Turning receptors on and off with intracellular pepducins: new insights into G-protein-coupled receptor drug development (Q27024397)

Journal of Biological Chemistry

published in

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volume

287

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1 reference

12787-96

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Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists

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The ATP-gated P2X1 receptor plays a pivotal role in activation of aspirin-treated platelets by thrombin and epinephrine

21 March 2017

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

21 March 2017

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Activation and inhibition of G protein-coupled receptors by cell-penetrating membrane-tethered peptides

21 March 2017

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Molecular tinkering of G protein-coupled receptors: an evolutionary success

21 March 2017

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Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation

21 March 2017

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Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist

21 March 2017

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

21 March 2017

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

21 March 2017

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Crystal structure of the ligand-free G-protein-coupled receptor opsin

21 March 2017

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A Specific Cholesterol Binding Site Is Established by the 2.8 Å Structure of the Human β2-Adrenergic Receptor

21 March 2017

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Crystal structure of rhodopsin: A G protein-coupled receptor

21 March 2017

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The 2.0 A crystal structure of a heterotrimeric G protein

21 March 2017

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Identification of G protein-coupled receptor genes from the human genome sequence

21 March 2017

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Protease-activated receptors in cardiovascular diseases

21 March 2017

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The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints

21 March 2017

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Structural diversity of G protein-coupled receptors and significance for drug discovery

7 April 2017

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The down regulation of neutrophil oxidative metabolism by S100A8 and S100A9: implication of the protease-activated receptor-2

7 April 2017

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Targeting CXCR4 with cell-penetrating pepducins in lymphoma and lymphocytic leukemia

28 September 2017

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Direct interaction between an allosteric agonist pepducin and the chemokine receptor CXCR4.

28 September 2017

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Targeting Protease-Activated Receptor-1 with Cell-Penetrating Pepducins in Lung Cancer

28 September 2017

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Interdicting protease-activated receptor-2-driven inflammation with cell-penetrating pepducins

28 September 2017

1 reference

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Peptide structure stabilization by membrane anchoring and its general applicability to the development of potent cell-permeable inhibitors.

28 September 2017

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Membrane-tethered peptides patterned after the TRP domain (TRPducins) selectively inhibit TRPV1 channel activity.

28 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3339939

Discovery of a CXCR4 agonist pepducin that mobilizes bone marrow hematopoietic cells.

28 September 2017

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Pharmacology, biodistribution, and efficacy of GPCR-based pepducins in disease models.

28 September 2017

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Identification of a metalloprotease-chemokine signaling system in the ovarian cancer microenvironment: implications for antiangiogenic therapy

28 September 2017

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Structural basis of G protein-coupled receptor-G protein interactions

28 September 2017

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G protein subunit Galpha13 binds to integrin alphaIIbbeta3 and mediates integrin "outside-in" signaling

28 September 2017

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Blockade of PAR1 signaling with cell-penetrating pepducins inhibits Akt survival pathways in breast cancer cells and suppresses tumor survival and metastasis

28 September 2017

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Met receptor tyrosine kinase transactivation is involved in proteinase-activated receptor-2-mediated hepatocellular carcinoma cell invasion.

28 September 2017

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Luminal cathepsin g and protease-activated receptor 4: a duet involved in alterations of the colonic epithelial barrier in ulcerative colitis

28 September 2017

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Targeting a metalloprotease-PAR1 signaling system with cell-penetrating pepducins inhibits angiogenesis, ascites, and progression of ovarian cancer

28 September 2017

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'Role reversal' for the receptor PAR1 in sepsis-induced vascular damage

28 September 2017

1 reference

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Structural analogues of smoothened intracellular loops as potent inhibitors of Hedgehog pathway and cancer cell growth

28 September 2017

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Distinct activity of peptide mimetic intracellular ligands (pepducins) for proteinase-activated receptor-1 in multiple cells/tissues

28 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3339939

Blocking the protease-activated receptor 1-4 heterodimer in platelet-mediated thrombosis

28 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3339939

PAR1 is a matrix metalloprotease-1 receptor that promotes invasion and tumorigenesis of breast cancer cells.

28 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3339939

G-proteins as transducers in transmembrane signalling

28 September 2017

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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3339939

Sequence analyses of G-protein-coupled receptors: similarities to rhodopsin

28 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3339939

A sequence within the cytoplasmic tail of GpIIb independently activates platelet aggregation and thromboxane synthesis

28 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3339939

GCRDb: a G-protein-coupled receptor database

28 September 2017

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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3339939

Constitutive activation of the alpha 1B-adrenergic receptor by all amino acid substitutions at a single site. Evidence for a region which constrains receptor activation

28 September 2017

1 reference

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Sequence alignment of the G-protein coupled receptor superfamily

28 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3339939

Platelet matrix metalloprotease-1 mediates thrombogenesis by activating PAR1 at a cryptic ligand site

28 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3339939

Role of the PAR1 receptor 8th helix in signaling: the 7-8-1 receptor activation mechanism

31 May 2018

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Neutrophils and the kallikrein-kinin system in proteinase-activated receptor 4-mediated inflammation in rodents

31 May 2018

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Proteinase-activated receptor-4: evaluation of tethered ligand-derived peptides as probes for receptor function and as inflammatory agonists in vivo

31 May 2018

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31 May 2018

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Activation of human monocytes by a formyl peptide receptor 2-derived pepducin

31 May 2018

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28 November 2018

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28 November 2018

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28 November 2018

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Length analyses of mammalian G-protein-coupled receptors

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Identification of a Gs activator region of the β2-adrenergic receptor that is autoregulated via protein kinase A-dependent phosphorylation

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