Relation Results

Summary

Name CHEK1
Full Name Serine/threonine-protein kinase Chk1
Synonyms CHK1 checkpoint homolog, Cell cycle checkpoint kinase, Checkpoint kinase-1 | CHK1
Primary ID O14757
Links - -
Type protein
Relations 91
Pathways DNA repair in cancer, FLT3-ITD signaling, Cell cycle: G2/M phase transition
Inhibitors 1-[5-bromo-4-methyl-2-[[(2S)-2-morpholinyl]methoxy]phenyl]-3-(5-methyl-2-pyrazinyl)urea; LY2603618; 3-(carbamoylamino)-5-(3-fluorophenyl)-N-[(3S)-3-piperidinyl]-2-thiophenecarboxamide; CHIR-124; 7-Hydroxystaurosporine; 6-bromo-3-(1-methyl-4-pyrazolyl)-5-(3-piperidinyl)-7-pyrazolo[1,5-a]pyrimidinamine; SCHEMBL14517914
Function Serine/threonine-protein kinase which is required for checkpoint-mediated cell cycle arrest and activation of DNA repair in response to the presence o ...
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Type: Score: Layout: SPV 
0.5640.8540.3330.7750.420.3570.20.8470.7830.3290.2660.20.4370.5420.4160.3140.20.9240.4830.2680.20.8420.2770.5970.3640.530.4820.20.710.5250.4990.3420.3170.4280.7760.4380.2720.20.8390.20.790.20.80.4990.20.30.80.3460.790.3270.3020.80.3040.80.80.80.80.7910.7280.70.4540.5050.20.601CHEK1E2F6CDC25AE2F3TP53ASF1ARASSF1PPP1R12ACDC25CCDC25BERRFI1NEK11AKTAKT1CDK2CDK1SYKATRPPP2CAPPP2CBPPM1FATMNFKB1FANCD2AURKBMDM4PPM1DPABIR1FANCETP73SETMARSRCPLK1RB1BLMTLK1TLK2H3-3ARAD51MAP4CLSPNSNCB1-[5-bromo-4-methyl-2-[[(2S)-2-morpholinyl]methoxy]phenyl]-3-(5-methyl-2-pyrazinyl)ureaHistone H3GSK3BLY2603618MUTYHMEK1/2HUWE13-(carbamoylamino)-5-(3-fluorophenyl)-N-[(3S)-3-piperidinyl]-2-thiophenecarboxamideCDH1CHIR-1247-Hydroxystaurosporine6-bromo-3-(1-methyl-4-pyrazolyl)-5-(3-piperidinyl)-7-pyrazolo[1,5-a]pyrimidinamineSCHEMBL14517914TIMELESSCDC7DNA_damageCullin 1-RBX1-Skp1FBXO6WEE1

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▶Modifications Tables

Relations
Regulator
Mechanism
target
score ℹ
+ CHEK1down-regulates activity img/direct_inhibition.png phosphorylation E2F6 0.564
Identifier Residue Sequence Organism Cell Line
SIGNOR-266370 Ser12 RPARKLPsLLLDPTE in vitro
pmid sentence
the checkpoint kinase Chk1 phosphorylates E2F6 leading to its dissociation from promoters.
Identifier Residue Sequence Organism Cell Line
SIGNOR-266371 Ser52 EDNVQYVsMRKALKV in vitro
pmid sentence
the checkpoint kinase Chk1 phosphorylates E2F6 leading to its dissociation from promoters.
Publications: 2 Organism: In Vitro
+ CHEK1down-regulates img/direct_inhibition.png phosphorylation CDC25A 0.854
Identifier Residue Sequence Organism Cell Line
SIGNOR-163134 Ser124 PALKRSHsDSLDHDI Homo sapiens
pmid sentence
The signal for ubiquitination after uv and ir exposure is created by phosphorylation of cdc25a mediated by chk1 and chk2, respectively. Chk1 is a major kinase phosphorylating cdc25a (ser76/124) and cdc25c (ser216).
Identifier Residue Sequence Organism Cell Line
SIGNOR-163138 Ser178 LFTQRQNsAPARMLS Homo sapiens
pmid sentence
The signal for ubiquitination after uv and ir exposure is created by phosphorylation of cdc25a mediated by chk1 and chk2, respectively. Chk1 is a major kinase phosphorylating cdc25a (ser76/124) and cdc25c (ser216). regulation;btrc(induces);14-3-3 beta(induces);apoptosis, altered;14-3-3 beta(induces);ccna1(disrupts);cdk2(disrupts);cdk1(disrupts);ccnb1(disrupts);
Identifier Residue Sequence Organism Cell Line
SIGNOR-163142 Ser279 VLKRPERsQEESPPG Homo sapiens
pmid sentence
The signal for ubiquitination after uv and ir exposure is created by phosphorylation of cdc25a mediated by chk1 and chk2, respectively. Chk1 is a major kinase phosphorylating cdc25a (ser76/124) and cdc25c (ser216). regulation;btrc(induces);14-3-3 beta(induces);apoptosis, altered;14-3-3 beta(induces);ccna1(disrupts);cdk2(disrupts);cdk1(disrupts);ccnb1(disrupts);
Identifier Residue Sequence Organism Cell Line
SIGNOR-163146 Ser293 GSTKRRKsMSGASPK Homo sapiens
pmid sentence
The signal for ubiquitination after uv and ir exposure is created by phosphorylation of cdc25a mediated by chk1 and chk2, respectively. Chk1 is a major kinase phosphorylating cdc25a (ser76/124) and cdc25c (ser216).
Identifier Residue Sequence Organism Cell Line
SIGNOR-163150 Ser76 SNLQRMGsSESTDSG Homo sapiens
pmid sentence
The signal for ubiquitination after uv and ir exposure is created by phosphorylation of cdc25a mediated by chk1 and chk2, respectively. Chk1 is a major kinase phosphorylating cdc25a (ser76/124) and cdc25c (ser216). regulation;btrc(induces);14-3-3 beta(induces);apoptosis, altered;14-3-3 beta(induces);ccna1(disrupts);cdk2(disrupts);cdk1(disrupts);ccnb1(disrupts);
Identifier Residue Sequence Organism Cell Line
SIGNOR-163154 Thr507 KFRTKSRtWAGEKSK Homo sapiens
pmid sentence
The signal for ubiquitination after uv and ir exposure is created by phosphorylation of cdc25a mediated by chk1 and chk2, respectively. Chk1 is a major kinase phosphorylating cdc25a (ser76/124) and cdc25c (ser216). regulation;btrc(induces);14-3-3 beta(induces);apoptosis, altered;14-3-3 beta(induces);ccna1(disrupts);cdk2(disrupts);cdk1(disrupts);ccnb1(disrupts);
Publications: 6 Organism: Homo Sapiens
Pathways:Cell cycle: G2/M phase transition
+ CHEK1up-regulates img/direct-activation.png phosphorylation E2F3 0.333
Identifier Residue Sequence Organism Cell Line
SIGNOR-161758 Ser124 PALGRGGsGGGGGPP Homo sapiens
pmid sentence
These results suggest that e2f3a is directly phosphorylated by chk kinases and that the phosphorylation of serine 124 is required for the posttranslational induction of e2f3a protein by chemotherapy.
Publications: 1 Organism: Homo Sapiens
+ CHEK1up-regulates activity img/direct-activation.png phosphorylation TP53 0.775
Identifier Residue Sequence Organism Cell Line
SIGNOR-217791 Ser15 PSVEPPLsQETFSDL Homo sapiens LNCaP Cell
pmid sentence
CHK1 and CHK2 phosphorylate the p53 N terminus at Ser15, Thr18, Ser20, and Ser37
Identifier Residue Sequence Organism Cell Line
SIGNOR-217795 Ser20 PLSQETFsDLWKLLP Homo sapiens LNCaP Cell
pmid sentence
CHK1 and CHK2 phosphorylate the p53 N terminus at Ser15, Thr18, Ser20, and Ser37
Identifier Residue Sequence Organism Cell Line
SIGNOR-217853 Ser366 PGGSRAHsSHLKSKK Homo sapiens LNCaP Cell
pmid sentence
Phosphorylation by chk1 of at least three of these sites, Ser366, Ser378, and Thr387, was induced by DNA damage.
Identifier Residue Sequence Organism Cell Line
SIGNOR-217799 Ser37 NVLSPLPsQAMDDLM Homo sapiens LNCaP Cell
pmid sentence
CHK1 and CHK2 phosphorylate the p53 N terminus at Ser15, Thr18, Ser20, and Ser37
Identifier Residue Sequence Organism Cell Line
SIGNOR-217857 Ser378 SKKGQSTsRHKKLMF Homo sapiens
pmid sentence
Phosphorylation by chk1 of at least three of these sites, Ser366, Ser378, and Thr387, was induced by DNA damage.
Identifier Residue Sequence Organism Cell Line
SIGNOR-217803 Thr18 EPPLSQEtFSDLWKL Homo sapiens
pmid sentence
CHK1 and CHK2 phosphorylate the p53 N terminus at Ser15, Thr18, Ser20, and Ser37
Identifier Residue Sequence Organism Cell Line
SIGNOR-217861 Thr387 HKKLMFKtEGPDSD Homo sapiens LNCaP Cell
pmid sentence
Phosphorylation by chk1 of at least three of these sites, Ser366, Ser378, and Thr387, was induced by DNA damage.
Publications: 7 Organism: Homo Sapiens
Pathways:FLT3-ITD signaling, Cell cycle: G2/M phase transition
+ CHEK1up-regulates activity img/direct-activation.png phosphorylation ASF1A 0.42
Identifier Residue Sequence Organism Cell Line
SIGNOR-277620 Ser166 KLEDAESsNPNLQSL Homo sapiens HEK-293T Cell
pmid sentence
Chk1 activated by ataxia telangiectasia mutated (ATM) kinase on DNA breaks in G1 promotes NHEJ through direct phosphorylation of ASF1A at Ser-166. ASF1A phosphorylated at Ser-166 interacts with the repair protein MDC1 and thus enhances MDC1's interaction with ATM and the stable localization of ATM at DNA breaks.
Publications: 1 Organism: Homo Sapiens
+ CHEK1 img/unknown.png phosphorylation RASSF1 0.357
Identifier Residue Sequence Organism Cell Line
SIGNOR-203144 Ser188 PSSKKPPsLQDARRG Homo sapiens
pmid sentence
This study reveals that chk1-mediated phosphorylation of rassf1a, at serine 184, plays an important role in cell-cycle regulation
Publications: 1 Organism: Homo Sapiens
+ CHEK1down-regulates quantity by destabilization img/direct_inhibition.png phosphorylation PPP1R12A 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-277870 Ser20 QLKRWIGsETDLEPP Homo sapiens HeLa Cell
pmid sentence
 MYPT1 is phosphorylated by CDK1, thus recruiting protein phosphatase 1β (PP1cβ) to dephosphorylate and inactivate Plk1. Here we identified that Chk1 directly interacts with MYPT1 and preferentially phosphorylates MYPT1 at Ser20, which is essential for MYPT1-PP1cβ interaction and subsequent Plk1 dephosphorylation.
Publications: 1 Organism: Homo Sapiens
+ CHEK1down-regulates quantity by destabilization img/direct_inhibition.png phosphorylation CDC25C 0.847
Identifier Residue Sequence Organism Cell Line
SIGNOR-163158 Ser216 SGLYRSPsMPENLNR Homo sapiens
pmid sentence
The signal for ubiquitination after uv and ir exposure is created by phosphorylation of cdc25a mediated by chk1 and chk2, respectively. Chk1 is a major kinase phosphorylating cdc25a (ser76/124) and cdc25c (ser216).
Publications: 1 Organism: Homo Sapiens
+ CHEK1down-regulates activity img/direct_inhibition.png phosphorylation CDC25B 0.783
Identifier Residue Sequence Organism Cell Line
SIGNOR-149898 Ser230 AFAQRPSsAPDLMCL Homo sapiens
pmid sentence
Here, we show that cdc25b is phosphorylated by chk1 in vitro on multiple residues, including s230 and s563.We show that the s230-phosphorylated form of cdc25b is located at the centrosome from early s phase until mitosis. Furthermore, mutation of s230 to alanine increases the mitotic-inducing activity of cdc25b
Publications: 1 Organism: Homo Sapiens
+ CHEK1down-regulates activity img/direct_inhibition.png phosphorylation ERRFI1 0.329
Identifier Residue Sequence Organism Cell Line
SIGNOR-276411 Ser251 RRLRRSHsGPAGSFN in vitro
pmid sentence
Our results suggest that Chk1 phosphorylates Mig-6 on Ser 251, resulting in the inhibition of Mig-6, and that Chk1 acts as a positive regulator of EGF signalling. This is a novel function of Chk1.
Publications: 1 Organism: In Vitro
+ CHEK1up-regulates img/direct-activation.png phosphorylation NEK11 0.266
Identifier Residue Sequence Organism Cell Line
SIGNOR-187863 Ser273 SMLNKNPsLRPSAIE Homo sapiens
pmid sentence
We demonstrate that chk1 (checkpoint kinase 1) directly activates nek11 by phosphorylating it on ser 273
Publications: 1 Organism: Homo Sapiens
+ AKTdown-regulates img/direct_inhibition.png phosphorylation CHEK1 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-244206 Ser280 AKRPRVTsGGVSESP Homo sapiens
pmid sentence
The chk1 protein phosphorylated by pkb on serine 280 does not enter into protein complexes after replication arrest. Moreover, chk1 phosphorylated by pkb fails to undergo activating phosphorylation on serine 345 by atm/atr. Phosphorylation by atm/atr and association with other checkpoint proteins are essential steps in activation of chk1.
Publications: 1 Organism: Homo Sapiens
Pathways:FLT3-ITD signaling, Cell cycle: G2/M phase transition
+ AKT1down-regulates img/direct_inhibition.png phosphorylation CHEK1 0.437
Identifier Residue Sequence Organism Cell Line
SIGNOR-124365 Ser280 AKRPRVTsGGVSESP Homo sapiens
pmid sentence
The chk1 protein phosphorylated by pkb on serine 280 does not enter into protein complexes after replication arrest. Moreover, chk1 phosphorylated by pkb fails to undergo activating phosphorylation on serine 345 by atm/atr. Phosphorylation by atm/atr and association with other checkpoint proteins are essential steps in activation of chk1.
Publications: 1 Organism: Homo Sapiens
Pathways:FLT3-ITD signaling
+ CDK2up-regulates img/direct-activation.png phosphorylation CHEK1 0.542
Identifier Residue Sequence Organism Cell Line
SIGNOR-175079 Ser286 TSGGVSEsPSGFSKH Homo sapiens
pmid sentence
Chk1 itself is also subject to cdk-mediated phosphorylation at serines 286 and 301 (s286 and 301). We show that chk1 s301 phosphorylation increases as cells progress through s and g2 and that both cdk1 and cdk2 are likely to contribute to this modification in vivo. We also find that substitution of s286 and s301 with non-phosphorylatable alanine residues strongly attenuates dna damage-induced chk1 activation and g2 checkpoint proficiency
Identifier Residue Sequence Organism Cell Line
SIGNOR-175083 Ser301 IQSNLDFsPVNSASS Homo sapiens
pmid sentence
Chk1 itself is also subject to cdk-mediated phosphorylation at serines 286 and 301 (s286 and 301). We show that chk1 s301 phosphorylation increases as cells progress through s and g2 and that both cdk1 and cdk2 are likely to contribute to this modification in vivo. We also find that substitution of s286 and s301 with non-phosphorylatable alanine residues strongly attenuates dna damage-induced chk1 activation and g2 checkpoint proficiency
Publications: 2 Organism: Homo Sapiens
+ CDK1up-regulates img/direct-activation.png phosphorylation CHEK1 0.416
Identifier Residue Sequence Organism Cell Line
SIGNOR-175071 Ser286 TSGGVSEsPSGFSKH Homo sapiens
pmid sentence
Chk1 itself is also subject to cdk-mediated phosphorylation at serines 286 and 301 (s286 and 301). We show that chk1 s301 phosphorylation increases as cells progress through s and g2 and that both cdk1 and cdk2 are likely to contribute to this modification in vivo. We also find that substitution of s286 and s301 with non-phosphorylatable alanine residues strongly attenuates dna damage-induced chk1 activation and g2 checkpoint proficiency
Identifier Residue Sequence Organism Cell Line
SIGNOR-175075 Ser301 IQSNLDFsPVNSASS Homo sapiens
pmid sentence
Chk1 itself is also subject to cdk-mediated phosphorylation at serines 286 and 301 (s286 and 301). We show that chk1 s301 phosphorylation increases as cells progress through s and g2 and that both cdk1 and cdk2 are likely to contribute to this modification in vivo. We also find that substitution of s286 and s301 with non-phosphorylatable alanine residues strongly attenuates dna damage-induced chk1 activation and g2 checkpoint proficiency
Publications: 2 Organism: Homo Sapiens
+ CHEK1down-regulates img/direct_inhibition.png phosphorylation SYK 0.314
Identifier Residue Sequence Organism Cell Line
SIGNOR-197528 Ser295 GIISRIKsYSFPKPG Homo sapiens
pmid sentence
We found that chk1 phosphorylated the tumor suppressor spleen tyrosine kinase (l) (syk[l]) and identified the phosphorylation site at ser295. Furthermore, chk1 phosphorylation of syk(l) promoted its subsequent proteasomal degradation.
Publications: 1 Organism: Homo Sapiens
+ CHEK1up-regulates activity img/direct-activation.png phosphorylation CHEK1 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-217904 Ser296 GFSKHIQsNLDFSPV Homo sapiens U2-OS Cell
pmid sentence
TheSer296autophosphorylation ofCHK1is mainly regulated by an intramolecular mechanism in response to DNA damage.
