2

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6 February 2020

Martha J Larsen

4

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6 February 2020

Benjamin M Greedy

5

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6 February 2020

publication date

22 June 2010

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6 February 2020

published in

Molecular Pharmacology

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6 February 2020

volume

78

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6 February 2020

issue

3

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6 February 2020

page(s)

524-533

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RGS inhibition at G(alpha)i2 selectively potentiates 5-HT1A-mediated antidepressant effects.

6 February 2020

cites work

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Allosteric inhibition of the regulator of G protein signaling-Galpha protein-protein interaction by CCG-4986

5 July 2018

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Differential scanning fluorimetry as secondary screening platform for small molecule inhibitors of Bcl-XL.

5 July 2018

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Irreversible pan-ErbB tyrosine kinase inhibitors and breast cancer: current status and future directions.

5 July 2018

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The road less traveled: modulating signal transduction enzymes by inhibiting their protein-protein interactions

5 July 2018

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Polyplexed flow cytometry protein interaction assay: a novel high-throughput screening paradigm for RGS protein inhibitors

5 July 2018

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A covalent peptide inhibitor of RGS4 identified in a focused one-bead, one compound library screen

5 July 2018

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From protein-protein interaction to therapy response: molecular imaging of heat shock proteins

5 July 2018

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RGS9-2: probing an intracellular modulator of behavior as a drug target

5 July 2018

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In search of small molecules blocking interactions between HIV proteins and intracellular cofactors

5 July 2018

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The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist

5 July 2018

1 reference

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Crystal structure of opsin in its G-protein-interacting conformation

5 July 2018

1 reference

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Small molecule protein-protein interaction inhibitors as CNS therapeutic agents: current progress and future hurdles.

5 July 2018

1 reference

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Small-molecule inhibitors of protein-protein interactions

5 July 2018

1 reference

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Novel peptide ligands of RGS4 from a focused one-bead, one-compound library

5 July 2018

1 reference

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Structure of a beta1-adrenergic G-protein-coupled receptor

5 July 2018

1 reference

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Identification of peptides that inhibit regulator of G protein signaling 4 function

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Structural determination of estrogen-related receptor gamma in the presence of phenol derivative compounds

5 July 2018

1 reference

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High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Crystal structure of the human beta2 adrenergic G-protein-coupled receptor

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

The RGS protein inhibitor CCG-4986 is a covalent modifier of the RGS4 Galpha-interaction face

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Identification of small-molecule inhibitors of RGS4 using a high-throughput flow cytometry protein interaction assay

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Pleiotropic phenotype of a genomic knock-in of an RGS-insensitive G184S Gnai2 allele

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Measurement of heterotrimeric G-protein and regulators of G-protein signaling interactions by time-resolved fluorescence resonance energy transfer.

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

In vivo interaction between RGS4 and calmodulin visualized with FRET techniques: possible involvement of lipid raft

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Thermodynamic stability of carbonic anhydrase: measurements of binding affinity and stoichiometry using ThermoFluor.

5 July 2018

1 reference

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Multi-tasking RGS proteins in the heart: the next therapeutic target?

5 July 2018

1 reference

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Regulators of G protein signaling & drugs of abuse.

5 July 2018

1 reference

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Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells.

5 July 2018

1 reference

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Phosphatidylinositol 3,4,5-trisphosphate and Ca2+/calmodulin competitively bind to the regulators of G-protein-signalling (RGS) domain of RGS4 and reciprocally regulate its action

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Quantitative real-time polymerase chain reaction measurement of regulators of G-protein signaling mRNA levels in mouse tissues

5 July 2018

1 reference

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Evaluation of fluorescence-based thermal shift assays for hit identification in drug discovery

5 July 2018

1 reference

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Small-molecule inhibitors of protein-protein interactions: progressing towards the dream

5 July 2018

1 reference

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Modulation of protein-protein interactions with small organic molecules

5 July 2018

1 reference

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Binding of small molecules to an adaptive protein-protein interface

5 July 2018

1 reference

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In situ assembly of enzyme inhibitors using extended tethering

5 July 2018

1 reference

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Small molecule antagonists of proteins

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Cellular regulation of RGS proteins: modulators and integrators of G protein signaling

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Regulators of G-protein signalling as new central nervous system drug targets.

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Regulator of G protein signaling proteins: novel multifunctional drug targets

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Site-directed ligand discovery

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Ca2+/Calmodulin reverses phosphatidylinositol 3,4, 5-trisphosphate-dependent inhibition of regulators of G protein-signaling GTPase-activating protein activity

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Gastric acid secretion: activation and inhibition.

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Isolation of two proteins with high affinity for guanine nucleotides from membranes of bovine brain.

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Action of opiates on gastrointestinal function

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Application of high-throughput isothermal denaturation to assess protein stability and screen for ligands

5 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors.

28 October 2018

1 reference

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Structural requirements of 2',4',6'-tris(methoxymethoxy) chalcone derivatives for anti-inflammatory activity: the importance of a 2'-hydroxy moiety

28 October 2018

1 reference

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Resistance to diet-induced obesity and improved insulin sensitivity in mice with a regulator of G protein signaling-insensitive G184S Gnai2 allele.

28 October 2018

1 reference

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A high-throughput screen for aggregation-based inhibition in a large compound library

28 October 2018

1 reference

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Mechanism of action and structural requirements of constrained peptide inhibitors of RGS proteins

28 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Up-regulation of regulator of G protein signaling 4 expression in a model of neuropathic pain and insensitivity to morphine

28 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Expression of G-protein alpha subunits in Escherichia coli.

28 October 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=2939488

Rapid kinetics of regulator of G-protein signaling (RGS)-mediated Galphai and Galphao deactivation. Galpha specificity of RGS4 AND RGS7

28 October 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/20571077

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

The GTPase-activating protein RGS4 stabilizes the transition state for nucleotide hydrolysis

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/20571077

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

A point mutation in Galphao and Galphai1 blocks interaction with regulator of G protein signaling proteins

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/20571077

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1124/MOL.110.065128

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:20571077%20AND%20SRC:MED&resulttype=core&format=json

6 February 2020

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:20571077%20AND%20SRC:MED&resulttype=core&format=json

6 February 2020

PubMed publication ID

20571077

1 reference