Id: acc2208
Group: 2sens
Protein: PLK1
Gene Symbol: PLK1
Protein Id: P53350
Protein Name: PLK1_HUMAN
PTM: phosphorylation
Site: Thr210
Site Sequence: VEYDGERKKTLCGTPNYIAPE
Disease Category: Cancer
Disease: Prostate Cancer
Disease Subtype: Hormone refractory prostate cancer (HRPC)
Disease Cellline: PC3
Disease Info:
Drug: KUD773
Drug Info: -
Effect: increase
Effect Info: Protein phosphorylation enhances the sensitivity to drug treatment.
Note:
Score: 5.0
Pubmed(PMID): 25563361
Sentence Index:
Sentence:

Sequence & Structure:

MSAAVTAGKLARAPADPGKAGVPGVAAPGAPAAAPPAKEIPEVLVDPRSRRRYVRGRFLGKGGFAKCFEISDADTKEVFAGKIVPKSLLLKPHQREKMSMEISIHRSLAHQHVVGFHGFFEDNDFVFVVLELCRRRSLLELHKRRKALTEPEARYYLRQIVLGCQYLHRNRVIHRDLKLGNLFLNEDLEVKIGDFGLATKVEYDGERKKTLCGTPNYIAPEVLSKKGHSFEVDVWSIGCIMYTLLVGKPPFETSCLKETYLRIKKNEYSIPKHINPVAASLIQKMLQTDPTARPTINELLNDEFFTSGYIPARLPITCLTIPPRFSIAPSSLDPSNRKPLTVLNKGLENPLPERPREKEEPVVRETGEVVDCHLSDMLQQLHSVNASKPSERGLVRQEEAEDPACIPIFWVSKWVDYSDKYGLGYQLCDNSVGVLFNDSTRLILYNDGDSLQYIERDGTESYLTVSSHPNSLMKKITLLKYFRNYMSEHLLKAGANITPREGDELARLPYLRTWFRTRSAIILHLSNGSVQINFFQDHTKLILCPLMAAVTYIDEKRDFRTYRLSLLEEYGCCKELASRLRYARTMVDKLLSSRSASNRLKAS

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
PLK1 VOLASERTIB Serine/threonine-protein kinase PLK1 inhibitor 3 Completed acute myeloid leukemia ClinicalTrials
PLK1 VOLASERTIB Serine/threonine-protein kinase PLK1 inhibitor 2 Terminated myelodysplastic syndrome ClinicalTrials
PLK1 BI-2536 Serine/threonine-protein kinase PLK1 inhibitor 2 Completed acute myeloid leukemia ClinicalTrials
PLK1 VOLASERTIB Serine/threonine-protein kinase PLK1 inhibitor 2 Completed acute myeloid leukemia ClinicalTrials
PLK1 VOLASERTIB Serine/threonine-protein kinase PLK1 inhibitor 2 Terminated acute myeloid leukemia ClinicalTrials
PLK1 VOLASERTIB Serine/threonine-protein kinase PLK1 inhibitor 2 Completed neoplasm ClinicalTrials
PLK1 BI-2536 Serine/threonine-protein kinase PLK1 inhibitor 2 Completed prostate adenocarcinoma ClinicalTrials
PLK1 BI-2536 Serine/threonine-protein kinase PLK1 inhibitor 2 Completed small cell lung carcinoma ClinicalTrials
PLK1 VOLASERTIB Serine/threonine-protein kinase PLK1 inhibitor 2 Completed non-small cell lung carcinoma ClinicalTrials
PLK1 BI-2536 Serine/threonine-protein kinase PLK1 inhibitor 2 Completed non-small cell lung carcinoma ClinicalTrials
PLK1 BI-2536 Serine/threonine-protein kinase PLK1 inhibitor 2 Completed pancreatic neoplasm ClinicalTrials
PLK1 VOLASERTIB Serine/threonine-protein kinase PLK1 inhibitor 2 Completed ovarian neoplasm ClinicalTrials
PLK1 ONVANSERTIB Serine/threonine-protein kinase PLK1 inhibitor 2 Active, not recruiting metastatic colorectal cancer ClinicalTrials
PLK1 ONVANSERTIB Serine/threonine-protein kinase PLK1 inhibitor 2 Active, not recruiting pancreatic ductal adenocarcinoma ClinicalTrials
PLK1 ONVANSERTIB Serine/threonine-protein kinase PLK1 inhibitor 2 Completed prostate cancer ClinicalTrials
PLK1 VOLASERTIB Serine/threonine-protein kinase PLK1 inhibitor 1 Terminated myelodysplastic syndrome ClinicalTrials
PLK1 VOLASERTIB Serine/threonine-protein kinase PLK1 inhibitor 1 Completed acute myeloid leukemia ClinicalTrials
PLK1 VOLASERTIB Serine/threonine-protein kinase PLK1 inhibitor 1 Terminated acute myeloid leukemia ClinicalTrials
PLK1 VOLASERTIB Serine/threonine-protein kinase PLK1 inhibitor 1 Withdrawn acute monocytic leukemia ClinicalTrials
PLK1 VOLASERTIB Serine/threonine-protein kinase PLK1 inhibitor 1 Withdrawn acute myeloid leukemia ClinicalTrials
ClinicalTrials
PLK1 CAFUSERTIB Serine/threonine-protein kinase PLK1 inhibitor 1 Unknown status acute myeloid leukemia ClinicalTrials
PLK1 ONVANSERTIB Serine/threonine-protein kinase PLK1 inhibitor 1 Completed acute myeloid leukemia ClinicalTrials
PLK1 VOLASERTIB Serine/threonine-protein kinase PLK1 inhibitor 1 Completed leukemia ClinicalTrials
PLK1 VOLASERTIB Serine/threonine-protein kinase PLK1 inhibitor 1 Withdrawn lymphoma ClinicalTrials
PLK1 ONVANSERTIB Serine/threonine-protein kinase PLK1 inhibitor 1 Completed neoplasm 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 data.

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
T 210 U Non-small cell lung cancer Phosphorylation 31548612
T 210 U Pediatric acute lymphoblastic leukemia Phosphorylation 23753023
T 210 U Pancreatic cancer Phosphorylation 34140642

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
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK A549 Staursporin 7.592 down
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK A549 Tideglusib 8.6844 -
P53350 PLK1 P Thr210 T(ph)LCGTPNYIAPEVLSK PC-9 LapatinibAZD4547 6.4446 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK PC-9 Lapatinib 6.5705 -
P53350 PLK1 P Thr210 T(ph)LCGTPNYIAPEVLSK PC-9 Lapatinib 8.2813 -
P53350 PLK1 P Thr210 T(ph)LCGTPNYIAPEVLSK PC-9 AZD4547 6.9826 -
P53350 PLK1 P Thr210 T(ph)LCGTPNYIAPEVLSK KYSE-520 SHP099 4.2445 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK K562 Imatinib 9.9489 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK K562 Dasatinib 7.9961 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK K562 Dasatinib 5.6405 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK K562 Dasatinib 9.256 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK K562 Dasatinib 9.2584 -
P53350 PLK1 P Thr210 T(ph)LCGTPNYIAPEVLSK HeLa SAHA 8.5707 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK HeLa A486 5.2621 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK HeLa A485 5.2747 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK A431 Imatinib 8.4398 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK A549 Refametinib 8.7809 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK A549 Pictilisib 15 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK A549 PD325901 8.7764 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK A549 PD325901 11.0464 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK A549 Nintedanib 10.7348 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK A549 MK2206 6.2085 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK A549 Dasatinib 2 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK A549 Dasatinib 6.1222 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK A549 Dactolisib 7.7137 -
P53350 PLK1 P Thr210 KKT(ph)LCGTPNYIAPEVLSK A549 AZD8055 6.7349 -
P53350 PLK1 P Thr210 T(ph)LCGTPNYIAPEVLSK A459 MK2206 5.7635 -

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: