Id: acc1908
Group: 2sens
Protein: Hsp27
Gene Symbol: HSPB1
Protein Id: P04792
Protein Name: HSPB1_HUMAN
PTM: phosphorylation
Site: Ser82
Site Sequence: YSRALSRQLSSGVSEIRHTAD
Disease Category: Cancer
Disease: Leukemia
Disease Subtype: monocytic leukemia
Disease Cellline: THP-1
Disease Info:
Drug: apigenin
Drug Info: "Apigenin is a naturally occurring flavonoid compound with demonstrated potential as an antifungal agent in the preparation of drugs against human fungal infections, and it is also being researched in drug delivery systems such as solid lipid nanoparticles (APG-SLNP) to enhance stability and bioavailability. "
Effect: inhibit
Effect Info: "Knocking out p38 or silencing PKC affects the phosphorylation of specific sites of Hsp27, ultimately enhancing the sensitivity of leukemia cells to apigenin-induced apoptosis."
Note:
Score: 5.0
Pubmed(PMID): 21364669
Sentence Index:
Sentence:

Sequence & Structure:

MTERRVPFSLLRGPSWDPFRDWYPHSRLFDQAFGLPRLPEEWSQWLGGSSWPGYVRPLPPAAIESPAVAAPAYSRALSRQLSSGVSEIRHTADRWRVSLDVNHFAPDELTVKTKDGVVEITGKHEERQDEHGYISRCFTRKYTLPPGVDPTQVSSSLSPEGTLTVEAPMPKLATQSNEITIPVTFESRAQLGGPEAAKSDETAAK

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
HSPB1 APATORSEN Heat shock protein beta-1 (HSP27) mRNA antisense inhibitor 2 Unknown status squamous cell lung carcinoma ClinicalTrials
HSPB1 APATORSEN Heat shock protein beta-1 (HSP27) mRNA antisense inhibitor 2 Completed pancreatic carcinoma ClinicalTrials
HSPB1 APATORSEN Heat shock protein beta-1 (HSP27) mRNA antisense inhibitor 2 Completed non-small cell lung carcinoma ClinicalTrials
HSPB1 APATORSEN Heat shock protein beta-1 (HSP27) mRNA antisense inhibitor 2 Completed prostate cancer ClinicalTrials
HSPB1 APATORSEN Heat shock protein beta-1 (HSP27) mRNA antisense inhibitor 2 Terminated prostate cancer ClinicalTrials
HSPB1 APATORSEN Heat shock protein beta-1 (HSP27) mRNA antisense inhibitor 1 Completed neoplasm ClinicalTrials
HSPB1 APATORSEN Heat shock protein beta-1 (HSP27) mRNA antisense inhibitor 1 Unknown status urinary bladder 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
HSPB1-Ser82
Cancer Intensity
BRCA 0.019
COAD -0.059
HGSC 2.597
ccRCC -0.808
GBM 0.039
HNSC 0.23
LUAD 0.195
LUSC -0.149
non_ccRCC -1.441
PDAC 0.017
UCEC -0.639

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
S 82 D Atherosclerosis Phosphorylation 15249501
S 82 N Dilated cardiomyopathy Phosphorylation 34477462
S 82 P Pancreatic cancer/carcinoma/adenocarcinoma Phosphorylation 22012255
S 82 U Esophageal squamous cell carcinoma Phosphorylation 32677057
S 82 U Head and neck squamous cell carcinoma Phosphorylation 34498800

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
Protein Gene PTM Position Modified sequence Cell Drug pEC50 Regulation Experiment
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A549 Dactolisib 6.0605 up
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR HeLa CUDC101 3.3284 up
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR HeLa Curcumin 4.2529 up
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR RPMI8226 BTZ 8.3757 up
P04792 HSPB1 P Ser82;Ser83 QLS(ph)S(ph)GVSEIR RPMI8226 BTZ 7.8377 up
P04792 HSPB1 P Ser82;Ser83 QLS(ph)S(ph)GVSEIR RPMI8226 BTZ 7.1638 up
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR RPMI8226 BTZ 7.0889 up
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR RPMI8226 BTZ 8.0294 up
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR RPMI8226 BTZ 7.8861 up
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR RPMI8226 BTZ 7.2749 up
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A549 Dasatinib 6.352 down
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIRHTADRWR RPMI8226 BTZ 9.6373 down
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR K562 Dasatinib 6.3955 down
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR MDA-MB-175 Lapatinib 5.6677 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR MDA-MB-175 Trastuzumab -0.9329 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR KYSE-520 SHP099 6.5541 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR K562 Paclitaxel 8.2867 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR K562 Imatinib 5.7884 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR K562 Dasatinib 4 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR K562 Dasatinib 7.9911 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR K562 Dasatinib 7.5238 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR K562 Dasatinib 11.0131 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR K562 Dasatinib 8.9899 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR K562 Dasatinib 9.0111 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR K562 Cytarabine 6.6059 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR HeLa SAHA 8.5519 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR HeLa Romidepsin 8.2438 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR SK-BR-3 Pertuzumab -0.9156 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR SK-BR-3 Trastuzumab 1.7802 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR SK-BR-3 Lapatinib 8.341 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIRHTADRWR RPMI8226 BTZ 8.7691 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR RPMI8226 BTZ 5.9103 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR RPMI8226 BTZ 7.9042 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR RPMI8226 BTZ 8.771 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIRHTADRWR RPMI8226 BTZ 10.1229 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR RPMI8226 BTZ 10.1272 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIRHTADRWR RPMI8226 BTZ 8.141 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR RPMI8226 BTZ 7.765 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR MDA-MB-175 Pertuzumab -3.7394 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR PC-9 LapatinibAZD4547 5.4968 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR PC-9 Lapatinib 7.255 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR PC-9 GeftinibAZD4547-1to80 7.8884 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR HeLa A485 12.5732 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR PC-9 AZD4547 5.5413 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR PC-9 AZD4547 7.7593 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIRHTADRWR MDA-MB-175 Pertuzumab -3.9966 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A431 Dasatinib 4.225 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A459 SelumetinibMK2206-3to1 7.745 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A459 SelumetinibMK2206-1to2 9.4222 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A459 Selumetinib 5.5528 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A459 MK2206 7.0597 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A431 Imatinib 5.9678 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A431 Gefitinib 13.3135 -
P04792 HSPB1 P Ser82;Ser86 QLS(ph)SGVS(ph)EIR A431 Gefitinib 5.791 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A431 Gefitinib 16.5229 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A431 Gefitinib 7.0041 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A431 Gefitinib 2.6993 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A549 AZD8055 6.6691 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A431 Dasatinib 7.1385 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A431 Dasatinib 6.1741 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A431 Dasatinib 3.7505 -
P04792 HSPB1 P Ser82;Ser86 QLS(ph)SGVS(ph)EIR A431 Dasatinib 5.9775 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A431 Dasatinib 6.1537 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A431 Afatinib 6.0243 -
P04792 HSPB1 P Ser82;Ser86 QLS(ph)SGVS(ph)EIR A431 Afatinib 16.5229 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A431 Afatinib 4.4685 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A431 Afatinib 6.088 -
P04792 HSPB1 P Ser82;Ser86 QLS(ph)SGVS(ph)EIR A431 Afatinib 6.9153 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR ARH-77 Rituximab -1.2345 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A431 Afatinib 4.5681 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR BT-474 Trastuzumab -2.5813 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR BT-474 Pertuzumab -1.1354 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR BT-474 Lapatinib 6.7023 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR ARH-77 Rituximab -3.6695 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR ARH-77 Rituximab -3.9794 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR ARH-77 Rituximab -3.6515 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR ARH-77 Rituximab -1.2236 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR ARH-77 Rituximab -3.7654 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR ARH-77 Rituximab -1.1318 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR HeLa A486 5.2855 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR ARH-77 Rituximab -1.6506 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A549 Tideglusib 2 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A549 Staursporin 7.7985 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A549 Refametinib 7.1732 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A549 Pictilisib 5.8355 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A549 PD325901 8.4449 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A549 PD325901 8.4574 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A549 Nintedanib 6.6242 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A549 MK2206 6.9052 -
P04792 HSPB1 P Ser82 QLS(ph)SGVSEIR A549 Dasatinib 6.4872 -

pEC50 Note: pEC50 is the negative logarithm of EC50 (half-maximal effective concentration, dosage unit Mol), calculated as pEC50 = -log10(EC50), which quantifies the potency of a drug or compound.

Function score:

source: funscoR

No data.

Cross Links: