Property Summary

NCBI Gene PubMed Count 132
Grant Count 323
R01 Count 192
Funding $26,985,893.72
PubMed Score 533.91
PubTator Score 296.11

Knowledge Summary

Patent (22,805)

Expression

  Differential Expression (8)

Disease log2 FC p
malignant mesothelioma 1.100 0.000
psoriasis -1.100 0.001
glioblastoma -1.100 0.005
medulloblastoma, large-cell -1.400 0.000
adrenocortical adenoma -1.703 0.000
adrenocortical carcinoma -2.574 0.000
adult high grade glioma -1.200 0.001
group 4 medulloblastoma -1.100 0.001

Synonym

Accession Q03431 Q2M1U3
Symbols PFE
PTHR
PTHR1

Gene

PDB

1ET3   3H3G   1ET2   3C4M   1BL1   3L2J   4Z8J  

  TechDev Info (1)

MLP Assay (2)

AID Type Active / Inconclusive / Inactive Description
743265 summary 0 / 0 / 0 qHTS of PTHR Inhibitors: Summary
743266 confirmatory 308 / 6687 / 401922 qHTS of PTHR Inhibitors: Primary Screen

Gene RIF (108)

PMID Text
26562265 Data suggest affinity of ligands for binding site on PTHR1, either in GTP-binding protein-dependent or -independent conformation, alters duration of action of ligand in target cells; ligands were fragments of PTHRP/parathyroid hormone-related protein.
26303600 This Review discusses current understanding of PTHR1 modes of action and how these findings might be applied in future therapeutic agents--{REVIEW}
26047699 Disruption of beta-catenin binding to parathyroid hormone (PTH) receptor PTH1R inhibits PTH-stimulated ERK1/2 activation.
25891861 A Homozygous [Cys25]PTH(1-84) Mutation That Impairs PTH/PTHrP Receptor Activation Defines a Novel Form of Hypoparathyroidism.
25431134 We show that sustained stimulation with PTH leads to diminished potentiation of carbachol-evoked Ca2+ signals. This does not require internalization of PTH1R.
25218037 salt bridge between Arg-20 on parathyroid hormone (PTH) and Asp-137 on the PTH1 receptor is essential for full affinity.
25128082 Treatment of recipient HEK 293a cells transiently expressing PTH1R with PTH-myc CM allowed the labeling of endosomal structures positive for Rab5 and/or for beta-arrestin1.
25043296 PTHR1 signaling is important in maintaining osteosarcoma proliferation and undifferentiated state.
24870837 It is a critical physiological regulator of various biological processes, including bone and cartilage metabolism. (review)
24825834 evaluation of clinical and radiographic characteristics can heighten the specificity of ruling out suspected PTHR1 involvement in PFE patients
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AA Sequence

MGTARIAPGLALLLCCPVLSSAYALVDADDVMTKEEQIFLLHRAQAQCEKRLKEVLQRPASIMESDKGWT      1 - 70
SASTSGKPRKDKASGKLYPESEEDKEAPTGSRYRGRPCLPEWDHILCWPLGAPGEVVAVPCPDYIYDFNH     71 - 140
KGHAYRRCDRNGSWELVPGHNRTWANYSECVKFLTNETREREVFDRLGMIYTVGYSVSLASLTVAVLILA    141 - 210
YFRRLHCTRNYIHMHLFLSFMLRAVSIFVKDAVLYSGATLDEAERLTEEELRAIAQAPPPPATAAAGYAG    211 - 280
CRVAVTFFLYFLATNYYWILVEGLYLHSLIFMAFFSEKKYLWGFTVFGWGLPAVFVAVWVSVRATLANTG    281 - 350
CWDLSSGNKKWIIQVPILASIVLNFILFINIVRVLATKLRETNAGRCDTRQQYRKLLKSTLVLMPLFGVH    351 - 420
YIVFMATPYTEVSGTLWQVQMHYEMLFNSFQGFFVAIIYCFCNGEVQAEIKKSWSRWTLALDFKRKARSG    421 - 490
SSSYSYGPMVSHTSVTNVGPRVGLGLPLSPRLLPTATTNGHPQLPGHAKPGTPALETLETTPPAMAAPKD    491 - 560
DGFLNGSCSGLDEEASGPERPPALLQEEWETVM                                         561 - 593
//

Text Mined References (137)

PMID Year Title
26562265 2016 Binding Selectivity of Abaloparatide for PTH-Type-1-Receptor Conformations and Effects on Downstream Signaling.
26303600 2015 PTH receptor-1 signalling-mechanistic insights and therapeutic prospects.
26047699 2015 Disruption of ?-catenin binding to parathyroid hormone (PTH) receptor inhibits PTH-stimulated ERK1/2 activation.
25891861 2015 A Homozygous [Cys25]PTH(1-84) Mutation That Impairs PTH/PTHrP Receptor Activation Defines a Novel Form of Hypoparathyroidism.
25431134 2015 Sustained signalling by PTH modulates IP3 accumulation and IP3 receptors through cyclic AMP junctions.
25218037 2014 A salt bridge between Arg-20 on parathyroid hormone (PTH) and Asp-137 on the PTH1 receptor is essential for full affinity.
25128082 2014 A tagged parathyroid hormone derivative as a carrier of antibody cargoes transported by the G protein coupled PTH1 receptor.
25043296 2015 Knockdown of PTHR1 in osteosarcoma cells decreases invasion and growth and increases tumor differentiation in vivo.
24870837 2014 [Role for PTHrP in bone and cartilage metabolism].
24825834 2014 Differential diagnosis of primary failure of eruption (PFE) with and without evidence of pathogenic mutations in the PTHR1 gene.
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