Gene Ontology annotation based on UniProtKB/Swiss-Prot Subcellular Location vocabulary mapping, accompanied by conservative changes to GO terms applied by UniProt
Molecular characterization of a dual endothelin-1/Angiotensin II receptor.
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A rat brain cDNA isolated with antisense oligonucleotide probes was reported to encode a single-transmembrane polypeptide with separate ET-1 and angiotensin II binding domains, coupling both ligands to Ca2+ mobilisation.
"Structural analysis revealed a receptor"
Embryonic lethality in Dear gene-deficient mice: new player in angiogenesis.
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Mouse Dear binds ET-1 and the VEGF signal peptide with comparable affinities but does not bind angiotensin II, and Dear-null mice die by embryonic day 12.5 with impaired angiogenesis and disordered neuroepithelial development.
"to Dahl R/JRHS rat Dear, but binds ET-1 and vascular endothelial growth factor"
Association of ATP1A1 and dear single-nucleotide polymorphism haplotypes with essential hypertension: sex-specific and haplotype-specific effects.
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SNP haplotypes at human ATP1A1 and at the DEAR locus associate with essential hypertension in a Sardinian case/control cohort, with sex-specific effects.
"Here we report the association of human ATP1A1 (P<0.000005) and Dear (P<0.03)"
Endothelin receptors: what's new and what do we need to know?
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The DEAR polypeptide is atypical among endothelin receptors in having a single transmembrane region, and its pharmacology and physiology have not been developed.
"The pharmacology and physiology of DEAR has not been developed."
The cardiovascular physiology and pharmacology of endothelin-1.
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Mouse DEAR binds ET-1 and the VEGF signal peptide rather than angiotensin II, and all the DEAR data derive from a single research group whose physiology and pharmacology have not been studied in depth.
"All these data come from one group of scientists, and the physiology and pharmacology of DEAR has not been studied in depth."
DEspR roles in tumor vasculo-angiogenesis, invasiveness, CSC-survival and anoikis resistance: a 'common receptor coordinator' paradigm.
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Anti-DEspR antibody binding to DEspR-expressing Cos1 transfectants and to Panc1 cancer stem-like cells is displaced by endothelin-1 and by the VEGF-A signal peptide, and each ligand elicits a distinct phosphoprotein signature that overlaps only partly with VEGF-VEGFR2 signalling.
"Collectively, these findings support the functionality of VEGFsp- and ET1-binding to DEspR."
Endothelin.
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The IUPHAR review of the endothelin system recognises only two endothelin receptors, ETA and ETB, and reports no further Family A GPCRs that bind endothelin peptides.
"Current evidence only supports the existence of two subtypes, ETA and ETB, according to NC-IUPHAR nomenclature"
Confirmation of translatability and functionality certifies the dual endothelin1/VEGFsp receptor (DEspR) protein.
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Anti-DEspR monoclonal antibodies against two distinct epitopes detect the same 17.5 kDa glycosylated protein in pull-downs from isolated cell membranes, which is deglycosylated by PNGase F, while mass spectrometry of the same pull-downs does not detect DEspR peptides.
"We note that although DEspR was detected consistently in denatured conditions via Western blot analysis of membrane protein pull-down products using 5g12e8 and 6g8g7 anti-DEspR mAbs, MS did not detect DEspR-specific peptides."
Humanized anti-DEspR IgG4(S228P) antibody increases overall survival in a pancreatic cancer stem cell-xenograft peritoneal carcinomatosis rat(nu/nu) model.
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Anti-DEspR antibodies bind the surface of pancreatic tumour and cancer stem-like cells and are internalised, and CRISPR/Cas9 knockout of ADAR1 abolishes DEspR protein expression, attributing the reference-genome stop codon at position 14 to A-to-I RNA editing.
"Blocking anti-DEspR murine precursor and humanized antibodies bind cell-surface DEspR, internalize, and co-translocate with gal1/gal3 nuclear shuttling proteins to the nucleus, subsequently inducing apoptosis in vitro and in vivo."
DEspR(high) neutrophils are associated with critical illness in COVID-19.
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Flow cytometry of fresh whole blood detects cell-surface DEspR on a subset of circulating neutrophils, whose abundance tracks with COVID-19 severity.
"To determine the cell surface expression of DEspR on circulating immune cells, we used flow cytometric analysis."