Id: acc2119
Group: 2sens
Protein: p27
Gene Symbol: CDKN1B
Protein Id: P46527
Protein Name: CDN1B_HUMAN
PTM: phosphorylation
Site: Ser10
Site Sequence: MSNVRVSNGSPSLERMDARQA
Disease Category: Cancer
Disease: Breast Cancer
Disease Subtype: HER2+
Disease Cellline: SK-BR-3
Disease Info:
Drug: erlotinib
Drug Info: "Erlotinib is a medication used in the treatment of certain types of lung cancer, particularly non-small cell lung cancer (NSCLC), and pancreatic cancer, often as a maintenance therapy or after chemotherapy failure."
Effect: resist
Effect Info: Phosphorylation of p27 leads to erlotinib resistance in breast cancer with epidermal growth factor receptor (EGFR) expression.
Note:
Score: 5.0
Pubmed(PMID): 21045138
Sentence Index:
Sentence:

Sequence & Structure:

MSNVRVSNGSPSLERMDARQAEHPKPSACRNLFGPVDHEELTRDLEKHCRDMEEASQRKWNFDFQNHKPLEGKYEWQEVEKGSLPEFYYRPPRPPKGACKVPAQESQDVSGSRPAAPLIGAPANSEDTHLVDPKTDPSDSQTGLAEQCAGIRKRPATDDSSTQNKRANRTEENVSDGSPNAGSVEQTPKKPGLRRRQT

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

No data.

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
CDKN1B-Ser10
Cancer Intensity
BRCA 0.427
COAD 0.021
HGSC 1.815
ccRCC -0.291
GBM 0.132
HNSC 0.113
LUAD 0.655
LUSC 0.426
non_ccRCC -1.023
PDAC -0.097
UCEC -2.178

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
S 10 P Epithelial ovarian cancer Phosphorylation 24018641
S 10 P Atherosclerosis Phosphorylation 21885849
S 10 P Breast cancer/tumor/carcinoma Phosphorylation 21067268 ;  21216562
S 10 U Chronic myelogenous leukemia/chronic myeloid leukemia Phosphorylation 24098519
S 10 U Non-alcoholic steatohepatitis Phosphorylation 24351862
S 10 U Breast cancer Phosphorylation 25205104
S 10 U Gallbladder carcinoma Phosphorylation 33444777

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
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER RPMI8226 BTZ 8.0516 down
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER RPMI8226 BTZ 8.4652 down
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER RPMI8226 BTZ 8.3159 down
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER RPMI8226 BTZ 8.4974 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER BT-474 Trastuzumab -2.7204 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER MDA-MB-175 Lapatinib 8.5177 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER MDA-MB-175 Pertuzumab -2.0198 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER MDA-MB-175 Trastuzumab 1.0537 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER PC-9 AZD4547 6.8725 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER PC-9 Lapatinib 7.7641 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER PC-9 LapatinibAZD4547 7.2568 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER BT-474 Pertuzumab -1.8836 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER RPMI8226 BTZ 6.8562 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER RPMI8226 BTZ 6.4278 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER RPMI8226 BTZ 3 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER RPMI8226 BTZ 8.4672 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER RPMI8226 BTZ 7.397 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER RPMI8226 BTZ 7.6661 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER SK-BR-3 Lapatinib 7.7637 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A431 Gefitinib 7.5289 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A431 Afatinib 5.2067 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A431 Afatinib 6.2541 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A431 Afatinib 7.7968 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A431 Dasatinib 6.2602 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A431 Dasatinib 7.9388 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A431 Dasatinib 7.2664 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A431 Gefitinib 5.9528 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A431 Gefitinib 6.7949 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A431 Afatinib 6.4994 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A431 Gefitinib 5.2422 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A459 MK2206 5.7471 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A459 MK2206 7.288 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A459 Selumetinib 5.7158 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A459 Selumetinib 6.766 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A459 SelumetinibMK2206-1to2 8.7701 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER A459 SelumetinibMK2206-3to1 8.2372 -
P46527 CDKN1B P Ser10 VSNGS(ph)PSLER BT-474 Lapatinib 6.8657 -

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: