Id: acc1768
Group: 2sens
Protein: IGF-IR
Gene Symbol: IGF1R
Protein Id: P08069
Protein Name: IGF1R_HUMAN
PTM: phosphorylation
Site: Tyr1136
Site Sequence: NANKFVHRDLAARNCMVAEDF
Disease Category: Cancer
Disease: Glioma
Disease Subtype:
Disease Cellline: U251
Disease Info:
Drug: TAE226
Drug Info: TAE226 is a dual inhibitor of focal adhesion kinase (FAK) and interleukin-1 receptor-associated kinase 4 (IRAK-4) that has demonstrated preclinical efficacy in targeting tumor progression and metastasis pathways.
Effect: modulate
Effect Info: "TAE226 inhibits the phosphorylation of FAK and IGF - IR, and cell viability assays and cell cycle analysis show that it slows down the proliferation and invasion of tumor cells."
Note:
Score: 4.0
Pubmed(PMID): 17431114
Sentence Index:
Sentence:

Sequence & Structure:

MKSGSGGGSPTSLWGLLFLSAALSLWPTSGEICGPGIDIRNDYQQLKRLENCTVIEGYLHILLISKAEDYRSYRFPKLTVITEYLLLFRVAGLESLGDLFPNLTVIRGWKLFYNYALVIFEMTNLKDIGLYNLRNITRGAIRIEKNADLCYLSTVDWSLILDAVSNNYIVGNKPPKECGDLCPGTMEEKPMCEKTTINNEYNYRCWTTNRCQKMCPSTCGKRACTENNECCHPECLGSCSAPDNDTACVACRHYYYAGVCVPACPPNTYRFEGWRCVDRDFCANILSAESSDSEGFVIHDGECMQECPSGFIRNGSQSMYCIPCEGPCPKVCEEEKKTKTIDSVTSAQMLQGCTIFKGNLLINIRRGNNIASELENFMGLIEVVTGYVKIRHSHALVSLSFLKNLRLILGEEQLEGNYSFYVLDNQNLQQLWDWDHRNLTIKAGKMYFAFNPKLCVSEIYRMEEVTGTKGRQSKGDINTRNNGERASCESDVLHFTSTTTSKNRIIITWHRYRPPDYRDLISFTVYYKEAPFKNVTEYDGQDACGSNSWNMVDVDLPPNKDVEPGILLHGLKPWTQYAVYVKAVTLTMVENDHIRGAKSEILYIRTNASVPSIPLDVLSASNSSSQLIVKWNPPSLPNGNLSYYIVRWQRQPQDGYLYRHNYCSKDKIPIRKYADGTIDIEEVTENPKTEVCGGEKGPCCACPKTEAEKQAEKEEAEYRKVFENFLHNSIFVPRPERKRRDVMQVANTTMSSRSRNTTAADTYNITDPEELETEYPFFESRVDNKERTVISNLRPFTLYRIDIHSCNHEAEKLGCSASNFVFARTMPAEGADDIPGPVTWEPRPENSIFLKWPEPENPNGLILMYEIKYGSQVEDQRECVSRQEYRKYGGAKLNRLNPGNYTARIQATSLSGNGSWTDPVFFYVQAKTGYENFIHLIIALPVAVLLIVGGLVIMLYVFHRKRNNSRLGNGVLYASVNPEYFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKGVVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIMELMTRGDLKSYLRSLRPEMENNPVLAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARNCMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGVVLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFLEIISSIKEEMEPGFREVSFYYSEENKLPEPEELDLEPENMESVPLDPSASSSSLPLPDRHSGHKAENGPGPGVLVLRASFDERQPYAHMNGGRKNERALPLPQSSTC

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
IGF1R TEPROTUMUMAB Insulin-like growth factor I receptor antagonist 4 - immune system disease ATC
IGF1R MASOPROCOL Insulin-like growth factor I receptor inhibitor 4 - neoplasm ATC
IGF1R MECASERMIN Insulin-like growth factor I receptor agonist 4 - hypothyroidism DailyMed
IGF1R TEPROTUMUMAB Insulin-like growth factor I receptor antagonist 4 - Graves ophthalmopathy DailyMed
FDA
IGF1R TEPROTUMUMAB Insulin-like growth factor I receptor antagonist 4 Completed Graves ophthalmopathy ClinicalTrials
IGF1R MECASERMIN Insulin-like growth factor I receptor agonist 4 - Growth delay DailyMed
IGF1R MECASERMIN Insulin-like growth factor I receptor agonist 4 - Laron syndrome EMA
IGF1R MECASERMIN Insulin-like growth factor I receptor agonist 3 Completed diabetes mellitus ClinicalTrials
IGF1R FIGITUMUMAB Insulin-like growth factor I receptor antagonist 3 Terminated squamous cell carcinoma ClinicalTrials
ClinicalTrials
IGF1R FIGITUMUMAB Insulin-like growth factor I receptor antagonist 3 Terminated non-small cell lung carcinoma ClinicalTrials
ClinicalTrials
IGF1R FIGITUMUMAB Insulin-like growth factor I receptor antagonist 3 Withdrawn non-small cell lung carcinoma ClinicalTrials
IGF1R FIGITUMUMAB Insulin-like growth factor I receptor antagonist 3 Terminated large cell lung carcinoma ClinicalTrials
ClinicalTrials
IGF1R TEPROTUMUMAB Insulin-like growth factor I receptor antagonist 3 Recruiting eye disease ClinicalTrials
IGF1R TEPROTUMUMAB Insulin-like growth factor I receptor antagonist 3 Completed eye disease ClinicalTrials
IGF1R LINSITINIB Insulin-like growth factor I receptor inhibitor 3 Completed adrenal cortex carcinoma ClinicalTrials
IGF1R TEPROTUMUMAB Insulin-like growth factor I receptor antagonist 3 Completed Graves ophthalmopathy ClinicalTrials
IGF1R MECASERMIN Insulin-like growth factor I receptor agonist 3 Completed Growth abnormality ClinicalTrials
IGF1R MECASERMIN Insulin-like growth factor I receptor agonist 3 Terminated Growth abnormality ClinicalTrials
IGF1R MECASERMIN Insulin-like growth factor I receptor agonist 3 Completed amyotrophic lateral sclerosis ClinicalTrials
IGF1R CIXUTUMUMAB Insulin-like growth factor I receptor antagonist 2 Completed hepatocellular carcinoma ClinicalTrials
IGF1R CIXUTUMUMAB Insulin-like growth factor I receptor antagonist 2 Completed head and neck squamous cell carcinoma ClinicalTrials
IGF1R LINSITINIB Insulin-like growth factor I receptor inhibitor 2 Completed Ewing sarcoma ClinicalTrials
IGF1R GANITUMAB Insulin-like growth factor I receptor antagonist 2 Completed Ewing sarcoma ClinicalTrials
IGF1R LINSITINIB Insulin-like growth factor I receptor inhibitor 2 Terminated hepatocellular carcinoma ClinicalTrials
IGF1R CIXUTUMUMAB Insulin-like growth factor I receptor antagonist 2 Completed alveolar rhabdomyosarcoma 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
IGF1R-Ser1339
Cancer Intensity
BRCA 0.418
COAD
HGSC
ccRCC
GBM
HNSC 0.723
LUAD
LUSC -1.141
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 1136 U Ewing sarcoma Phosphorylation 36394520

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: