Property Summary

NCBI Gene PubMed Count 369
Grant Count 598
R01 Count 397
Funding $57,589,244.04
PubMed Score 1014.60
PubTator Score 805.37

Knowledge Summary

Patent (55,198)

Expression

Synonym

Accession O14757 A8K934 B4DDD0 B4DSK3 B5BTY6 F5H7S4 H2BI51
Symbols CHK1

Gene

PDB

1IA8   1NVQ   1NVR   1NVS   1ZLT   1ZYS   2AYP   2BR1   2BRB   2BRG   2BRH   2BRM   2BRN   2BRO   2C3J   2C3K   2C3L   2CGU   2CGV   2CGW   2CGX   2E9N   2E9O   2E9P   2E9U   2E9V   2GDO   2GHG   2HOG   2HXL   2HXQ   2HY0   2QHM   2QHN   2R0U   2WMQ   2WMR   2WMS   2WMT   2WMU   2WMV   2WMW   2WMX   2X8D   2X8E   2X8I   2XEY   2XEZ   2XF0   2YDI   2YDJ   2YDK   2YER   2YEX   2YM3   2YM4   2YM5   2YM6   2YM7   2YM8   2YWP   3F9N   3JVR   3JVS   3NLB   3OT3   3OT8   3PA3   3PA4   3PA5   3TKH   3TKI   3U9N   4FSM   4FSN   4FSQ   4FSR   4FST   4FSU   4FSW   4FSY   4FSZ   4FT0   4FT3   4FT5   4FT7   4FT9   4FTA   4FTC   4FTI   4FTJ   4FTK   4FTL   4FTM   4FTN   4FTO   4FTQ   4FTR   4FTT   4FTU   4GH2   4HYH   4HYI   4JIK   4QYE   4QYF   4QYG   4QYH   4RVK   4RVL   4RVM   5DLS   5F4N  

  TechDev Info (1)

Gary Johnson Kinome profile via MIB/MS Technology

MLP Assay (1)

AID Type Active / Inconclusive / Inactive Description
1982 other 0 / 0 / 0 Kinase inhibition selectivity assay for compound SID-48409448

Gene RIF (327)

PMID Text
27129240 This study shows that Chk1 indeed maintains a closed conformation in the absence of DNA damage through an intramolecular interaction between a region (residues 31-87) at the N-terminal kinase domain and the distal C terminus. A highly conserved Leu-449 at the C terminus is important for this intramolecular interaction.
26921499 We suggest that MNNG-stimulated ATR/CHK1 signaling stabilizes E2F3 by S124 phosphorylation, and then E2F3 together with NFY co-transactivate RRM2 expression for DNA repair.
26810087 Human induced pluripotent stem cells fail to activate CHK1 when exposed to DNA replication inhibitors and commit to apoptosis instead.
26804904 Avoiding damage formation through invalidation of Mus81-Eme2 and Mre11, or preventing damage signaling by turning off the ATM pathway, suppresses the replication phenotypes of Chk1-deficient cells.
26748709 In conclusion, this study exemplifies cancer-specific synthetic lethality between two proteins in the same pathway and raises the prospect of combining ATR and CHK1 inhibitors as promising cancer therapy.
26693937 A new pathway of proliferation restriction for tetraploid untransformed cells that seems to be specific for loss of adhesion dependent cytokinesis failure involves Chk1 and p53 activation during G2.
26667770 RAD9 has a prominent role in the ATR-Chk1 pathway that is necessary for successful formation of the damage-sensing complex and DNA damage checkpoint signaling.
26658951 these results demonstrate a positive feedback loop involving Rad9A-dependend activation of Chk1.
26542114 Results support the inhibition of checkpoint kinase 1 (Chk1) as a new therapeutic strategy in acute lymphoblastic leukemia.
26459098 Chk1 is a predictive biomarker of radiotherapy resistance and early local recurrence.
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AA Sequence

MAVPFVEDWDLVQTLGEGAYGEVQLAVNRVTEEAVAVKIVDMKRAVDCPENIKKEICINKMLNHENVVKF      1 - 70
YGHRREGNIQYLFLEYCSGGELFDRIEPDIGMPEPDAQRFFHQLMAGVVYLHGIGITHRDIKPENLLLDE     71 - 140
RDNLKISDFGLATVFRYNNRERLLNKMCGTLPYVAPELLKRREFHAEPVDVWSCGIVLTAMLAGELPWDQ    141 - 210
PSDSCQEYSDWKEKKTYLNPWKKIDSAPLALLHKILVENPSARITIPDIKKDRWYNKPLKKGAKRPRVTS    211 - 280
GGVSESPSGFSKHIQSNLDFSPVNSASSEENVKYSSSQPEPRTGLSLWDTSPSYIDKLVQGISFSQPTCP    281 - 350
DHMLLNSQLLGTPGSSQNPWQRLVKRMTRFFTKLDADKSYQCLKETCEKLGYQWKKSCMNQVTISTTDRR    351 - 420
NNKLIFKVNLLEMDDKILVDFRLSKGDGLEFKRHFLKIKGKLIDIVSSQKIWLPAT                  421 - 476
//

Text Mined References (387)

PMID Year Title
27129240 2016 Conformational Change of Human Checkpoint Kinase 1 (Chk1) Induced by DNA Damage.
26921499 2016 ATR-CHK1-E2F3 signaling transactivates human ribonucleotide reductase small subunit M2 for DNA repair induced by the chemical carcinogen MNNG.
26810087 2016 Apoptosis and failure of checkpoint kinase 1 activation in human induced pluripotent stem cells under replication stress.
26804904 2016 Signaling from Mus81-Eme2-Dependent DNA Damage Elicited by Chk1 Deficiency Modulates Replication Fork Speed and Origin Usage.
26748709 2016 Cancer-Specific Synthetic Lethality between ATR and CHK1 Kinase Activities.
26693937 2016 Tetraploid cells produced by absence of substrate adhesion during cytokinesis are limited in their proliferation and enter senescence after DNA replication.
26667770 2015 Regulation of ATRIP protein abundance by RAD9 in the DNA damage repair pathway.
26658951 2015 Chk1 Activation Protects Rad9A from Degradation as Part of a Positive Feedback Loop during Checkpoint Signalling.
26542114 2015 In vitro and in vivo single-agent efficacy of checkpoint kinase inhibition in acute lymphoblastic leukemia.
26459098 2016 Chk1 phosphorylated at serine345 is a predictor of early local recurrence and radio-resistance in breast cancer.
More...