Identifier Residue Sequence Organism Cell Line
SIGNOR-219240 Ser296 GFSKHIQsNLDFSPV Xenopus laevis
pmid sentence
This suggests that Ser296 is probably one of the sites autophosphorylated when Chk1 is fully activated [21], despite the sequence surrounding Ser296 (FSKHIQS296NL) being only weakly related to the optimal Chk1-recognition motif (M/I/L/V)-X-(R/K)-X-X-(S/T), where (S/T) is the phosphorylated residue
Publications: 2 Organism: Homo Sapiens, Xenopus Laevis
Pathways:DNA repair in cancer, FLT3-ITD signaling, Cell cycle: G2/M phase transition
+ ATRup-regulates img/direct-activation.png phosphorylation CHEK1 0.924
Identifier Residue Sequence Organism Cell Line
SIGNOR-134712 Ser317 ENVKYSSsQPEPRTG Homo sapiens
pmid sentence
Atr activation typically leads to chk1 phosphorylation and activation. In response to genotoxic stress, chk1 is phosphorylated on serines 317 (s317) and 345 (s345) by the ataxia-telangiectasia-related (atr) protein kinase.
Identifier Residue Sequence Organism Cell Line
SIGNOR-134716 Ser345 LVQGISFsQPTCPDH Homo sapiens
pmid sentence
Atr activation typically leads to chk1 phosphorylation and activation. In response to genotoxic stress, chk1 is phosphorylated on serines 317 (s317) and 345 (s345) by the ataxia-telangiectasia-related (atr) protein kinase.
Publications: 2 Organism: Homo Sapiens
Pathways:DNA repair in cancer, FLT3-ITD signaling, Cell cycle: G2/M phase transition
+ PPP2CAdown-regulates activity img/direct_inhibition.png dephosphorylation CHEK1 0.483
Identifier Residue Sequence Organism Cell Line
SIGNOR-248616 Ser317 ENVKYSSsQPEPRTG Homo sapiens
pmid sentence
Phosphorylation of Chk1 by ATR is antagonized by a Chk1-regulated protein phosphatase 2A circuit|In response to genotoxic stress, Chk1 is phosphorylated on serines 317 (S317) and 345 (S345) by the ataxia-telangiectasia-related (ATR) protein kinase. Phosphorylation of Chk1 on these C-terminal serine residues is used as an indicator of Chk1 activation in vivo.
Identifier Residue Sequence Organism Cell Line
SIGNOR-248615 Ser345 LVQGISFsQPTCPDH Homo sapiens
pmid sentence
Phosphorylation of Chk1 by ATR is antagonized by a Chk1-regulated protein phosphatase 2A circuit|In response to genotoxic stress, Chk1 is phosphorylated on serines 317 (S317) and 345 (S345) by the ataxia-telangiectasia-related (ATR) protein kinase. Phosphorylation of Chk1 on these C-terminal serine residues is used as an indicator of Chk1 activation in vivo.
Publications: 2 Organism: Homo Sapiens
+ PPP2CBdown-regulates activity img/direct_inhibition.png dephosphorylation CHEK1 0.268
Identifier Residue Sequence Organism Cell Line
SIGNOR-248579 Ser317 ENVKYSSsQPEPRTG Homo sapiens
pmid sentence
Phosphorylation of Chk1 by ATR is antagonized by a Chk1-regulated protein phosphatase 2A circuit|In response to genotoxic stress, Chk1 is phosphorylated on serines 317 (S317) and 345 (S345) by the ataxia-telangiectasia-related (ATR) protein kinase. Phosphorylation of Chk1 on these C-terminal serine residues is used as an indicator of Chk1 activation in vivo.
Identifier Residue Sequence Organism Cell Line
SIGNOR-248578 Ser345 LVQGISFsQPTCPDH Homo sapiens
pmid sentence
Phosphorylation of Chk1 by ATR is antagonized by a Chk1-regulated protein phosphatase 2A circuit|In response to genotoxic stress, Chk1 is phosphorylated on serines 317 (S317) and 345 (S345) by the ataxia-telangiectasia-related (ATR) protein kinase. Phosphorylation of Chk1 on these C-terminal serine residues is used as an indicator of Chk1 activation in vivo.
Publications: 2 Organism: Homo Sapiens
+ PPM1Fdown-regulates activity img/direct_inhibition.png dephosphorylation CHEK1 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-276987 Ser317 ENVKYSSsQPEPRTG Homo sapiens
pmid sentence
As a result, inactivation of Chk1 by POPX2 leads to impaired G1S checkpoint activation and cells are able to proceed from G1 to S phase despite DNA damage.|We also determined that POPX2 can dephosphorylate Chk1Ser317 and -Ser345 and is a potential regulator of Chk1 function in the cell.
Identifier Residue Sequence Organism Cell Line
SIGNOR-276988 Ser345 LVQGISFsQPTCPDH Homo sapiens
pmid sentence
As a result, inactivation of Chk1 by POPX2 leads to impaired G1S checkpoint activation and cells are able to proceed from G1 to S phase despite DNA damage.|We also determined that POPX2 can dephosphorylate Chk1Ser317 and -Ser345 and is a potential regulator of Chk1 function in the cell.
Publications: 2 Organism: Homo Sapiens
+ ATMup-regulates img/direct-activation.png phosphorylation CHEK1 0.842
Identifier Residue Sequence Organism Cell Line
SIGNOR-163106 Ser317 ENVKYSSsQPEPRTG Homo sapiens
pmid sentence
Atr (predominantly) or atm (to a lesser extent) phosphorylates chk1 at ser317/345, directly leading to activation.
Identifier Residue Sequence Organism Cell Line
SIGNOR-163110 Ser345 LVQGISFsQPTCPDH Homo sapiens
pmid sentence
Atr (predominantly) or atm (to a lesser extent) phosphorylates chk1 at ser317/345, directly leading to activation.
Publications: 2 Organism: Homo Sapiens
Pathways:DNA repair in cancer, FLT3-ITD signaling, Cell cycle: G2/M phase transition
+ CHEK1down-regulates img/direct_inhibition.png phosphorylation NFKB1 0.277
Identifier Residue Sequence Organism Cell Line
SIGNOR-195208 Ser328 INITKPAsVFVQLRR Homo sapiens
pmid sentence
Taken together, the above findings suggest that chk1 phosphorylates p50 at s329 and further, that this phosphorylation blocks p50 dna binding.
