Id: acc3247
Group: 2sens
Protein: Chk2
Gene Symbol: CHEK2
Protein Id: O96017
Protein Name: CHK2_HUMAN
PTM: phosphorylation
Site: Thr68
Site Sequence: TLSSLETVSTQELYSIPEDQE
Disease Category: Cancer
Disease: Cancer
Disease Subtype:
Disease Cellline: HeLa
Disease Info:
Drug: Hyperthermia?
Drug Info: "Hyperthermia is not a drug. It refers to a condition where the body's temperature rises above normal, such as in fever or due to external heat sources."
Effect: decrease
Effect Info: "Under the condition of ATR inhibition, hyperthermia enhanced the phosphorylation of Thr68 in Chk2 of cancer cells, suggesting that the ATM - Chk2 pathway serves as a compensatory mechanism for stress response in the absence of ATR to improve thermotolerance. "
Note: Non-conventional drugs
Score: 4.5
Pubmed(PMID): 23383325
Sentence Index:
Sentence:

Sequence & Structure:

MSRESDVEAQQSHGSSACSQPHGSVTQSQGSSSQSQGISSSSTSTMPNSSQSSHSSSGTLSSLETVSTQELYSIPEDQEPEDQEPEEPTPAPWARLWALQDGFANLECVNDNYWFGRDKSCEYCFDEPLLKRTDKYRTYSKKHFRIFREVGPKNSYIAYIEDHSGNGTFVNTELVGKGKRRPLNNNSEIALSLSRNKVFVFFDLTVDDQSVYPKALRDEYIMSKTLGSGACGEVKLAFERKTCKKVAIKIISKRKFAIGSAREADPALNVETEIEILKKLNHPCIIKIKNFFDAEDYYIVLELMEGGELFDKVVGNKRLKEATCKLYFYQMLLAVQYLHENGIIHRDLKPENVLLSSQEEDCLIKITDFGHSKILGETSLMRTLCGTPTYLAPEVLVSVGTAGYNRAVDCWSLGVILFICLSGYPPFSEHRTQVSLKDQITSGKYNFIPEVWAEVSEKALDLVKKLLVVDPKARFTTEEALRHPWLQDEDMKRKFQDLLSEENESTALPQVLAQPSTSRKRPREGEAEGAETTKRPAVCAAVL

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 2 Completed small cell lung carcinoma ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 2 Completed cancer ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 2 Terminated breast cancer ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 2 Terminated ovarian cancer ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 2 Completed ovarian cancer ClinicalTrials
CHEK2 XL-844 Serine/threonine-protein kinase Chk2 inhibitor 1 Terminated chronic lymphocytic leukemia ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 1 Completed myelodysplastic syndrome ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 1 Completed acute myeloid leukemia ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 1 Active, not recruiting central nervous system cancer ClinicalTrials
CHEK2 XL-844 Serine/threonine-protein kinase Chk2 inhibitor 1 Terminated lymphoma ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 1 Completed neoplasm ClinicalTrials
ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 1 Completed squamous cell lung carcinoma ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 1 Completed squamous cell carcinoma ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 1 Active, not recruiting medulloblastoma ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 1 Completed non-small cell lung carcinoma ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 1 Completed colorectal neoplasm ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 1 Completed upper aerodigestive tract neoplasm ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 1 Completed metastasis ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 1 Completed Central Nervous System Neoplasm ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 1 Completed chronic myelomonocytic leukemia ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 1 Active, not recruiting brain cancer ClinicalTrials
CHEK2 PREXASERTIB Serine/threonine-protein kinase Chk2 inhibitor 1 Completed cancer ClinicalTrials
ClinicalTrials
ClinicalTrials
CHEK2 XL-844 Serine/threonine-protein kinase Chk2 inhibitor 1 Terminated cancer 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!

CHEK2-Ser163
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM
HNSC 0.165
LUAD 0.907
LUSC -1.072
non_ccRCC
PDAC
UCEC
CHEK2-Thr430
Cancer Intensity
BRCA
COAD
HGSC -0.707
ccRCC
GBM
HNSC
LUAD 0.707
LUSC
non_ccRCC
PDAC
UCEC
CHEK2-Thr432
Cancer Intensity
BRCA
COAD
HGSC -1.151
ccRCC
GBM
HNSC 0.655
LUAD 0.496
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
T 68 D Colorectal cancer Phosphorylation 33500399
T 68 U Colorectal carcinoma Phosphorylation 35999268
T 68 U Gastric cancer Phosphorylation 33747205
T 68 U Bladder cancer Phosphorylation 15361851
T 68 U Bloom syndrome Phosphorylation 17634426
T 68 U Non-small cell lung cancer/carcinoma Phosphorylation 16705183

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: