Id: acc1387
Group: 2sens
Protein: IGF-IR
Gene Symbol: IGF1R
Protein Id: P08069
Protein Name: IGF1R_HUMAN
PTM: phosphorylation
Site: Tyr1131
Site Sequence: GMAYLNANKFVHRDLAARNCM
Disease Category: Cancer
Disease: Sarcoma
Disease Subtype: Rhabdomyosarcoma
Disease Cellline: Rh18
Disease Info:
Drug: SCH717454
Drug Info: "SCH717454 (MK-3475), also known as pembrolizumab, is a humanized monoclonal antibody targeting the PD-1 receptor, used in immunotherapy for various cancers including melanoma and non-small cell lung cancer."
Effect: modulate
Effect Info: "SCH717454 can block IGF-1-stimulated Akt phosphorylation in sarcoma cells, but not IGF-2-stimulated Akt phosphorylation. Similarly, SCH717454 blocks both IGF-1- and IGF-2-stimulated IGF-1R phosphorylation, but does not block IGF-2-stimulated IN-R phosphorylation. Moreover, it blocks VEGF-stimulated HUVEC proliferation and tube formation, but exogenous IGF-2 and insulin circumvent these inhibitory effects."
Note:
Score: 4.0
Pubmed(PMID): 22188815
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
- - P Prostate cancer/carcinoma/adenocarcinoma Glycosylation 23724116
Y 1165 U Breast cancer/tumor/carcinoma Phosphorylation 23663564
Y 1166 U Breast cancer/tumor/carcinoma Phosphorylation 23663564
Y 980 U Ewing sarcoma Phosphorylation 36394520
Y 1135 U Ewing sarcoma Phosphorylation 36394520
Y 1136 U Ewing sarcoma Phosphorylation 36394520
Y 1161 U Neuroblastoma Phosphorylation 24349301
- - U Barrett's neoplasia Phosphorylation 14608530
K 1025 U Acute myelogenous leukemia SUMOylation 25448401
K 1100 U Acute myelogenous leukemia SUMOylation 25448401
- - U Non-small cell lung cancer Ubiquitination 33415003

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: