Details of the Drug Combination

General Information of Drug Combination (ID: DCYVERR)

Drug Combination Name
Fenretinide GDC-0980/RG7422
Indication
Disease Entry Status REF
Glioblastoma Investigative [1]
Component Drugs Fenretinide   DMRD5SP GDC-0980/RG7422   DMF3MV1
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL
High-throughput Screening Result Testing Cell Line: JHH-136
Zero Interaction Potency (ZIP) Score: 73.421
Bliss Independence Score: 70.803
Loewe Additivity Score: 7.684
LHighest Single Agent (HSA) Score: 10.276

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Fenretinide
Disease Entry ICD 11 Status REF
Macular degeneration 9B78.3 Phase 3 [2]
Lymphoma 2A80-2A86 Phase 2 [3]
Peripheral T-cell lymphoma 2A90.C Phase 2 [4]
Solid tumour/cancer 2A00-2F9Z Phase 2 [3]
Tumour 2A00-2F9Z Phase 1 [3]
Fenretinide Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Retinoic acid receptor (RAR) TTOD7B3 NOUNIPROTAC Modulator [14]
------------------------------------------------------------------------------------
Fenretinide Interacts with 1 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Metabolism [15]
------------------------------------------------------------------------------------
Fenretinide Interacts with 183 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Cytochrome P450 26A1 (CYP26A1) OTL1DFWV CP26A_HUMAN Increases Expression [16]
Class E basic helix-loop-helix protein 40 (BHLHE40) OTITX14U BHE40_HUMAN Increases Expression [17]
Krueppel-like factor 7 (KLF7) OTS3YVA0 KLF7_HUMAN Increases Expression [17]
Short-chain dehydrogenase/reductase 3 (DHRS3) OTSK1DTP DHRS3_HUMAN Increases Expression [17]
Low-density lipoprotein receptor (LDLR) OTH559LU LDLR_HUMAN Decreases Expression [17]
72 kDa type IV collagenase (MMP2) OT5NIWA2 MMP2_HUMAN Decreases Activity [17]
Interferon regulatory factor 1 (IRF1) OT43DI6J IRF1_HUMAN Increases Expression [17]
Bone morphogenetic protein 2 (BMP2) OT23T37S BMP2_HUMAN Increases Expression [17]
Aminopeptidase N (ANPEP) OTP3WYFD AMPN_HUMAN Decreases Activity [17]
E-selectin (SELE) OT33RZWY LYAM2_HUMAN Increases Expression [17]
Cyclic AMP-dependent transcription factor ATF-3 (ATF3) OTC1UOHP ATF3_HUMAN Increases Expression [17]
C-X-C motif chemokine 2 (CXCL2) OTEJCYMY CXCL2_HUMAN Increases Expression [17]
C-X-C motif chemokine 3 (CXCL3) OTSL94KH CXCL3_HUMAN Increases Expression [17]
Hematopoietic progenitor cell antigen CD34 (CD34) OT1MOFLZ CD34_HUMAN Decreases Expression [17]
Prostaglandin G/H synthase 2 (PTGS2) OT75U9M4 PGH2_HUMAN Increases Expression [17]
DNA damage-inducible transcript 3 protein (DDIT3) OTI8YKKE DDIT3_HUMAN Increases Expression [17]
Nuclear receptor-interacting protein 1 (NRIP1) OTIZOJQV NRIP1_HUMAN Increases Expression [17]
Heat shock-related 70 kDa protein 2 (HSPA2) OTSDET7B HSP72_HUMAN Decreases Expression [17]
C-C motif chemokine 20 (CCL20) OTUCJY4N CCL20_HUMAN Increases Expression [17]
Large neutral amino acids transporter small subunit 1 (SLC7A5) OT2WPVXD LAT1_HUMAN Increases Expression [17]
Trefoil factor 3 (TFF3) OTJJDRTU TFF3_HUMAN Decreases Expression [17]
CMP-N-acetylneuraminate-beta-galactosamide-alpha-2,3-sialyltransferase 1 (ST3GAL1) OTFCO8QX SIA4A_HUMAN Increases Expression [17]
Homocysteine-responsive endoplasmic reticulum-resident ubiquitin-like domain member 1 protein (HERPUD1) OT9EROL6 HERP1_HUMAN Increases Expression [17]
Retinoic acid-induced protein 3 (GPRC5A) OTPOCWR7 RAI3_HUMAN Increases Expression [17]
Semaphorin-3C (SEMA3C) OTEGUY7F SEM3C_HUMAN Increases Expression [17]
Growth/differentiation factor 15 (GDF15) OTWQN50N GDF15_HUMAN Increases Expression [17]
Protein DEPP1 (DEPP1) OTB36PHJ DEPP1_HUMAN Increases Expression [17]
DNA damage-inducible transcript 4 protein (DDIT4) OTHY8SY4 DDIT4_HUMAN Increases Expression [17]
E3 ubiquitin-protein ligase TRIM33 (TRIM33) OT0KS4J7 TRI33_HUMAN Increases Expression [17]
Protein phosphatase 1 regulatory subunit 3C (PPP1R3C) OTEU05TX PPR3C_HUMAN Decreases Expression [17]
Pirin (PIR) OT8ALXHU PIR_HUMAN Increases Expression [7]
Claudin-4 (CLDN4) OT9C4PZ4 CLD4_HUMAN Increases Expression [7]
Regulator of G-protein signaling 5 (RGS5) OTUY0Q2I RGS5_HUMAN Increases Expression [7]
Claudin-3 (CLDN3) OT71MN9S CLD3_HUMAN Increases Expression [7]
Double-strand-break repair protein rad21 homolog (RAD21) OTQS84ZF RAD21_HUMAN Decreases Expression [7]
Trafficking kinesin-binding protein 2 (TRAK2) OTXVA7FN TRAK2_HUMAN Increases Expression [7]
Securin (PTTG1) OTIMYS4W PTTG1_HUMAN Decreases Expression [7]
Alpha-crystallin B chain (CRYAB) OTY4JGYU CRYAB_HUMAN Increases Expression [7]
Plasminogen activator inhibitor 2 (SERPINB2) OT72QLZB PAI2_HUMAN Decreases Expression [7]
Non-histone chromosomal protein HMG-17 (HMGN2) OTN20MEF HMGN2_HUMAN Decreases Expression [7]
Cyclin-dependent kinase 1 (CDK1) OTW1SC2N CDK1_HUMAN Decreases Expression [7]
Amino acid transporter heavy chain SLC3A2 (SLC3A2) OTBR33M9 4F2_HUMAN Increases Expression [7]
Signal recognition particle 19 kDa protein (SRP19) OT8RP8JB SRP19_HUMAN Decreases Expression [7]
Fructose-bisphosphate aldolase C (ALDOC) OTEC13I5 ALDOC_HUMAN Increases Expression [7]
Histone H2A.Z (H2AZ1) OT3KJJNQ H2AZ_HUMAN Decreases Expression [7]
Proliferating cell nuclear antigen (PCNA) OTHZ1RIA PCNA_HUMAN Decreases Expression [7]
Cyclic AMP-dependent transcription factor ATF-4 (ATF4) OTRFV19J ATF4_HUMAN Increases Expression [7]
Lymphocyte function-associated antigen 3 (CD58) OTIUGMGS LFA3_HUMAN Decreases Expression [7]
Alanine--glyoxylate aminotransferase (AGXT) OTIPTH3Q AGT1_HUMAN Increases Expression [7]
Midkine (MDK) OTF24HKC MK_HUMAN Increases Expression [7]
Insulin-like growth factor-binding protein 5 (IGFBP5) OTRE5V0C IBP5_HUMAN Decreases Expression [7]
NKG2-C type II integral membrane protein (KLRC2) OTT4N86S NKG2C_HUMAN Increases Expression [7]
Peptidyl-prolyl cis-trans isomerase F, mitochondrial (PPIF) OTRA8ZVE PPIF_HUMAN Increases Expression [7]
