Table 2 Small molecule inhibitors of the signaling pathways and their target genes (5)
From: Signaling pathways involved in colorectal cancer progression
Signaling pathways | Factors/drugs approved (or) in development | Function | Target |
|---|---|---|---|
EGFR–RAS–MAPK | Cetuximab | EGFR inhibitor | EGFR |
Panitumumab | EGFR inhibitor | EGFR | |
Gefitinib | EGFR inhibitor | EGFR | |
Sorafenib | Tyrosine kinase inhibitor | RAF | |
Pertuzumab | Monoclonal antibody for Her 2 | Her2 | |
Erlotinib | Receptor tyrosine kinase inhibitor | EGFR | |
Canertinib (CI-1033) | Irreversible tyrosine kinase inhibitor | EGFR Her2 ErbB-4 | |
Lapatinib | Tyrosine kinase inhibitor | EGFR Her2 | |
Dacomitinib | Irreversible EGFR inhibitor | EGFR | |
Sunitinib | Receptor tyrosine kinase inhibitor | RTKs | |
PD158780 | Tyrosine kinase inhibitor | EGFR ErbB-3 ErbB-4 | |
Matuzumab (EMD72000) | Monoclonal antibody for EGFR | EGFR | |
Vemurafenib (PLX4032) | BRAFV600E inhibitor | BRAFV600E | |
Dabrafenib (GSK2118436) | BRAFV600E inhibitor | BRAFV600E C-RAF BRAF | |
Encorafenib (LGX818) | RAF inhibitor | BRAFV600E | |
XL281(BMS-908662) | RAF kinases inhibitor | RAF | |
Trametinib (GSK1120212) | MEK1/2 inhibitor | MEK1/2 | |
Binimetinib | MEK1/2 inhibitor | MEK1/2 | |
Selumetinib (AZD6244) | MEK inhibitor | MEK1/2 | |
VX-11e | ERK2 inhibitor | ERK2 | |
SCH772984 | ERK1/2 inhibitor | ERK1/2 | |
NOTCH | RO4929097 | γ Secretase inhibitor | γ Secretase |
DAPT (GSI-IX) | γ Secretase inhibitor | γ Secretase | |
Dibenzazepine (DBZ) | γ Secretase inhibitor | γ Secretase | |
LY411575 | γ Secretase inhibitor | γ Secretase | |
GSI34 | γ Secretase inhibitor | γ Secretase | |
PI3K–Akt–mTOR | OSI027 | mTOR kinase inhibitor | mTOR PI3Kγ |
MK2206 | AKT inhibitor | AKT | |
GSK690693 | AKT inhibitor | AKT | |
Everolimus (RAD001) | mTOR inhibitor | mTOR | |
Idelalisib (CAL-101) | P110 inhibitor | P110γ/δ | |
BGT226 | PI3K/mTOR inhibitor | mTOR PI3Kα/β/γ | |
Buparlisib (BKM120) | PI3K inhibitor | P110α/β/γ | |
Dactolisib (NVP-BEZ235) | PI3K and mTOR inhibitor | mTOR P110α/γδ | |
GSK690693 | Akt inhibitor | AKT | |
AZD8055 | mTOR inhibitor | mTOR | |
Alpelisib (BYL719) | PI3Kα inhibitor | PI3Kα | |
Perifosine | Akt inhibitor | AKT | |
SF-1126 | Inhibitors of the PI3K pathway | PI3K mTOR | |
Pilaralisib (XL147) | PI3K inhibitor | PI3Kα/β/γ/δ | |
Triciribine (VQD002) | Akt inhibitor | AKT | |
Temsirolimus | Kinase Inhibitor | mTOR | |
TGF-β | LY2109761 | TGF-β receptor inhibitor | TGFBRI/II |
AP15012 | Antisense molecules | TGF-β1 | |
AP11014 | Antisense molecules | TGF-β | |
Wnt/β-catenin | BC2059 | β-catenin inhibitor | β-catenin |
Sulindac | Blocking the PDZ domain of the protein Dishevelled | Dishevelled | |
PNU-74654 | Wnt/B-catenin inhibitor | Wnt/B-catenin |