Table 1. Validated EGFR-sensitizing genes.
Validated screen hits. Symbol is the official Entrez gene name, ID is Entrez gene ID.
Symbol | ID | Gene Description | Origin | Clinical agent |
---|---|---|---|---|
ABL1 | 25 | v-abl Abelson murine leukemia viral oncogene homolog 1 | PPI1 | Imatinib, dasatinib |
AKT2 | 208 | v-akt murine thymoma viral oncogene homolog 2 | PG | Perifosine, triciribine, GSK690693 |
ANXA6 | 309 | annexin A6 | C, PPI2 | |
ARF4 | 378 | ADP-ribosylation factor 4 | PM, PPI1 | |
ARF5 | 381 | ADP-ribosylation factor 5 | PG | |
ASCL2 | 430 | achaete-scute complex homolog 2 (Drosophila) | PPI2, DG | |
BCAR1 | 9564 | breast cancer anti-estrogen resistance 1 | PM, C, PPI1 | |
CALM1 | 801 | calmodulin 1 (phosphorylase kinase, delta) | C PPI1 | phenothiazines |
CBLC | 23624 | Cas-Br-M (murine) ecotropic retroviral transforming sequence c | PM PPI1 | |
CCND1 | 595 | cyclin D1 | PM, PPI2 | |
CD59 | 966 | CD59 molecule, complement regulatory protein | C, PPI2 | Roche, Preclinical |
CDH3 | 1001 | cadherin 3, type 1, P-cadherin (placental) | PG | |
CXCL12 | 6387 | chemokine (C-X-C motif) ligand 12 (stromal cell-derived factor 1) | MA | |
DCN | 1634 | decorin | PPI1 | |
DDR2 | 4921 | discoidin domain receptor family, member 2 | PPI1 | |
DIXDC1 | 85458 | DIX domain containing 1 | MA | |
DLG4 | 1742 | discs, large homolog 4 (Drosophila) | PPI1 | |
DUSP4 | 1846 | dual specificity phosphatase 4 | MA | |
DUSP6 | 1848 | dual specificity phosphatase 6 | DG | |
DUSP7 | 1849 | dual specificity phosphatase 7 | DG | |
EPHA5 | 2044 | EPH receptor A5 | PG | |
ERBB3 | 2065 | v-erb-b2 erythroblastic leukemia viral oncogene homolog 3 (avian) | PM, PPI1, DG | antibodies, for example MM-121 |
FER | 2241 | fer (fps/fes related) tyrosine kinase (phosphoprotein NCP94) | PPI1 | |
FGFR2 | 2263 | fibroblast growth factor receptor 2 (bacteria-expressed kinase, keratinocyte growth factor receptor, craniofacial dysostosis 1, Crouzon syndrome, Pfeiffer syndrome, Jackson-Weiss syndrome) | DG | For example, brivanib, masitinib, TKI258, PHA-739358 |
FLNA | 2316 | filamin PG, alpha (actin binding protein 280) | C, PPI2 | |
GRB7 | 2886 | growth factor receptor-bound protein 7 | PM, PPI1 | |
HSPA9 | 3313 | heat shock 70kDa protein 9 (mortalin) | C, PPI2 | |
INPPL1 | 3636 | inositol polyphosphate phosphatase-like 1 | PM, PPI1 | |
KLF10 | 7071 | Kruppel-like factor 10 | MA | |
LOC284393 | 284393 | similar to ribosomal protein L10 | PG | |
LOC63920 | 63920 | transposon-derived Buster3 transposase-like | MA | |
LTK | 4058 | leukocyte tyrosine kinase | PPI1 | |
MAP3K1 | 4214 | mitogen-activated protein kinase kinase kinase 1 | PM, PPI2 | |
MAPK1 | 5594 | mitogen-activated protein kinase 1 | PM, PPI1 | |
MATK | 4145 | megakaryocyte-associated tyrosine kinase | PM, PPI1 | |
NEDD9 | 4739 | neural precursor cell expressed, developmentally down-regulated 9 | PPI1 | |
NOTCH2 | 4853 | notch 2 | DG | |
PIK3R1 | 5295 | phosphoinositide-3-kinase, regulatory subunit 1 (p85 alpha) | PM, PPI1 | For example, PX-866, BGT226, GDC-0941, XL765 |
PIK3R2 | 5296 | phosphoinositide-3-kinase, regulatory subunit 2 (p85 beta) | PM, PPI1 | |
PIN1 | 5300 | protein (peptidylprolyl cis/trans isomerase) NIMA-interacting 1 | PM | |
PKN2 | 5586 | protein kinase N2 | PM, PPI2 | |
PLSCR1 | 5359 | phospholipid scramblase 1 | PM, PPI1, MA | |
PPIA | 5478 | peptidylprolyl isomerase PG (cyclophilin PG) | C, PPI2 | |
PRKACB | 5567 | protein kinase, cAMP-dependent, catalytic, beta | PG | |
PRKCD | 5580 | protein kinase C, delta | PM, PPI1 | ruboxistaurin, enzastaurin, tamoxifen |
PRKCE | 5581 | protein kinase C, epsilon | PM, PPI2 | |
PRKCZ | 5590 | protein kinase C, zeta | PM, PPI2 | |
PTPRF | 5792 | protein tyrosine phosphatase, receptor type, F nexin-II, Alzheimer disease) | PPI1 | |
RAC1 | 5879 | ras-related C3 botulinum toxin substrate 1 (rho family, small GTP binding protein Rac1) | PM, PPI2 | |
RAPGEF1 | 2889 | Rap guanine nucleotide exchange factor (GEF) 1 | PPI1 | |
RASA3 | 22821 | RAS p21 protein activator 3 | DG | |
RET | 5979 | ret proto-oncogene | PPI1, M2 | valdetanib |
RPS6KA5 | 9252 | ribosomal protein S6 kinase, 90kDa, polypeptide 5 | PM | ruboxistaurin |
SC4MOL | 6307 | sterol-C4-methyl oxidase-like | MA | |
SH2D3C | 10044 | SH2 domain containing 3C | PM, PPI1 | |
SHC1 | 6464 | SHC (Src homology 2 domain containing) transforming protein 1 | PM, C, PPI1, DG | |
SMAD2 | 4087 | SMAD family member 2 | PM, PPI1 | peptide 144 targets TGFβ1RIII |
SOS2 | 6655 | son of sevenless homolog 2 (Drosophila) | PM, PPI1, DG | |
STAT3 | 6774 | signal transducer and activator of transcription | PM, C, PPI1 | STAT 3 decoy oligonucleotide |
TBL1Y | 90665 | 3 (acute-phase response factor) transducin (beta)-like 1Y-linked | DG | |
VAV3 | 10451 | vav 3 oncogene | PM, C, PPI1 |
Hits are listed alphabetically by Gene Symbol (Symbol). Entrez Gene ID (ID), description (including alternative common names), reason for inclusion in the library (Origin), and existence of any targeted small molecule agent (Clinical Agent) are also provided. C, found in a protein complex with seeds; DG, identified from Drosophila genetics; MA, microarray indicates transcriptionally responsive to EGFR; PG, paralog; PM, present in pathway maps; PPI1, direct protein interactions with seeds; PPI2, direct protein interactions with a protein within the PPI1 group.