Id: acc0887
Group: 2sens
Protein: PI3K
Gene Symbol: PIK3CA
Protein Id: P42336
Protein Name: PK3CA_HUMAN
PTM: phosphorylation
Site: Tyr458
Site Sequence: PHGLEDLLNPIGVTGSNPNKE
Disease Category: Cancer
Disease: Lung Cancer
Disease Subtype: NSCLC
Disease Cellline: A549
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: modulate
Effect Info: "Cisplatin reduces the phosphorylation of PI3K and AKT and significantly inhibits the phosphorylation of FOXO3a, thereby inducing cell apoptosis."
Note:
Score: 4.0
Pubmed(PMID): 24814195
Sentence Index:
Sentence:

Sequence & Structure:

MPPRPSSGELWGIHLMPPRILVECLLPNGMIVTLECLREATLITIKHELFKEARKYPLHQLLQDESSYIFVSVTQEAEREEFFDETRRLCDLRLFQPFLKVIEPVGNREEKILNREIGFAIGMPVCEFDMVKDPEVQDFRRNILNVCKEAVDLRDLNSPHSRAMYVYPPNVESSPELPKHIYNKLDKGQIIVVIWVIVSPNNDKQKYTLKINHDCVPEQVIAEAIRKKTRSMLLSSEQLKLCVLEYQGKYILKVCGCDEYFLEKYPLSQYKYIRSCIMLGRMPNLMLMAKESLYSQLPMDCFTMPSYSRRISTATPYMNGETSTKSLWVINSALRIKILCATYVNVNIRDIDKIYVRTGIYHGGEPLCDNVNTQRVPCSNPRWNEWLNYDIYIPDLPRAARLCLSICSVKGRKGAKEEHCPLAWGNINLFDYTDTLVSGKMALNLWPVPHGLEDLLNPIGVTGSNPNKETPCLELEFDWFSSVVKFPDMSVIEEHANWSVSREAGFSYSHAGLSNRLARDNELRENDKEQLKAISTRDPLSEITEQEKDFLWSHRHYCVTIPEILPKLLLSVKWNSRDEVAQMYCLVKDWPPIKPEQAMELLDCNYPDPMVRGFAVRCLEKYLTDDKLSQYLIQLVQVLKYEQYLDNLLVRFLLKKALTNQRIGHFFFWHLKSEMHNKTVSQRFGLLLESYCRACGMYLKHLNRQVEAMEKLINLTDILKQEKKDETQKVQMKFLVEQMRRPDFMDALQGFLSPLNPAHQLGNLRLEECRIMSSAKRPLWLNWENPDIMSELLFQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRMLPYGCLSIGDCVGLIEVVRNSHTIMQIQCKGGLKGALQFNSHTLHQWLKDKNKGEIYDAAIDLFTRSCAGYCVATFILGIGDRHNSNIMVKDDGQLFHIDFGHFLDHKKKKFGYKRERVPFVLTQDFLIVISKGAQECTKTREFERFQEMCYKAYLAIRQHANLFINLFSMMLGSGMPELQSFDDIAYIRKTLALDKTEQEALEYFMKQMNDAHHGGWTTKMDWIFHTIKQHALN

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
PIK3CA COPANLISIB HYDROCHLORIDE PI3-kinase p110-alpha subunit inhibitor 4 - neoplasm of mature B-cells FDA
PIK3CA ALPELISIB PI3-kinase p110-alpha subunit inhibitor 4 - breast carcinoma FDA
PIK3CA ALPELISIB PI3-kinase p110-alpha subunit inhibitor 4 - neoplasm ATC
PIK3CA COPANLISIB PI3-kinase p110-alpha subunit inhibitor 4 - neoplasm ATC
PIK3CA ALPELISIB PI3-kinase p110-alpha subunit inhibitor 4 - breast neoplasm EMA
FDA
PIK3CA ALPELISIB PI3-kinase p110-alpha subunit inhibitor 4 - breast cancer DailyMed
PIK3CA ALPELISIB PI3-kinase p110-alpha subunit inhibitor 4 Recruiting breast cancer ClinicalTrials
PIK3CA COPANLISIB HYDROCHLORIDE PI3-kinase p110-alpha subunit inhibitor 4 - follicular lymphoma DailyMed
PIK3CA DACTOLISIB PI3-kinase class I inhibitor 3 Completed infection ClinicalTrials
PIK3CA ALPELISIB PI3-kinase p110-alpha subunit inhibitor 3 Active, not recruiting breast neoplasm ClinicalTrials
PIK3CA COPANLISIB PI3-kinase p110-alpha subunit inhibitor 3 Active, not recruiting non-Hodgkins lymphoma ClinicalTrials
PIK3CA COPANLISIB PI3-kinase p110-alpha subunit inhibitor 3 Completed non-Hodgkins lymphoma ClinicalTrials
PIK3CA COPANLISIB PI3-kinase p110-alpha subunit inhibitor 3 Terminated non-Hodgkins lymphoma ClinicalTrials
PIK3CA BUPARLISIB PI3-kinase class I inhibitor 3 Active, not recruiting head and neck malignant neoplasia ClinicalTrials
PIK3CA BUPARLISIB PI3-kinase class I inhibitor 3 Completed breast cancer ClinicalTrials
PIK3CA BUPARLISIB PI3-kinase class I inhibitor 3 Terminated breast cancer ClinicalTrials
PIK3CA TASELISIB PI3-kinase class I inhibitor 3 Terminated breast cancer ClinicalTrials
PIK3CA ALPELISIB PI3-kinase p110-alpha subunit inhibitor 3 Active, not recruiting breast cancer ClinicalTrials
ClinicalTrials
PIK3CA ALPELISIB PI3-kinase p110-alpha subunit inhibitor 3 Completed breast cancer ClinicalTrials
ClinicalTrials
PIK3CA ALPELISIB PI3-kinase p110-alpha subunit inhibitor 3 Recruiting breast cancer ClinicalTrials
ClinicalTrials
ClinicalTrials
PIK3CA GEDATOLISIB PI3-kinase class I inhibitor 3 Recruiting breast cancer ClinicalTrials
PIK3CA INAVOLISIB PI3-kinase p110-alpha subunit inhibitor 3 Recruiting breast cancer ClinicalTrials
ClinicalTrials
PIK3CA BUPARLISIB PI3-kinase class I inhibitor 2 Terminated head and neck squamous cell carcinoma ClinicalTrials
PIK3CA ALPELISIB PI3-kinase p110-alpha subunit inhibitor 2 Unknown status head and neck squamous cell carcinoma ClinicalTrials
PIK3CA BUPARLISIB PI3-kinase class I inhibitor 2 Unknown status head and neck squamous cell carcinoma 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
Y 508 P Colorectal cancer Phosphorylation 37689735
Y 317 P Colorectal cancer Phosphorylation 37689735
- - U Gastric cancer Methylation 24513424

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: