Property Summary

NCBI Gene PubMed Count 64
Grant Count 14
R01 Count 5
Funding $1,444,595.33
PubMed Score 168.63
PubTator Score 114.41

Knowledge Summary

Patent (7,580)

Expression

  Differential Expression (18)

Disease log2 FC p
Endometriosis -1.300 0.034
astrocytic glioma -2.600 0.000
ependymoma -2.800 0.000
oligodendroglioma -2.300 0.007
glioblastoma -3.100 0.000
medulloblastoma -3.100 0.000
atypical teratoid / rhabdoid tumor -2.900 0.000
medulloblastoma, large-cell -3.000 0.001
primitive neuroectodermal tumor -3.200 0.000
adrenocortical adenoma -1.341 0.000
adrenocortical carcinoma -1.957 0.000
non-small cell lung carcinoma -2.600 0.000
lung adenocarcinoma -2.200 0.000
pediatric high grade glioma -2.400 0.000
pilocytic astrocytoma -2.400 0.000
lung carcinoma -2.600 0.000
Alzheimer's disease -1.700 0.037
Pick disease -2.100 0.000

MLP Assay (6)

AID Type Active / Inconclusive / Inactive Description
2676 confirmatory 1093 / 3806 / 360488 qHTS Assay for Agonists of the Relaxin Receptor RXFP1
2703 summary 0 / 0 / 0 qHTS Assay for Agonists of the Relaxin Receptor RXFP1: Summary
489012 confirmatory 140 / 201 / 129 qHTS Assay for Agonists of the Relaxin Receptor RXFP1: RXFP1 Hit Validation
492949 confirmatory 119 / 248 / 90 qHTS Assay for Agonists of the Relaxin Receptor RXFP1: THP1 Hit Validation
602256 confirmatory 48 / 10 / 9 qHTS Assay for Agonists of the Relaxin Receptor RXFP1: RXFP1 SAR
602291 other 5 / 0 / 0 qHTS Assay for Agonists of the Relaxin Receptor RXFP1: Cell Impedance

Gene RIF (53)

PMID Text
27088579 The complex binding mode of the peptide hormone H2 relaxin to its receptor RXFP1 has been deciphered.
26238605 RXFP1 gene expression was dysregulated in the anterior cingulate of bipolar patients.
25685807 Synthetic covalently linked dimeric form of H2 relaxin retains native RXFP1 activity and has improved in vitro serum stability.
25547165 H2 relaxin amide is fully active at the relaxin receptor RXFP1 and thus dimerization is not required for biological activity.
25389293 Using cells stably expressing RXFP1, we found that relaxin regulation of PPARgamma activity requires accumulation of cAMP and subsequent activation of cAMP-dependent protein kinase (PKA).
24797570 RXFP-1 receptors are present at the ligament, cartilage, and synovium of the TM joint, indicating that it is a potential target for relaxin. This suggests that circulating relaxin may impact joint stability.
24640558 We have developed and assessed four microRNA against human RXFP1.
24640556 RXFP1, is a complex G-protein coupled receptor (GPCR)and has a rhodopsin-like 7 transmembrane helix region and a large ecto-domain containing Leucine-rich repeats and a Low Desnsity Lipoprotein Class-A module at the N-terminus.
24640555 To create a tool to investigate the low-affinity interaction, a protein scaffold system displaying exoloops 1 and 2 from RXFP1 was designed.
23926099 the RXFP1 receptor lacking the LDLa module binds ligand normally but cannot signal through any characterized G protein-coupled receptor signaling pathway
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AA Sequence

MTSGSVFFYILIFGKYFSHGGGQDVKCSLGYFPCGNITKCLPQLLHCNGVDDCGNQADEDNCGDNNGWSL      1 - 70
QFDKYFASYYKMTSQYPFEAETPECLVGSVPVQCLCQGLELDCDETNLRAVPSVSSNVTAMSLQWNLIRK     71 - 140
LPPDCFKNYHDLQKLYLQNNKITSISIYAFRGLNSLTKLYLSHNRITFLKPGVFEDLHRLEWLIIEDNHL    141 - 210
SRISPPTFYGLNSLILLVLMNNVLTRLPDKPLCQHMPRLHWLDLEGNHIHNLRNLTFISCSNLTVLVMRK    211 - 280
NKINHLNENTFAPLQKLDELDLGSNKIENLPPLIFKDLKELSQLNLSYNPIQKIQANQFDYLVKLKSLSL    281 - 350
EGIEISNIQQRMFRPLMNLSHIYFKKFQYCGYAPHVRSCKPNTDGISSLENLLASIIQRVFVWVVSAVTC    351 - 420
FGNIFVICMRPYIRSENKLYAMSIISLCCADCLMGIYLFVIGGFDLKFRGEYNKHAQLWMESTHCQLVGS    421 - 490
LAILSTEVSVLLLTFLTLEKYICIVYPFRCVRPGKCRTITVLILIWITGFIVAFIPLSNKEFFKNYYGTN    491 - 560
GVCFPLHSEDTESIGAQIYSVAIFLGINLAAFIIIVFSYGSMFYSVHQSAITATEIRNQVKKEMILAKRF    561 - 630
FFIVFTDALCWIPIFVVKFLSLLQVEIPGTITSWVVIFILPINSALNPILYTLTTRPFKEMIHRFWYNYR    631 - 700
QRKSMDSKGQKTYAPSFIWVEMWPLQEMPPELMKPDLFTYPCEMSLISQSTRLNSYS                 701 - 757
//

Text Mined References (66)

PMID Year Title
27088579 2016 The complex binding mode of the peptide hormone H2 relaxin to its receptor RXFP1.
26238605 2015 Transcriptome sequencing of the anterior cingulate in bipolar disorder: dysregulation of G protein-coupled receptors.
25685807 2015 Synthetic covalently linked dimeric form of H2 relaxin retains native RXFP1 activity and has improved in vitro serum stability.
25547165 2015 Solution structure, aggregation behavior, and flexibility of human relaxin-2.
25389293 2015 Relaxin activates peroxisome proliferator-activated receptor ? (PPAR?) through a pathway involving PPAR? coactivator 1? (PGC1?).
24797570 2014 Detection of relaxin receptor in the dorsoradial ligament, synovium, and articular cartilage of the trapeziometacarpal joint.
24640558 2013 Development of human cells with RXFP1 knockdown using retroviral delivery of microRNA against human RXFP1.
24640556 2013 Recombinant RXFP1-LDL-A module does not form dimers.
24640555 2013 Development of a scaffold displaying exoloops of RXFP1.
23926099 2013 The relaxin receptor (RXFP1) utilizes hydrophobic moieties on a signaling surface of its N-terminal low density lipoprotein class A module to mediate receptor activation.
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