Id: acc1182
Group: 2sens
Protein: CHK1
Gene Symbol: CHEK1
Protein Id: O14757
Protein Name: CHK1_HUMAN
PTM: phosphorylation
Site: Ser345
Site Sequence: DKLVQGISFSQPTCPDHMLLN
Disease Category: Cancer
Disease: Breast Cancer
Disease Subtype:
Disease Cellline: MCF7
Disease Info:
Drug: Cisplatin
Drug Info: "Cisplatin is a platinum-based chemotherapeutic agent widely used in the treatment of various malignancies, including ovarian, bladder, testicular, and non-small cell lung cancers, by forming DNA cross-links to interfere with replication and repair, thereby inhibiting cancer cell growth and proliferation."
Effect: inhibit
Effect Info: "Phosphorylation of CHK1 at the ser345 site is a specific marker of ATR activity, and NU6027 sensitizes cells to DNA damage therapy by inhibiting ATR."
Note:
Score: 5.0
Pubmed(PMID): 21730979
Sentence Index:
Sentence:

Sequence & Structure:

MAVPFVEDWDLVQTLGEGAYGEVQLAVNRVTEEAVAVKIVDMKRAVDCPENIKKEICINKMLNHENVVKFYGHRREGNIQYLFLEYCSGGELFDRIEPDIGMPEPDAQRFFHQLMAGVVYLHGIGITHRDIKPENLLLDERDNLKISDFGLATVFRYNNRERLLNKMCGTLPYVAPELLKRREFHAEPVDVWSCGIVLTAMLAGELPWDQPSDSCQEYSDWKEKKTYLNPWKKIDSAPLALLHKILVENPSARITIPDIKKDRWYNKPLKKGAKRPRVTSGGVSESPSGFSKHIQSNLDFSPVNSASSEENVKYSSSQPEPRTGLSLWDTSPSYIDKLVQGISFSQPTCPDHMLLNSQLLGTPGSSQNPWQRLVKRMTRFFTKLDADKSYQCLKETCEKLGYQWKKSCMNQVTISTTDRRNNKLIFKVNLLEMDDKILVDFRLSKGDGLEFKRHFLKIKGKLIDIVSSQKIWLPAT

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
CHEK1 UCN-01 Serine/threonine-protein kinase Chk1 inhibitor 2 Terminated lymphoma ClinicalTrials
CHEK1 PREXASERTIB Serine/threonine-protein kinase Chk1 inhibitor 2 Completed small cell lung carcinoma ClinicalTrials
CHEK1 UCN-01 Serine/threonine-protein kinase Chk1 inhibitor 2 Completed small cell lung carcinoma ClinicalTrials
CHEK1 UCN-01 Serine/threonine-protein kinase Chk1 inhibitor 2 Terminated melanoma ClinicalTrials
CHEK1 UCN-01 Serine/threonine-protein kinase Chk1 inhibitor 2 Completed pancreatic carcinoma ClinicalTrials
CHEK1 RABUSERTIB Serine/threonine-protein kinase Chk1 inhibitor 2 Completed non-small cell lung carcinoma ClinicalTrials
CHEK1 UCN-01 Serine/threonine-protein kinase Chk1 inhibitor 2 Completed peritoneum cancer ClinicalTrials
CHEK1 UCN-01 Serine/threonine-protein kinase Chk1 inhibitor 2 Completed fallopian tube cancer ClinicalTrials
CHEK1 UCN-01 Serine/threonine-protein kinase Chk1 inhibitor 2 Unknown status kidney cancer ClinicalTrials
CHEK1 PREXASERTIB Serine/threonine-protein kinase Chk1 inhibitor 2 Completed cancer ClinicalTrials
CHEK1 PREXASERTIB Serine/threonine-protein kinase Chk1 inhibitor 2 Completed ovarian cancer ClinicalTrials
CHEK1 PREXASERTIB Serine/threonine-protein kinase Chk1 inhibitor 2 Terminated ovarian cancer ClinicalTrials
CHEK1 PREXASERTIB Serine/threonine-protein kinase Chk1 inhibitor 2 Terminated breast cancer ClinicalTrials
CHEK1 UCN-01 Serine/threonine-protein kinase Chk1 inhibitor 2 Completed ovarian cancer ClinicalTrials
CHEK1 XL-844 Serine/threonine-protein kinase Chk1 inhibitor 1 Terminated chronic lymphocytic leukemia ClinicalTrials
CHEK1 SCH-900776 Serine/threonine-protein kinase Chk1 inhibitor 1 Completed Hodgkins lymphoma ClinicalTrials
CHEK1 PREXASERTIB Serine/threonine-protein kinase Chk1 inhibitor 1 Completed acute myeloid leukemia ClinicalTrials
CHEK1 UCN-01 Serine/threonine-protein kinase Chk1 inhibitor 1 Completed acute erythroleukemia ClinicalTrials
CHEK1 PREXASERTIB Serine/threonine-protein kinase Chk1 inhibitor 1 Completed myelodysplastic syndrome ClinicalTrials
CHEK1 UCN-01 Serine/threonine-protein kinase Chk1 inhibitor 1 Completed myelodysplastic syndrome ClinicalTrials
ClinicalTrials
CHEK1 UCN-01 Serine/threonine-protein kinase Chk1 inhibitor 1 Completed acute monocytic leukemia ClinicalTrials
CHEK1 UCN-01 Serine/threonine-protein kinase Chk1 inhibitor 1 Completed acute myelomonocytic leukemia ClinicalTrials
CHEK1 SCH-900776 Serine/threonine-protein kinase Chk1 inhibitor 1 Terminated acute lymphoblastic leukemia ClinicalTrials
CHEK1 SCH-900776 Serine/threonine-protein kinase Chk1 inhibitor 1 Terminated acute myeloid leukemia ClinicalTrials
CHEK1 UCN-01 Serine/threonine-protein kinase Chk1 inhibitor 1 Completed acute promyelocytic leukemia ClinicalTrials

Note: Only show clinically investigational or approved drugs with protein targets.

Protein Tractability:

source: Open Targets
Small molecule
Antibody
PROTAC
Other modalities
Approved Drug
Advanced Clinical
Phase 1 Clinical
Structure with Ligand
High-Quality Ligand
High-Quality Pocket
Med-Quality Pocket
Druggable Family
Approved Drug
Advanced Clinical
Phase 1 Clinical
UniProt loc high conf
GO CC high conf
UniProt loc med conf
UniProt SigP or TMHMM
GO CC med conf
Human Protein Atlas loc
Approved Drug
Advanced Clinical
Phase 1 Clinical
Literature
UniProt Ubiquitination
Database Ubiquitination
Half-life Data
Small Molecule Binder
Approved Drug
Advanced Clinical
Phase 1 Clinical

PTM Intensity:

source: CPTAC

No intensity data of this site,
show all other sites!

CHEK1-Ser286
Cancer Intensity
BRCA -0.573
COAD
HGSC -0.61
ccRCC
GBM
HNSC -0.303
LUAD
LUSC
non_ccRCC
PDAC
UCEC 1.486
CHEK1-Ser296
Cancer Intensity
BRCA
COAD 0.707
HGSC -0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
CHEK1-Ser301
Cancer Intensity
BRCA
COAD 0.707
HGSC -0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
CHEK1-Ser317
Cancer Intensity
BRCA
COAD 0.707
HGSC -0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC
CHEK1-Ser331
Cancer Intensity
BRCA
COAD 0.941
HGSC -1.05
ccRCC
GBM
HNSC 0.11
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
S 345 D Riddle syndrome Phosphorylation 17940005
S 345 U Colorectal cancer Phosphorylation 32357935
S 345 U Head and neck squamous cell carcinoma Phosphorylation 21281788
S 345 U Multiple myeloma Phosphorylation 35190641

State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.

PTM-Drug Perturbation Response:

source: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: