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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