Publications: 1 Organism: Homo Sapiens
+ CHEK1up-regulates activity img/direct-activation.png phosphorylation FANCD2 0.597
Identifier Residue Sequence Organism Cell Line
SIGNOR-263252 Ser331 KSKGRASsSGNQESS Homo sapiens Fanconi Anemia Disease Specific Cell Type
pmid sentence
In this study, we report a novel phosphorylation site serine 331 (S331) of FANCD2, the pivotal downstream player of the Fanconi anemia pathway. Phosphorylation of S331 is important for its DNA damage-inducible monoubiquitylation, resistance to DNA cross-linkers, and in vivo interaction with FANCD1/BRCA2.|In vitro and in vivo experiments show that phosphorylation of S331 is mediated by CHK1,
Identifier Residue Sequence Organism Cell Line
SIGNOR-107042 Ser331 KSKGRASsSGNQESS Homo sapiens HeLa Cell
pmid sentence
In vitro and in vivo experiments show that phosphorylation of s331 is mediated by chk1, the s-phase checkpoint kinase implicated in the fanconi anemia dna repair pathway. phosphorylation at this site is dependent on chk1, signifying the importance of the s-phase checkpoint in the activation of fanconi anemia pathway.
Publications: 2 Organism: Homo Sapiens
+ CHEK1up-regulates img/direct-activation.png phosphorylation AURKB 0.364
Identifier Residue Sequence Organism Cell Line
SIGNOR-152926 Ser331 HPWVRANsRRVLPPS Homo sapiens
pmid sentence
Chk1 phosphorylates aurora-b and enhances its catalytic activity in vitro.
Publications: 1 Organism: Homo Sapiens
+ CHEK1down-regulates activity img/direct_inhibition.png phosphorylation MDM4 0.53
Identifier Residue Sequence Organism Cell Line
SIGNOR-250770 Ser342 SKLTHSLsTSDITAI Homo sapiens SAOS-2 Cell
pmid sentence
MDMX is a direct substrate for Chk1 and Chk2 in vitro. Phosphorylation of MDMX leads to increased binding to MDM2 and more efficient ubiquitination, providing an explanation for the enhanced degradation of MDMX after DNA damage. | Western blot showed that Chk1 modified S342 and S367, but with strong preference for S342.
Publications: 1 Organism: Homo Sapiens
+ PPM1Ddown-regulates img/direct_inhibition.png dephosphorylation CHEK1 0.482
Identifier Residue Sequence Organism Cell Line
SIGNOR-135972 Ser345 LVQGISFsQPTCPDH Homo sapiens
pmid sentence
Ppm1d dephosphorylates chk1 phospho-ser 345
Publications: 1 Organism: Homo Sapiens
+ PPM1Ddown-regulates activity img/direct_inhibition.png dephosphorylation CHEK1 0.482
Identifier Residue Sequence Organism Cell Line
SIGNOR-248317 Ser345 LVQGISFsQPTCPDH Homo sapiens
pmid sentence
Here we show that the oncogenic p53-induced serine/threonine phosphatase, PPM1D (or Wip1), dephosphorylates two ATM/ATR targets, Chk1 and p53. PPM1D binds Chk1 and dephosphorylates the ATR-targeted phospho-Ser 345, leading to decreased Chk1 kinase activity.
Identifier Residue Sequence Organism Cell Line
SIGNOR-276986 Ser345 LVQGISFsQPTCPDH Homo sapiens
pmid sentence
Because Chk1 phosphorylates and activates p53, the inhibition of Chk1 by Wip1 also places Wip1 in a negative feedback regulatory loop for p53 .|In vitro phosphatase assays showed that Wip1 dephosphorylated Chk1 at Ser345, but not Ser317.
Publications: 2 Organism: Homo Sapiens
+ CHEK1down-regulates quantity by destabilization img/direct_inhibition.png phosphorylation MDM4 0.53
Identifier Residue Sequence Organism Cell Line
SIGNOR-178067 Ser367 PDCRRTIsAPVVRPK Homo sapiens
pmid sentence
The chk1 and chk2 kinases have also been shown to phosphorylate ser367, leading to 14-3-3 binding (34_36, 38, 44). In both cases, the outcome differed: in chk1-mediated phosphorylation, mdmx was translocated to the cytoplasm;in chk2-mediated phosphorylation, mdmx was degraded (34_36, 38, 44). It is possible that the damage response is mediated through additional phosphorylation sites other than ser367 and that, depending on the type of damage, certain sites will be modified, leading to different outcomes.
Publications: 1 Organism: Homo Sapiens
+ CHEK1down-regulates activity img/direct_inhibition.png phosphorylation PABIR1 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-266380 Ser37 GGLRRSNsAPLIHGL Homo sapiens A-549 Cell
pmid sentence
Knockout of FAM122A results in activation of PP2A-B55α, a phosphatase that dephosphorylates the WEE1 protein and rescues WEE1 from ubiquitin-mediated degradation. in tumor cells with oncogene-driven replication stress, CHK1 can directly phosphorylate FAM122A, leading to activation of the PP2A-B55α phosphatase and increased WEE1 expression.
Publications: 1 Organism: Homo Sapiens
+ CHEK1up-regulates img/direct-activation.png phosphorylation FANCE 0.71
Identifier Residue Sequence Organism Cell Line
SIGNOR-153023 Ser374 LFLGRILsLTSSASR Homo sapiens
pmid sentence
Chk1 directly phosphorylates the fance subunit of the fa core complex on two conserved sites (threonine 346 and serine 374). chk1-mediated phosphorylation of fance is required for the fanconi anemia/brca pathway.
Identifier Residue Sequence Organism Cell Line
SIGNOR-153027 Thr346 LGLLRLCtWLLALSP Homo sapiens
pmid sentence
Chk1 directly phosphorylates the fance subunit of the fa core complex on two conserved sites (threonine 346 and serine 374). chk1-mediated phosphorylation of fance is required for the fanconi anemia/brca pathway.
Publications: 2 Organism: Homo Sapiens
+ CHEK1up-regulates img/direct-activation.png phosphorylation TP73 0.525
Identifier Residue Sequence Organism Cell Line
SIGNOR-118913 Ser47 EVVGGTDsSMDVFHL Homo sapiens
pmid sentence
We found that endogenous p73alpha is serine phosphorylated by endogenous chk1 upon dna damage, which is a mechanism required for the apoptotic-inducing function of p73alpha.
Publications: 1 Organism: Homo Sapiens
+ CHEK1down-regulates activity img/direct_inhibition.png phosphorylation SETMAR 0.499
Identifier Residue Sequence Organism Cell Line
SIGNOR-273610 Ser508 LYDNRRRsAQWLDQE Homo sapiens HEK-293 Cell
pmid sentence
We previously found that Chk1 phosphorylation of Metnase on S495 enhanced its DNA DSB repair activity but decreased its ability to re-start stalled replication forks. Here we show that phosphorylated Metnase feeds back to increase the half-life of Chk1. Chk1 half-life is regulated by DDB1 targeting it to Cul4A for ubiquitination and destruction. Metnase decreases Chk1 interaction with DDB1, and decreases Chk1 ubiquitination. 
Publications: 1 Organism: Homo Sapiens
+ CHEK1up-regulates activity img/direct-activation.png phosphorylation SRC 0.342
Identifier Residue Sequence Organism Cell Line
SIGNOR-278332 Ser51 ADGHRGPsAAFAPAA Homo sapiens
pmid sentence
In this study, we show that Chk1 phosphorylates human Src at the newly identified site serine 51 to fully induce Src kinase activity.
Publications: 1 Organism: Homo Sapiens
+ CHEK1down-regulates activity img/direct_inhibition.png phosphorylation PLK1 0.317
Identifier Residue Sequence Organism Cell Line
SIGNOR-277913 Ser529 ILHLSNGsVQINFFQ Homo sapiens HeLa Cell
pmid sentence
 Chk1 directly phosphorylates Plk1 to disturb its interaction with Sgo1. 
Identifier Residue Sequence Organism Cell Line
SIGNOR-277914 Thr539 INFFQDHtKLILCPL Homo sapiens HeLa Cell
pmid sentence
 Chk1 directly phosphorylates Plk1 to disturb its interaction with Sgo1. 
Publications: 2 Organism: Homo Sapiens
+ CHEK1up-regulates activity img/direct-activation.png phosphorylation RB1 0.428
Identifier Residue Sequence Organism Cell Line
SIGNOR-153904 Ser612 MYLSPVRsPKKKGST Homo sapiens
pmid sentence
These results suggest that ser612 is phosphorylated by chk1/2 after dna damage, leading to the formation of prb-e2f-1. phosphorylation of prb at ser612 enhanced the formation of a complex between prb and e2f-1
Publications: 1 Organism: Homo Sapiens
Pathways:FLT3-ITD signaling, Cell cycle: G2/M phase transition
+ CHEK1up-regulates img/direct-activation.png phosphorylation BLM 0.776
Identifier Residue Sequence Organism Cell Line
SIGNOR-167534 Ser646 LKHERFQsLSFPHTK Homo sapiens
pmid sentence
Hese results indicated that chk1-mediated phosphorylation on blm at ser(646) might be a determinant for regulating subnuclear localization and could act as a marker for the activation status of blm in response to dna damage.
Publications: 1 Organism: Homo Sapiens
+ CHEK1down-regulates img/direct_inhibition.png phosphorylation TLK1 0.438
Identifier Residue Sequence Organism Cell Line
SIGNOR-99653 Ser743 PHMRRSNsSGNLHMA Homo sapiens
pmid sentence
Chk1 phosphorylates tlk1 on serine 695 (s695) these findings identify an unprecedented functional co- operation between atm and chk1 in propagation of a checkpoint response during s phase and suggest that, through transient inhibition of tlk kinases, the atm_chk1_tlk pathway may regulate processes involved in chromatin assembly.
Publications: 1 Organism: Homo Sapiens
+ CHEK1down-regulates activity img/direct_inhibition.png phosphorylation TLK2 0.272
Identifier Residue Sequence Organism Cell Line
SIGNOR-262740 Ser750 PHIRKSVsTSSPAGA in vitro
pmid sentence
Chk1 phosphorylates GST-fusion fragments of TLK1 in vitro.When Chk1 protein was depleted in cells transfected with pSuper-Chk1, TLK activity was not suppressed after short aphidicolin treatment of S-phase cells (Figure 8a, b).
Publications: 1 Organism: In Vitro
+ CHEK1down-regulates activity img/direct_inhibition.png phosphorylation H3-3A 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-160557 Thr12 KQTARKStGGKAPRK Homo sapiens
pmid sentence
We identify chk1 as the kinase responsible for h3-t11 phosphorylation. H3-t11 phosphorylation occurs throughout the cell cycle and is chk1 dependent in vivo.Phosphorylation at thr-12 (h3t11ph) by pkn1 is a specific tag for epigenetic transcriptional activation that promotes demethylation of lys-10 (h3k9me) by kdm4c/jmjd2c.
Publications: 1 Organism: Homo Sapiens
+ CHEK1down-regulates quantity by destabilization img/direct_inhibition.png phosphorylation BLM 0.776
Identifier Residue Sequence Organism Cell Line
SIGNOR-276909 Thr182 SHFVRVStAQKSKKG Homo sapiens HEK-293T Cell
pmid sentence
We now provide evidence that BLM undergoes K48-linked ubiquitylation and subsequent degradation during mitosis due to the E3 ligase, Fbw7α. Fbw7α carries out its function after GSK3β- and CDK2/cyclin A2-dependent phosphorylation events on Thr171 and Ser175 of BLM which lies within a well-defined phosphodegron, a sequence which is conserved in all primates.Phosphorylation on BLM Thr171 and Ser175 depends on prior phosphorylation at Thr182 by Chk1/Chk2. Thr182 phosphorylation not only controls BLM ubiquitylation and degradation during mitosis but is also a determinant for its localization on the ultrafine bridges.
Publications: 1 Organism: Homo Sapiens
+ CHEK1up-regulates img/direct-activation.png phosphorylation RAD51 0.839
Identifier Residue Sequence Organism Cell Line
SIGNOR-133375 Thr309 LRKGRGEtRICKIYD Homo sapiens
pmid sentence
We demonstrate that chk1 interacts with rad51, and that rad51 is phosphorylated on thr 309 in a chk1-dependent manner
Publications: 1 Organism: Homo Sapiens
Pathways:DNA repair in cancer, FLT3-ITD signaling, Cell cycle: G2/M phase transition
+ CHEK1down-regulates quantity by destabilization img/direct_inhibition.png phosphorylation MAP4 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-277846 Thr521 MALGKDVtPPPETEV Homo sapiens
pmid sentence
MAP4 is a novel target of FBXW7 via the phosphorylated threonine T521 modified by CHEK1 in ESCC. The threonine T521 of MAP4, which was phosphorylated by CHEK1, played a key role in the FBXW7-related degradation system.
Publications: 1 Organism: Homo Sapiens
+ CHEK1up-regulates img/direct-activation.png phosphorylation CLSPN 0.79
Identifier Residue Sequence Organism Cell Line
SIGNOR-149411 Thr916 DELLDLCtGKFTSQA Homo sapiens
pmid sentence
We found that thr-916 on claspin is phosphorylated by chk1, suggesting that chk1 regulates claspin during checkpoint response.
Publications: 1 Organism: Homo Sapiens
+ CHEK1 img/unknown.png phosphorylation SNCB 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-174590 Tyr127 EDPPQEEyQEYEPEA Homo sapiens
pmid sentence
Chk preferentially phosphorylates recombinant _-synuclein at tyrosine-127
Publications: 1 Organism: Homo Sapiens
+ 1-[5-bromo-4-methyl-2-[[(2S)-2-morpholinyl]methoxy]phenyl]-3-(5-methyl-2-pyrazinyl)ureadown-regulates img/direct_inhibition.png chemical inhibition CHEK1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-193787 Homo sapiens
pmid sentence
Publications: 1 Organism: Homo Sapiens
+ SETMARup-regulates quantity by stabilization img/indirect-activation.png CHEK1 0.499
Identifier Residue Sequence Organism Cell Line
SIGNOR-273609 Homo sapiens HEK-293 Cell
pmid sentence
We previously found that Chk1 phosphorylation of Metnase on S495 enhanced its DNA DSB repair activity but decreased its ability to re-start stalled replication forks. Here we show that phosphorylated Metnase feeds back to increase the half-life of Chk1. Chk1 half-life is regulated by DDB1 targeting it to Cul4A for ubiquitination and destruction. Metnase decreases Chk1 interaction with DDB1, and decreases Chk1 ubiquitination.  Phosphorylated Chk1 phosphorylates S495 of Metnase. Phosphorylated Metnase decreases the interaction of DDB1 with Chk1, reducing Chk1 targeting to the Cul4a E3 ubiquitin ligase, increasing Chk1 stability.
Publications: 1 Organism: Homo Sapiens
+ CHEK1down-regulates activity img/direct_inhibition.png phosphorylation Histone H3 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-265326 Homo sapiens
pmid sentence
We identify chk1 as the kinase responsible for h3-t11 phosphorylation. H3-t11 phosphorylation occurs throughout the cell cycle and is chk1 dependent in vivo.Phosphorylation at thr-12 (h3t11ph) by pkn1 is a specific tag for epigenetic transcriptional activation that promotes demethylation of lys-10 (h3k9me) by kdm4c/jmjd2c.
Publications: 1 Organism: Homo Sapiens
+ GSK3Bdown-regulates activity img/indirect_inhibition.png CHEK1 0.3
Identifier Residue Sequence Organism Cell Line
SIGNOR-263050 Mus musculus
pmid sentence
Involvement of GSK3 Inhibition by the PI3K/Akt Pathway in Regulation of Etoposide-induced Chk1 Activation. GSK3ß regulates etoposide-induced Chk1 activation. GSK3 inhibitors, including LiCl and SB216763, restored the sustained Chk1 activation and mitigated apoptosis in cells treated with etoposide and the inhibitors for aberrant kinases, PI3K, or Akt. Thus, proteasomal degradation of Chk1 as well as GSK3 activation may be involved in negative regulation of etoposide-induced Chk1 by imatinib in these cells.
Publications: 1 Organism: Mus Musculus
Pathways:FLT3-ITD signaling, Cell cycle: G2/M phase transition
+ LY2603618down-regulates activity img/direct_inhibition.png chemical inhibition CHEK1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-262538 Homo sapiens
pmid sentence
Here, using a panel of basal-like cancer cell lines, we explored the synergistic interactions of CHK1 inhibitors (rabusertib and SAR020106) with approved therapies in breast cancer and evaluated their potential to overcome resistance.
Publications: 1 Organism: Homo Sapiens
Pathways:FLT3-ITD signaling
+ MUTYHup-regulates img/indirect-activation.png CHEK1 0.346
Identifier Residue Sequence Organism Cell Line
SIGNOR-173969 Homo sapiens
pmid sentence
Hmyh is involved in the activation mechanism of chk1 upon dna damage, but not in stability or inactivation.
Publications: 1 Organism: Homo Sapiens
+ CLSPNup-regulates img/direct-activation.png binding CHEK1 0.79
Identifier Residue Sequence Organism Cell Line
SIGNOR-84474 Homo sapiens
pmid sentence
Binding of claspin to xchk1 is highly elevated in the presence of dna templates that trigger a checkpoint arrest of the cell cycle in xenopus egg extracts
Publications: 1 Organism: Homo Sapiens
+ CHEK1down-regulates activity img/indirect_inhibition.png MEK1/2 0.327
Identifier Residue Sequence Organism Cell Line
SIGNOR-263059 Homo sapiens
pmid sentence
Mechanistically, Ras-MEK signaling drives Chk1 expression and promotes cancer cell growth that produces genotoxic stress that requires Chk1 to mediate a response to the consequent DNA damage. Reciprocally, Chk1 engages a negative feedback loop to prevent hyperactivation of Ras-MEK signaling, thereby limiting DNA damage. Ras–MEK signaling transcriptionally activates Chk1, which appears to sustain cancer cell growth by maintaining DNA damage levels below a threshold that would otherwise drive apoptosis.
