Relation Results

Summary

Name CFTR
Full Name Cystic fibrosis transmembrane conductance regulator
Synonyms CFTR, ATP-binding cassette sub-family C member 7, Channel conductance-controlling ATPase, 3.6.3.49, cAMP-dependent chloride channel | ABCC7
Primary ID P13569
Links - -
Type protein
Relations 38
Inhibitors tolbutamide; glyburide; ivacaftor
Function Epithelial ion channel that plays an important role in the regulation of epithelial ion and water transport and fluid homeostasis (PubMed:26823428). M ...
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Type: Score: Layout: SPV 
0.280.4730.5160.4040.4080.4810.4050.4790.20.80.20.350.6570.80.2550.7150.80.664CSNK2A1CFTRPRKACAPRKG1PRKCALMTK2PRKAA1AMPKSTUB1MARCHF2tolbutamidePP1STK39RNF5glyburideFOXI1GOPCivacaftorHSPA8

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▶Modifications Tables

Relations
Regulator
Mechanism
target
score ℹ
+ CSNK2A1up-regulates img/direct-activation.png phosphorylation CFTR 0.28
Identifier Residue Sequence Organism Cell Line
SIGNOR-176619 Ser422 NNNNRKTsNGDDSLF Homo sapiens
pmid sentence
Cftr possesses two ck2 phosphorylation sites (s422 and t1471)this is consistent with an important role for s422 phosphorylation in increasing cftr activity.
Publications: 1 Organism: Homo Sapiens
+ CSNK2A1down-regulates img/direct_inhibition.png phosphorylation CFTR 0.28
Identifier Residue Sequence Organism Cell Line
SIGNOR-176623 Ser511 ENIIFGVsYDEYRYR Homo sapiens
pmid sentence
Serine 511 has been previously implicated in the regulation of cftr by ck2, as the mutant s511d was found to be insensitive to tbb in xenopus oocytes but to have no major impact on the single-channel behavior of cftr
Identifier Residue Sequence Organism Cell Line
SIGNOR-176627 Thr1471 IAALKEEtEEEVQDT Homo sapiens
pmid sentence
Cftr possesses two ck2 phosphorylation sites (s422 and t1471) the t1471 residue, previously described as a site for cftr phosphorylation by ck2 (25), seems to be critical for cftr turnover and processing.
Publications: 2 Organism: Homo Sapiens
+ PRKACAup-regulates img/direct-activation.png phosphorylation CFTR 0.473
Identifier Residue Sequence Organism Cell Line
SIGNOR-21312 Ser660 FSAERRNsILTETLH Homo sapiens
pmid sentence
Cftr, the protein associated with cystic fibrosis, is phosphorylated on serine residues in response to camp agonists. Serines 660, 737, 795, and 813 were identified as in vivo targets for phosphorylation by protein kinase a.mutagenesis of all four sites abolished the response.
Identifier Residue Sequence Organism Cell Line
SIGNOR-21320 Ser795 TASTRKVsLAPQANL Homo sapiens
pmid sentence
Cftr, the protein associated with cystic fibrosis, is phosphorylated on serine residues in response to camp agonists. Serines 660, 737, 795, and 813 were identified as in vivo targets for phosphorylation by protein kinase a.mutagenesis of all four sites abolished the response.
Identifier Residue Sequence Organism Cell Line
SIGNOR-21324 Ser813 DIYSRRLsQETGLEI Homo sapiens
pmid sentence
Cftr, the protein associated with cystic fibrosis, is phosphorylated on serine residues in response to camp agonists. Serines 660, 737, 795, and 813 were identified as in vivo targets for phosphorylation by protein kinase a.mutagenesis of all four sites abolished the response.
Publications: 3 Organism: Homo Sapiens
+ PRKG1up-regulates img/direct-activation.png phosphorylation CFTR 0.516
Identifier Residue Sequence Organism Cell Line
SIGNOR-18237 Ser660 FSAERRNsILTETLH Homo sapiens
pmid sentence
Direct amino acid sequencing and peptide mapping of cf-2 revealed that serines 660, 700, 737, and 813 as well as serine 768, serine 795, or both were phosphorylated by pka and pkgcftr possesses a large cluster of strict dibasic consensus sites for phosphorylation by protein kinase a (pka) in the r-domain and an obligatory dependence on phosphorylation is a hallmark of cftr cl(-) channel function
Identifier Residue Sequence Organism Cell Line
SIGNOR-72712 Ser660 FSAERRNsILTETLH Homo sapiens
pmid sentence
Direct amino acid sequencing and peptide mapping of cf-2 revealed that serines 660, 700, 737, and 813 as well as serine 768, serine 795, or both were phosphorylated by pka and pkgcftr possesses a large cluster of strict dibasic consensus sites for phosphorylation by protein kinase a (pka) in the r-domain and an obligatory dependence on phosphorylation is a hallmark of cftr cl(-) channel function
Identifier Residue Sequence Organism Cell Line
SIGNOR-18249 Ser795 TASTRKVsLAPQANL Homo sapiens
pmid sentence
Direct amino acid sequencing and peptide mapping of cf-2 revealed that serines 660, 700, 737, and 813 as well as serine 768, serine 795, or both were phosphorylated by pka and pkgcftr possesses a large cluster of strict dibasic consensus sites for phosphorylation by protein kinase a (pka) in the r-domain and an obligatory dependence on phosphorylation is a hallmark of cftr cl(-) channel function
Identifier Residue Sequence Organism Cell Line
SIGNOR-72724 Ser795 TASTRKVsLAPQANL Homo sapiens
pmid sentence
Direct amino acid sequencing and peptide mapping of cf-2 revealed that serines 660, 700, 737, and 813 as well as serine 768, serine 795, or both were phosphorylated by pka and pkgcftr possesses a large cluster of strict dibasic consensus sites for phosphorylation by protein kinase a (pka) in the r-domain and an obligatory dependence on phosphorylation is a hallmark of cftr cl(-) channel function
Identifier Residue Sequence Organism Cell Line
SIGNOR-72728 Ser813 DIYSRRLsQETGLEI Homo sapiens
pmid sentence
Direct amino acid sequencing and peptide mapping of cf-2 revealed that serines 660, 700, 737, and 813 as well as serine 768, serine 795, or both were phosphorylated by pka and pkgcftr possesses a large cluster of strict dibasic consensus sites for phosphorylation by protein kinase a (pka) in the r-domain and an obligatory dependence on phosphorylation is a hallmark of cftr cl(-) channel function
Identifier Residue Sequence Organism Cell Line
SIGNOR-18253 Ser813 DIYSRRLsQETGLEI Homo sapiens
pmid sentence
Direct amino acid sequencing and peptide mapping of cf-2 revealed that serines 660, 700, 737, and 813 as well as serine 768, serine 795, or both were phosphorylated by pka and pkgcftr possesses a large cluster of strict dibasic consensus sites for phosphorylation by protein kinase a (pka) in the r-domain and an obligatory dependence on phosphorylation is a hallmark of cftr cl(-) channel function
Publications: 6 Organism: Homo Sapiens
+ PRKACAup-regulates activity img/direct-activation.png phosphorylation CFTR 0.473
Identifier Residue Sequence Organism Cell Line
SIGNOR-250349 Ser660 FSAERRNsILTETLH in vitro
pmid sentence
CFTR is phosphorylated directly by PKA and PKC in vivo. phosphorylation by PKA is necessary to allow ATP hydrolysis by CFTR and that ATP hydrolysis is necessary for channel opening. CF-2 was phosphorylated by PKA in vitro on serines 660,700, 737, 813 and most likely on both serines 768 and 795.
Identifier Residue Sequence Organism Cell Line
SIGNOR-250348 Ser700 FGEKRKNsILNPINS in vitro
pmid sentence
CFTR is phosphorylated directly by PKA and PKC in vivo. phosphorylation by PKA is necessary to allow ATP hydrolysis by CFTR and that ATP hydrolysis is necessary for channel opening. CF-2 was phosphorylated by PKA in vitro on serines 660,700, 737, 813 and most likely on both serines 768 and 795.
Identifier Residue Sequence Organism Cell Line
SIGNOR-250351 Ser813 DIYSRRLsQETGLEI in vitro
pmid sentence
CFTR is phosphorylated directly by PKA and PKC in vivo. phosphorylation by PKA is necessary to allow ATP hydrolysis by CFTR and that ATP hydrolysis is necessary for channel opening. CF-2 was phosphorylated by PKA in vitro on serines 660,700, 737, 813 and most likely on both serines 768 and 795.
Publications: 3 Organism: In Vitro
+ PRKCAup-regulates activity img/direct-activation.png phosphorylation CFTR 0.404
Identifier Residue Sequence Organism Cell Line
SIGNOR-248849 Ser686 WTETKKQsFKQTGEF in vitro
pmid sentence
Direct amino acid sequencing and peptide mapping of CF-2 revealed that serines 660, 700, 737, and 813 as well as serine 768, serine 795, or both were phosphorylated by PKA and PKG, and serines 686 and 790 were phosphorylated by PKC.
Identifier Residue Sequence Organism Cell Line
SIGNOR-248851 Ser790 IHRKTTAsTRKVSLA in vitro
pmid sentence
Direct amino acid sequencing and peptide mapping of CF-2 revealed that serines 660, 700, 737, and 813 as well as serine 768, serine 795, or both were phosphorylated by PKA and PKG, and serines 686 and 790 were phosphorylated by PKC.
Publications: 2 Organism: In Vitro
+ PRKG1up-regulates activity img/direct-activation.png phosphorylation CFTR 0.516
Identifier Residue Sequence Organism Cell Line
SIGNOR-248850 Ser700 FGEKRKNsILNPINS in vitro
pmid sentence
Direct amino acid sequencing and peptide mapping of CF-2 revealed that serines 660, 700, 737, and 813 as well as serine 768, serine 795, or both were phosphorylated by PKA and PKG, and serines 686 and 790 were phosphorylated by PKC.
Publications: 1 Organism: In Vitro
+ LMTK2down-regulates activity img/direct_inhibition.png phosphorylation CFTR 0.408
Identifier Residue Sequence Organism Cell Line
SIGNOR-278227 Ser737 EPLERRLsLVPDSEQ Homo sapiens
pmid sentence
The present study discovered that in human airway epithelial cells CFTR endocytosis is regulated by the LMTK2-mediated phosphorylation of CFTR-Ser737 that decreases the cell surface density of CFTR Cl\u2212 channels and inhibits CFTR-mediated Cl\u2212 secretion.|Together, the above results demonstrate that the LMTK2 phosphorylation of CFTR-Ser737 facilitates CFTR endocytosis and reduces the plasma membrane abundance of CFTR in human airway epithelial cells.
Publications: 1 Organism: Homo Sapiens
+ PRKAA1down-regulates activity img/direct_inhibition.png phosphorylation CFTR 0.481
Identifier Residue Sequence Organism Cell Line
SIGNOR-259858 Ser737 EPLERRLsLVPDSEQ Homo sapiens
pmid sentence
AMPK phosphorylates CFTR¬†in vitro¬†at two essential serines (Ser737and Ser768) in the R domain, formerly identified as "inhibitory" PKA sites.|Interestingly two of these sites, namely Ser737 and Ser768, have been identified as “inhibitory” R domain sites, i.e. when mutated to alanines they augment the open probability of CFTR relative to wild type|Our present results suggest that it might be AMPK rather than PKA that is phosphorylating Ser737 and Ser768 under baseline conditions
Identifier Residue Sequence Organism Cell Line
SIGNOR-259867 Ser768 LQARRRQsVLNLMTH Homo sapiens
pmid sentence
AMPK phosphorylates CFTR¬†in vitro¬†at two essential serines (Ser737and Ser768) in the R domain, formerly identified as "inhibitory" PKA sites.|Interestingly two of these sites, namely Ser737 and Ser768, have been identified as “inhibitory” R domain sites, i.e. when mutated to alanines they augment the open probability of CFTR relative to wild type|Our present results suggest that it might be AMPK rather than PKA that is phosphorylating Ser737 and Ser768 under baseline conditions
Publications: 2 Organism: Homo Sapiens
+ PRKACAdown-regulates activity img/direct_inhibition.png phosphorylation CFTR 0.473
Identifier Residue Sequence Organism Cell Line
SIGNOR-21316 Ser737 EPLERRLsLVPDSEQ Homo sapiens
pmid sentence
AMPK phosphorylates CFTR in vitro at two essential serines (Ser737and Ser768) in the R domain, formerly identified as "inhibitory" PKA sites.
Identifier Residue Sequence Organism Cell Line
SIGNOR-18141 Ser768 EPLERRLsLVPDSEQ Homo sapiens
pmid sentence
AMPK phosphorylates CFTR in vitro at two essential serines (Ser737and Ser768) in the R domain, formerly identified as "inhibitory" PKA sites.
Publications: 2 Organism: Homo Sapiens
+ AMPKdown-regulates activity img/direct_inhibition.png phosphorylation CFTR 0.405
Identifier Residue Sequence Organism Cell Line
SIGNOR-250350 Ser737 EPLERRLsLVPDSEQ Homo sapiens
pmid sentence
AMPK phosphorylates CFTR¬†in vitro¬†at two essential serines (Ser737and Ser768) in the R domain, formerly identified as "inhibitory" PKA sites.|Interestingly two of these sites, namely Ser737 and Ser768, have been identified as “inhibitory” R domain sites, i.e. when mutated to alanines they augment the open probability of CFTR relative to wild type|Our present results suggest that it might be AMPK rather than PKA that is phosphorylating Ser737 and Ser768 under baseline conditions
Identifier Residue Sequence Organism Cell Line
SIGNOR-72708 Ser768 LQARRRQsVLNLMTH Homo sapiens
pmid sentence
AMPK phosphorylates CFTR¬†in vitro¬†at two essential serines (Ser737and Ser768) in the R domain, formerly identified as "inhibitory" PKA sites.|Interestingly two of these sites, namely Ser737 and Ser768, have been identified as “inhibitory” R domain sites, i.e. when mutated to alanines they augment the open probability of CFTR relative to wild type|Our present results suggest that it might be AMPK rather than PKA that is phosphorylating Ser737 and Ser768 under baseline conditions
Publications: 2 Organism: Homo Sapiens
+ STUB1down-regulates quantity by destabilization img/direct_inhibition.png polyubiquitination, ubiquitination CFTR 0.479
Identifier Residue Sequence Organism Cell Line
SIGNOR-272584 Homo sapiens HEK-293 Cell
pmid sentence
Here we show that CHIP functions with Hsc70 to sense the folded state of CFTR and targets aberrant forms for proteasomal degradation by promoting their ubiquitination. 
Identifier Residue Sequence Organism Cell Line
SIGNOR-278668 Homo sapiens
pmid sentence
Our results indicate that the post-endocytic ubiquitination of CFTR by CHIP is a critical step in the peripheral quality control of cell surface DeltaF508 CFTR.
Publications: 2 Organism: Homo Sapiens
+ MARCHF2down-regulates quantity by destabilization img/direct_inhibition.png ubiquitination CFTR 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-278584 Homo sapiens
pmid sentence
A catalytically dead MARCH2 RING mutant was unable to promote CFTR degradation.|In vivo ubiquitination assays demonstrated the ubiquitination of CFTR by MARCH2, and overexpression of MARCH2, like that of CAL and STX6, led to a dose dependent degradation of mature CFTR that was blocked by bafilomycin A1 treatment.
Publications: 1 Organism: Homo Sapiens
+ tolbutamidedown-regulates activity img/direct_inhibition.png chemical inhibition CFTR 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258345 Mus musculus
pmid sentence
The sulfonylureas, tolbutamide and glibenclamide, inhibited whole-cell CFTR Cl- currents at half-maximal concentrations of approximately 150 and 20 microM, respectively.
Publications: 1 Organism: Mus Musculus
+ PP1up-regulates activity img/direct-activation.png dephosphorylation CFTR 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-264646 Mus musculus
pmid sentence
WNK kinases acted as scaffolds to recruit SPAK, which phosphorylated CFTR and NBCe1-B, reducing their cell surface expression. IRBIT opposed the effects of WNKs and SPAK by recruiting PP1 to the complex to dephosphorylate CFTR and NBCe1-B, restoring their cell surface expression,
Publications: 1 Organism: Mus Musculus
Tissue: Pancreas
+ STK39down-regulates activity img/direct_inhibition.png phosphorylation CFTR 0.35
Identifier Residue Sequence Organism Cell Line
SIGNOR-264643 Mus musculus
pmid sentence
WNK kinases acted as scaffolds to recruit SPAK, which phosphorylated CFTR and NBCe1-B, reducing their cell surface expression. IRBIT opposed the effects of WNKs and SPAK by recruiting PP1 to the complex to dephosphorylate CFTR and NBCe1-B, restoring their cell surface expression,
Identifier Residue Sequence Organism Cell Line
SIGNOR-263134 Homo sapiens HEK-293 Cell
pmid sentence
SPAK phosphorylates the transporters to reduce their surface expression and thus their activity and consequently inhibits ductal secretion to stabilize the resting state. PP1 reverses the effect of SPAK. Molecular analysis revealed that the WNK kinases acted as scaffolds to recruit SPAK, which phosphorylated CFTR and NBCe1-B, reducing their cell surface expression.
Publications: 2 Organism: Mus Musculus, Homo Sapiens
Tissue: Pancreas
+ RNF5down-regulates quantity by destabilization img/direct_inhibition.png ubiquitination CFTR 0.657
Identifier Residue Sequence Organism Cell Line
SIGNOR-271494 Homo sapiens HEK-293 Cell
pmid sentence
JB12 cooperates with cytosolic Hsc70 and the ubiquitin ligase RMA1 to target CFTR and CFTRΔF508 for degradation.
Publications: 1 Organism: Homo Sapiens
+ glyburidedown-regulates activity img/direct_inhibition.png chemical inhibition CFTR 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258344 Mus musculus NIH-3T3 Cell
pmid sentence
The sulfonylureas, tolbutamide and glibenclamide, inhibited whole-cell CFTR Cl- currents at half-maximal concentrations of approximately 150 and 20 microM, respectively.
Publications: 1 Organism: Mus Musculus
+ FOXI1up-regulates quantity by expression img/indirect-activation.png transcriptional regulation CFTR 0.255
Identifier Residue Sequence Organism Cell Line
SIGNOR-254176 Homo sapiens
pmid sentence
Results of transiently transfected vas deferens cells with either the -33G wild-type or the -33A variant CFTR directed luciferase reporter gene confirmed that the -33A variant, which alters the FOXI1 (Forkhead box I1) binding, significantly decreases the CFTR promoter activity.
Publications: 1 Organism: Homo Sapiens
+ GOPCdown-regulates img/direct_inhibition.png binding CFTR 0.715
Identifier Residue Sequence Organism Cell Line
SIGNOR-111671 Homo sapiens
pmid sentence
Cal binds to cftr / cal affects insertion of cftr to the plasma membrane as well as its half-life in the plasma membrane.
Publications: 1 Organism: Homo Sapiens
+ ivacaftordown-regulates img/direct_inhibition.png chemical inhibition CFTR 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-193495 Homo sapiens
pmid sentence
Publications: 1 Organism: Homo Sapiens
+ HSPA8down-regulates quantity img/direct_inhibition.png binding CFTR 0.664
Identifier Residue Sequence Organism Cell Line
SIGNOR-271492 Homo sapiens HEK-293 Cell
pmid sentence
JB12 cooperates with cytosolic Hsc70 and the ubiquitin ligase RMA1 to target CFTR and CFTRΔF508 for degradation. JB12 drives Hsc70 to associate with CFTR and the RMA1 E3 complex
Publications: 1 Organism: Homo Sapiens
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