Publications: 1 Organism: Homo Sapiens
Pathways:FLT3-ITD signaling
+ HUWE1down-regulates quantity by destabilization img/direct_inhibition.png ubiquitination CHEK1 0.302
Identifier Residue Sequence Organism Cell Line
SIGNOR-278568 Homo sapiens
pmid sentence
Taken together, these results are consistent with our hypothesis that HUWE1 directly poly-ubiquitinates and targets Chk1 to the proteasome.
Publications: 1 Organism: Homo Sapiens
+ 3-(carbamoylamino)-5-(3-fluorophenyl)-N-[(3S)-3-piperidinyl]-2-thiophenecarboxamidedown-regulates img/direct_inhibition.png chemical inhibition CHEK1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-190203 Homo sapiens
pmid sentence
Publications: 1 Organism: Homo Sapiens
+ CHEK1down-regulates activity img/direct_inhibition.png phosphorylation CDH1 0.304
Identifier Residue Sequence Organism Cell Line
SIGNOR-278396 Homo sapiens
pmid sentence
Phosphorylation of Cdh1 by Chk1 promotes recognition of Cdh1 by SCF betaTRCP1.|These data suggest that Chk1 negatively regulates APC/C Cdh1 activity by both promoting Cdh1 destruction and by destabilizing its association with the APC/C.
Publications: 1 Organism: Homo Sapiens
+ CHIR-124down-regulates img/direct_inhibition.png chemical inhibition CHEK1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-190973 Homo sapiens
pmid sentence
Publications: 1 Organism: Homo Sapiens
+ 7-Hydroxystaurosporinedown-regulates img/direct_inhibition.png chemical inhibition CHEK1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-163222 Homo sapiens
pmid sentence
The clinical use of ucn-01, the first chk1 inhibitor evaluated in humans, is limited by its prolonged plasma half-life due to extensive plasma binding to alfa1 acidic glycoprotein
Publications: 1 Organism: Homo Sapiens
+ 6-bromo-3-(1-methyl-4-pyrazolyl)-5-(3-piperidinyl)-7-pyrazolo[1,5-a]pyrimidinaminedown-regulates img/direct_inhibition.png chemical inhibition CHEK1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-206838 Homo sapiens
pmid sentence
Publications: 1 Organism: Homo Sapiens
+ SCHEMBL14517914down-regulates img/direct_inhibition.png chemical inhibition CHEK1 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-163231 Homo sapiens
pmid sentence
Xl844 (exelixis) a potent atp-competitive inhibitor of chk1 (ki, 2.2nm) and chk2 (ki, 0.07nm).
Publications: 1 Organism: Homo Sapiens
+ TIMELESSup-regulates activity img/direct-activation.png binding CHEK1 0.791
Identifier Residue Sequence Organism Cell Line
SIGNOR-268054 Chlorocebus aethiops
pmid sentence
We performed a detailed molecular characterization of TIM interactions with the core clock protein CRY1 and the DNA damage signal transducer CHK1, and found that the N-terminus of TIM is required for association with both proteins, as well as for homodimerization.
Publications: 1 Organism: Chlorocebus Aethiops
+ CHEK1up-regulates img/direct-activation.png phosphorylation CDC7 0.728
Identifier Residue Sequence Organism Cell Line
SIGNOR-163161 Homo sapiens
pmid sentence
Chk1 directly phosphorylates essential s-phase kinases cdc7.
Publications: 1 Organism: Homo Sapiens
+ DNA_damageup-regulates img/indirect-activation.png CHEK1 0.7
Identifier Residue Sequence Organism Cell Line
SIGNOR-242616 Homo sapiens
pmid sentence
Checkpoint kinase 1 (CHK1) is a key component of the ATR-dependent DNA damage response pathway that protects cells from RS by preventing replication fork collapse and activating homologous DNA repair.
Publications: 1 Organism: Homo Sapiens
Pathways:DNA repair in cancer, FLT3-ITD signaling, Cell cycle: G2/M phase transition
+ Cullin 1-RBX1-Skp1down-regulates quantity by destabilization img/direct_inhibition.png polyubiquitination CHEK1 0.454
Identifier Residue Sequence Organism Cell Line
SIGNOR-271880 Homo sapiens HEK-293 Cell
pmid sentence
 Here, we report that DNA damage not only activates Chk1, but also exposes a degron-like region at the carboxyl terminus of Chk1 to an Fbx6-containing SCF (Skp1-Cul1-F box) E3 ligase, which mediates the ubiquitination and degradation of Chk1 and, in turn, terminates the checkpoint.
Publications: 1 Organism: Homo Sapiens
+ FBXO6down-regulates quantity by destabilization img/direct_inhibition.png binding CHEK1 0.505
Identifier Residue Sequence Organism Cell Line
SIGNOR-271879 Homo sapiens HEK-293 Cell
pmid sentence
 Here, we report that DNA damage not only activates Chk1, but also exposes a degron-like region at the carboxyl terminus of Chk1 to an Fbx6-containing SCF (Skp1-Cul1-F box) E3 ligase, which mediates the ubiquitination and degradation of Chk1 and, in turn, terminates the checkpoint.
Publications: 1 Organism: Homo Sapiens
+ MEK1/2up-regulates quantity by expression img/indirect-activation.png transcriptional regulation CHEK1 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-263069 Homo sapiens
pmid sentence
Mechanistically, Ras-MEK signaling drives Chk1 expression and promotes cancer cell growth that produces genotoxic stress that requires Chk1 to mediate a response to the consequent DNA damage. Reciprocally, Chk1 engages a negative feedback loop to prevent hyperactivation of Ras-MEK signaling, thereby limiting DNA damage. Ras–MEK signaling transcriptionally activates Chk1, which appears to sustain cancer cell growth by maintaining DNA damage levels below a threshold that would otherwise drive apoptosis.
Publications: 1 Organism: Homo Sapiens
Pathways:FLT3-ITD signaling
+ CHEK1up-regulates img/direct-activation.png phosphorylation WEE1 0.601
Identifier Residue Sequence Organism Cell Line
SIGNOR-163164 Homo sapiens
pmid sentence
Chk1 also phosphorylates and stabilizes wee1.
Publications: 1 Organism: Homo Sapiens
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