Deoxyuridine 5'-triphosphate nucleotidohydrolase, mitochondrial (DUT) OT0THBVA DUT_HUMAN Decreases Expression [7]
Very long-chain specific acyl-CoA dehydrogenase, mitochondrial (ACADVL) OT50L4XB ACADV_HUMAN Increases Expression [7]
6-phosphogluconate dehydrogenase, decarboxylating (PGD) OTVG296F 6PGD_HUMAN Increases Expression [7]
Cysteine-rich protein 2 (CRIP2) OTVVJSYX CRIP2_HUMAN Decreases Expression [7]
Apolipoprotein C-IV (APOC4) OTE8ZUXY APOC4_HUMAN Decreases Expression [7]
Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-11 (GNG11) OTHIXBGW GBG11_HUMAN Decreases Expression [7]
ETS-related transcription factor Elf-3 (ELF3) OTUTLEQO ELF3_HUMAN Increases Expression [7]
Neutrophil gelatinase-associated lipocalin (LCN2) OTSB42BR NGAL_HUMAN Increases Expression [7]
Nucleobindin-2 (NUCB2) OTHO6JWN NUCB2_HUMAN Increases Expression [7]
Peptidyl-prolyl cis-trans isomerase FKBP4 (FKBP4) OTPV1D60 FKBP4_HUMAN Decreases Expression [7]
Aldo-keto reductase family 1 member C1 (AKR1C1) OTQKR4CM AK1C1_HUMAN Increases Expression [7]
Tumor protein D53 (TPD52L1) OTSA6U0I TPD53_HUMAN Increases Expression [7]
Single-stranded DNA-binding protein 4 (SSBP4) OTTK1ZHQ SSBP4_HUMAN Decreases Expression [7]
Microtubule-associated proteins 1A/1B light chain 3B (MAP1LC3B) OTUYHB84 MLP3B_HUMAN Increases Expression [7]
Nuclear ubiquitous casein and cyclin-dependent kinase substrate 1 (NUCKS1) OTL4VJC5 NUCKS_HUMAN Decreases Expression [7]
Heat shock protein beta-8 (HSPB8) OT0I83YS HSPB8_HUMAN Increases Expression [7]
BTB/POZ domain-containing protein KCTD3 (KCTD3) OT6EGR42 KCTD3_HUMAN Decreases Expression [7]
Methylated-DNA--protein-cysteine methyltransferase (MGMT) OT40A9WH MGMT_HUMAN Increases Expression [18]
Superoxide dismutase (SOD1) OT39TA1L SODC_HUMAN Increases Expression [19]
Glutathione peroxidase 1 (GPX1) OTE2O72Q GPX1_HUMAN Increases Expression [19]
Glucose-6-phosphate 1-dehydrogenase (G6PD) OT300SMK G6PD_HUMAN Increases Expression [19]
Glycogen synthase kinase-3 beta (GSK3B) OTL3L14B GSK3B_HUMAN Increases Phosphorylation [19]
Ribosomal protein S6 kinase alpha-2 (RPS6KA2) OTIOYUSU KS6A2_HUMAN Increases Phosphorylation [19]
Nuclear factor erythroid 2-related factor 2 (NFE2L2) OT0HENJ5 NF2L2_HUMAN Increases Expression [19]
Acyl carrier protein, mitochondrial (NDUFAB1) OTF906UR ACPM_HUMAN Affects Expression [8]
Tumor necrosis factor receptor superfamily member 10B (TNFRSF10B) OTA1CPBV TR10B_HUMAN Increases Expression [20]
Mitochondrial import inner membrane translocase subunit Tim23 (TIMM23) OTAAS85T TIM23_HUMAN Affects Expression [8]
NADH dehydrogenase 1 alpha subcomplex subunit 1 (NDUFA1) OTKBUQXP NDUA1_HUMAN Affects Expression [8]
CASP8 and FADD-like apoptosis regulator (CFLAR) OTX14BAS CFLAR_HUMAN Decreases Expression [21]
NADH dehydrogenase 1 beta subcomplex subunit 3 (NDUFB3) OTDV12IF NDUB3_HUMAN Affects Expression [8]
Germinal-center associated nuclear protein (MCM3AP) OT895FEC GANP_HUMAN Affects Expression [8]
Nuclear protein 1 (NUPR1) OT4FU8C0 NUPR1_HUMAN Affects Expression [22]
Protein phosphatase 1 regulatory subunit 15A (PPP1R15A) OTYG179K PR15A_HUMAN Increases Expression [22]
Isocitrate dehydrogenase cytoplasmic (IDH1) OT4DLHC8 IDHC_HUMAN Affects Expression [8]
PRA1 family protein 3 (ARL6IP5) OTYZ6BEQ PRAF3_HUMAN Affects Expression [23]
NADH dehydrogenase 1 beta subcomplex subunit 6 (NDUFB6) OTIXNT91 NDUB6_HUMAN Affects Expression [8]
NADH dehydrogenase 1 beta subcomplex subunit 2, mitochondrial (NDUFB2) OT4717TF NDUB2_HUMAN Affects Expression [8]
Brain mitochondrial carrier protein 1 (SLC25A14) OT1ZQSKS UCP5_HUMAN Increases Expression [8]
NADH dehydrogenase 1 alpha subcomplex subunit 10, mitochondrial (NDUFA10) OTBURQ3A NDUAA_HUMAN Affects Expression [8]
Mitochondrial import receptor subunit TOM40 homolog (TOMM40) OTZDQ29F TOM40_HUMAN Affects Expression [8]
L-lactate dehydrogenase A chain (LDHA) OTN7K4XB LDHA_HUMAN Decreases Expression [8]
Epidermal growth factor receptor (EGFR) OTAPLO1S EGFR_HUMAN Increases Expression [8]
Myc proto-oncogene protein (MYC) OTPV5LUK MYC_HUMAN Decreases Expression [24]
Retinol-binding protein 4 (RBP4) OTL9RBH5 RET4_HUMAN Affects Binding [25]
Cellular tumor antigen p53 (TP53) OTIE1VH3 P53_HUMAN Decreases Expression [24]
Insulin-like growth factor I (IGF1) OTIIZR61 IGF1_HUMAN Decreases Activity [26]
Eukaryotic translation initiation factor 2 subunit 1 (EIF2S1) OTM0GDTP IF2A_HUMAN Increases Phosphorylation [22]
Transcription factor Jun (JUN) OTCYBO6X JUN_HUMAN Increases Expression [27]
Keratin, type I cytoskeletal 18 (KRT18) OTVLQFIP K1C18_HUMAN Increases Expression [28]
Keratin, type II cytoskeletal 8 (KRT8) OTTM4X11 K2C8_HUMAN Increases Expression [28]
Retinoblastoma-associated protein (RB1) OTQJUJMZ RB_HUMAN Increases Expression [8]
DNA excision repair protein ERCC-1 (ERCC1) OTNPYQHI ERCC1_HUMAN Increases Expression [27]
Heme oxygenase 1 (HMOX1) OTC1W6UX HMOX1_HUMAN Increases Expression [29]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Decreases Cleavage [13]
Retinoic acid receptor alpha (RARA) OT192V9V RARA_HUMAN Increases Expression [26]
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Decreases Expression [24]
Microtubule-associated protein tau (MAPT) OTMTP2Z7 TAU_HUMAN Increases Expression [8]
Retinoic acid receptor beta (RARB) OT367U3E RARB_HUMAN Increases Expression [30]
Endoplasmic reticulum chaperone BiP (HSPA5) OTFUIRAO BIP_HUMAN Increases Expression [10]
Retinoic acid receptor gamma (RARG) OT8LHMDH RARG_HUMAN Decreases Expression [31]
Bifunctional methylenetetrahydrofolate dehydrogenase/cyclohydrolase, mitochondrial (MTHFD2) OT1LQSGX MTDC_HUMAN Affects Expression [8]
NAD(P)H dehydrogenase 1 (NQO1) OTZGGIVK NQO1_HUMAN Affects Expression [8]
NADH dehydrogenase 1 beta subcomplex subunit 7 (NDUFB7) OT2CHQQ1 NDUB7_HUMAN Affects Expression [8]
Glutathione peroxidase 2 (GPX2) OTXI2NTI GPX2_HUMAN Increases Expression [32]
Retinoic acid receptor RXR-alpha (RXRA) OTP1TBDM RXRA_HUMAN Increases Expression [8]
Neutrophil cytosol factor 2 (NCF2) OTAUW7L2 NCF2_HUMAN Increases Expression [27]
Cyclin-A2 (CCNA2) OTPHHYZJ CCNA2_HUMAN Decreases Expression [33]
Nuclear receptor subfamily 4immunitygroup A member 1 (NR4A1) OTGP6GA4 NR4A1_HUMAN Increases Expression [34]
Tyrosine-protein kinase JAK1 (JAK1) OT0X3D17 JAK1_HUMAN Increases Expression [27]
G1/S-specific cyclin-D1 (CCND1) OT8HPTKJ CCND1_HUMAN Decreases Expression [28]
Interleukin-4 receptor subunit alpha (IL4R) OTTXOTCW IL4RA_HUMAN Decreases Expression [8]
Growth arrest and DNA damage-inducible protein GADD45 alpha (GADD45A) OTDRV63V GA45A_HUMAN Increases Expression [8]
Paired box protein Pax-6 (PAX6) OTOC9876 PAX6_HUMAN Decreases Expression [12]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Increases Phosphorylation [35]
Calreticulin (CALR) OTYD2TR1 CALR_HUMAN Increases Expression [10]
Calnexin (CANX) OTYP1F6J CALX_HUMAN Increases Expression [10]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Increases Phosphorylation [35]
Retinoic acid receptor RXR-beta (RXRB) OTNPDXG2 RXRB_HUMAN Increases Expression [8]
Protein disulfide-isomerase A3 (PDIA3) OTHPQ0Q3 PDIA3_HUMAN Increases Expression [10]
Peroxisome proliferator-activated receptor gamma (PPARG) OTHMARHO PPARG_HUMAN Increases Activity [36]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Increases Expression [33]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Decreases Expression [13]
Caspase-2 (CASP2) OTUDYSPP CASP2_HUMAN Increases Activity [29]
Cyclin-dependent kinase inhibitor 2A (CDKN2A) OTN0ZWAE CDN2A_HUMAN Increases Expression [8]
Mitogen-activated protein kinase 8 (MAPK8) OTEREYS5 MK08_HUMAN Increases Activity [35]
Dual specificity mitogen-activated protein kinase kinase 4 (MAP2K4) OTZPZX11 MP2K4_HUMAN Increases Phosphorylation [35]
Cyclin-dependent kinase inhibitor 1B (CDKN1B) OTNY5LLZ CDN1B_HUMAN Increases Expression [37]
Dual specificity mitogen-activated protein kinase kinase 3 (MAP2K3) OTI2OREX MP2K3_HUMAN Increases Phosphorylation [35]
Retinoic acid receptor RXR-gamma (RXRG) OT254B09 RXRG_HUMAN Decreases Expression [8]
Glutamate--cysteine ligase catalytic subunit (GCLC) OTESDI4D GSH1_HUMAN Increases Expression [30]
Nuclear receptor subfamily 2 group C member 2 (NR2C2) OTDZWVOJ NR2C2_HUMAN Increases Expression [8]
Breast cancer type 2 susceptibility protein (BRCA2) OTF1XSV1 BRCA2_HUMAN Decreases Expression [8]
NADH dehydrogenase 1 alpha subcomplex subunit 8 (NDUFA8) OTBO0YKI NDUA8_HUMAN Affects Expression [8]
Dual specificity mitogen-activated protein kinase kinase 6 (MAP2K6) OTK13JKC MP2K6_HUMAN Increases Phosphorylation [35]
Paired mesoderm homeobox protein 1 (PRRX1) OTTZK5G8 PRRX1_HUMAN Increases Expression [8]
Caspase-7 (CASP7) OTAPJ040 CASP7_HUMAN Increases Activity [38]
Growth factor receptor-bound protein 2 (GRB2) OTOP7LTE GRB2_HUMAN Increases Expression [27]
Transcription factor A, mitochondrial (TFAM) OTXXV5V7 TFAM_HUMAN Affects Expression [8]
Heat shock factor protein 1 (HSF1) OTYNJ4KP HSF1_HUMAN Increases Activity [39]
E3 ubiquitin-protein ligase Mdm2 (MDM2) OTOVXARF MDM2_HUMAN Decreases Expression [8]
Apoptosis regulator BAX (BAX) OTAW0V4V BAX_HUMAN Increases Expression [13]
Bcl-2-like protein 1 (BCL2L1) OTRC5K9O B2CL1_HUMAN Decreases Expression [40]
Retinoblastoma-like protein 2 (RBL2) OTBQSOE6 RBL2_HUMAN Increases Expression [27]
Histone-binding protein RBBP4 (RBBP4) OTG3BT3M RBBP4_HUMAN Increases Expression [8]
TP53-binding protein 1 (TP53BP1) OTL8879S TP53B_HUMAN Increases Expression [8]
TNF receptor-associated factor 1 (TRAF1) OTTLM5RU TRAF1_HUMAN Decreases Expression [21]
Baculoviral IAP repeat-containing protein 2 (BIRC2) OTFXFREP BIRC2_HUMAN Decreases Expression [21]
Phorbol-12-myristate-13-acetate-induced protein 1 (PMAIP1) OTXEE550 APR_HUMAN Increases Expression [41]
Cyclin-dependent kinase 5 activator 1 (CDK5R1) OTJELWK0 CD5R1_HUMAN Decreases Expression [8]
Mitogen-activated protein kinase 14 (MAPK14) OT5TCO3O MK14_HUMAN Increases Activity [35]
Bcl-2-related protein A1 (BCL2A1) OTWRYSNA B2LA1_HUMAN Decreases Expression [21]
Bcl-2 homologous antagonist/killer (BAK1) OTDP6ILW BAK_HUMAN Increases Expression [20]
NADH dehydrogenase 1 alpha subcomplex subunit 5 (NDUFA5) OTR848KZ NDUA5_HUMAN Affects Expression [8]
NADH dehydrogenase 1 alpha subcomplex subunit 9, mitochondrial (NDUFA9) OTMKQJJ8 NDUA9_HUMAN Affects Expression [8]
DnaJ homolog subfamily C member 10 (DNAJC10) OTD2EG0R DJC10_HUMAN Increases Expression [10]
Leukocyte immunoglobulin-like receptor subfamily B member 2 (LILRB2) OT0HFPCD LIRB2_HUMAN Decreases Expression [8]
Bcl-2-binding component 3, isoforms 3/4 (BBC3) OTUAXDAY BBC3B_HUMAN Increases Expression [42]
BRCA1-associated RING domain protein 1 (BARD1) OTTC0Z9Y BARD1_HUMAN Decreases Expression [8]
Mitochondrial intermediate peptidase (MIPEP) OTB2IHCT MIPEP_HUMAN Affects Expression [8]
BAG family molecular chaperone regulator 1 (BAG1) OTRQNIA4 BAG1_HUMAN Affects Localization [12]
Eukaryotic translation initiation factor 2A (EIF2A) OTWXELQP EIF2A_HUMAN Increases Phosphorylation [10]
Apoptosis facilitator Bcl-2-like protein 14 (BCL2L14) OT87E7HW B2L14_HUMAN Increases Expression [8]
Isoleucine--tRNA ligase, mitochondrial (IARS2) OTDX4SCA SYIM_HUMAN Affects Expression [8]
RB-associated KRAB zinc finger protein (RBAK) OTYJ6EAU RBAK_HUMAN Increases Expression [8]
Mitochondrial carrier homolog 1 (MTCH1) OT0F9ADF MTCH1_HUMAN Affects Expression [8]
FAS-associated factor 1 (FAF1) OTGAMLM4 FAF1_HUMAN Decreases Expression [8]
Tumor necrosis factor ligand superfamily member 13B (TNFSF13B) OTND26XR TN13B_HUMAN Increases Expression [8]
Mediator of RNA polymerase II transcription subunit 16 (MED16) OT8SCI48 MED16_HUMAN Decreases Expression [8]
Eukaryotic translation initiation factor 2-alpha kinase 3 (EIF2AK3) OT0DZGY4 E2AK3_HUMAN Decreases Response To Substance [22]
Galactosylceramide sulfotransferase (GAL3ST1) OTSFFZRD G3ST1_HUMAN Decreases Response To Substance [37]
------------------------------------------------------------------------------------
⏷ Show the Full List of 183 DOT(s)
Indication(s) of GDC-0980/RG7422
Disease Entry ICD 11 Status REF
Non-hodgkin lymphoma 2B33.5 Phase 2 [5]
Solid tumour/cancer 2A00-2F9Z Phase 1 [6]
GDC-0980/RG7422 Interacts with 2 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Serine/threonine-protein kinase mTOR (mTOR) TTCJG29 MTOR_HUMAN Modulator [44]
PI3-kinase gamma (PIK3CG) TTHBTOP PK3CG_HUMAN Modulator [45]
------------------------------------------------------------------------------------
GDC-0980/RG7422 Interacts with 19 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PIK3CD) OTOMP6TH PK3CD_HUMAN Decreases Activity [45]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [45]
G1/S-specific cyclin-D1 (CCND1) OT8HPTKJ CCND1_HUMAN Decreases Expression [45]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Decreases Phosphorylation [45]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Decreases Phosphorylation [45]
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (PIK3CB) OTO8JQJA PK3CB_HUMAN Decreases Activity [45]
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (PIK3CG) OT3FAU4Y PK3CG_HUMAN Decreases Activity [45]
Hepatocyte growth factor receptor (MET) OT7K55MU MET_HUMAN Increases Expression [43]
Receptor tyrosine-protein kinase erbB-3 (ERBB3) OTRSST0A ERBB3_HUMAN Increases Expression [43]
Tuberin (TSC2) OT47LWI9 TSC2_HUMAN Decreases Phosphorylation [46]
Induced myeloid leukemia cell differentiation protein Mcl-1 (MCL1) OT2YYI1A MCL1_HUMAN Decreases Expression [43]
Eukaryotic translation initiation factor 4E-binding protein 1 (EIF4EBP1) OTHBQVD5 4EBP1_HUMAN Decreases Phosphorylation [46]
Cyclin-G2 (CCNG2) OTII38K2 CCNG2_HUMAN Increases Expression [43]
Atos homolog protein A (ATOSA) OTWFM5G0 ATOSA_HUMAN Increases Expression [43]
Phosphoinositide-3-kinase-interacting protein 1 (PIK3IP1) OTWE5G4T P3IP1_HUMAN Increases Expression [43]
Serine/threonine-protein kinase STK11 (STK11) OT1YZSP3 STK11_HUMAN Increases Response To Substance [43]
Epidermal growth factor receptor (EGFR) OTAPLO1S EGFR_HUMAN Increases Response To Substance [43]
Phosphatidylinositol 3,4,5-trisphosphate 3-phosphatase and dual-specificity protein phosphatase PTEN (PTEN) OTOWDUNT PTEN_HUMAN Increases Response To Substance [43]
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PIK3CA) OTTOMI8J PK3CA_HUMAN Increases Response To Substance [43]
------------------------------------------------------------------------------------
⏷ Show the Full List of 19 DOT(s)

References

1 Recurrent recessive mutation in deoxyguanosine kinase causes idiopathic noncirrhotic portal hypertension.Hepatology. 2016 Jun;63(6):1977-86. doi: 10.1002/hep.28499. Epub 2016 Mar 31.
2 ClinicalTrials.gov (NCT00003075) Fenretinide in Treating Patients With Cervical Neoplasia. U.S. National Institutes of Health.
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5 Clinical pipeline report, company report or official report of Roche.
6 Clinical pipeline report, company report or official report of Genentech (2011).
7 Regulation of lipocalin-2 gene by the cancer chemopreventive retinoid 4-HPR. Int J Cancer. 2006 Oct 1;119(7):1599-606.
8 4-HPR modulates gene expression in ovarian cells. Int J Cancer. 2006 Sep 1;119(5):1005-13. doi: 10.1002/ijc.21797.
9 Cholecalciferol (vitamin D3) and the retinoid N-(4-hydroxyphenyl)retinamide (4-HPR) are synergistic for chemoprevention of prostate cancer. J Exp Ther Oncol. 2006;5(4):323-33.
10 Targeting homeostatic mechanisms of endoplasmic reticulum stress to increase susceptibility of cancer cells to fenretinide-induced apoptosis: the role of stress proteins ERdj5 and ERp57. Br J Cancer. 2007 Apr 10;96(7):1062-71. doi: 10.1038/sj.bjc.6603672. Epub 2007 Mar 13.
11 [The role of reactive oxygen species in N-[4-hydroxyphenyl] retinamide induced apoptosis in bladder cancer cell lineT24]. Zhonghua Lao Dong Wei Sheng Zhi Ye Bing Za Zhi. 2005 Jun;23(3):191-4.
12 Fenretinide-induced neuronal differentiation of ARPE-19 human retinal pigment epithelial cells is associated with the differential expression of Hsp70, 14-3-3, pax-6, tubulin beta-III, NSE, and bag-1 proteins. Mol Vis. 2006 Nov 1;12:1355-63.
13 Anti-proliferative activity of fenretinide in human hepatoma cells in vitro and in vivo. Anticancer Drugs. 2007 Jan;18(1):47-53. doi: 10.1097/CAD.0b013e32800feeb5.
14 National Cancer Institute Drug Dictionary (drug id 39582).
15 Characterization of the metabolism of fenretinide by human liver microsomes, cytochrome P450 enzymes and UDP-glucuronosyltransferases. Br J Pharmacol. 2011 Feb;162(4):989-99.
16 Nuclear retinoid receptors are involved in N-(4-hydroxyphenyl) retinamide (Fenretinide)-induced gene expression and growth inhibition in HL-60 acute myeloid leukemia cells. Leuk Lymphoma. 2004 May;45(5):979-85.
17 The transforming growth factor-beta family members bone morphogenetic protein-2 and macrophage inhibitory cytokine-1 as mediators of the antiangiogenic activity of N-(4-hydroxyphenyl)retinamide. Clin Cancer Res. 2005 Jun 15;11(12):4610-9.
18 Increased expression of the MGMT repair protein mediated by cysteine prodrugs and chemopreventative natural products in human lymphocytes and tumor cell lines. Carcinogenesis. 2007 Feb;28(2):378-89.
19 Glycogen synthase kinase 3 regulates cell death and survival signaling in tumor cells under redox stress. Neoplasia. 2014 Sep;16(9):710-22.
20 Fenretinide up-regulates DR5/TRAIL-R2 expression via the induction of the transcription factor CHOP and combined treatment with fenretinide and TRAIL induces synergistic apoptosis in colon cancer cell lines. Int J Oncol. 2007 Mar;30(3):679-87.
21 N-(4-hydroxyphenyl)retinamide inhibits invasion, suppresses osteoclastogenesis, and potentiates apoptosis through down-regulation of I(kappa)B(alpha) kinase and nuclear factor-kappaB-regulated gene products. Cancer Res. 2005 Oct 15;65(20):9555-65. doi: 10.1158/0008-5472.CAN-05-1585.
22 Regulation of endoplasmic reticulum stress-induced cell death by ATF4 in neuroectodermal tumor cells. J Biol Chem. 2010 Feb 26;285(9):6091-100. doi: 10.1074/jbc.M109.014092. Epub 2009 Dec 18.
23 Comparing the effect of ATRA, 4-HPR, and CD437 in bladder cancer cells. Front Biosci. 2006 Sep 1;11:2007-16. doi: 10.2741/1942.
24 Regulation of apoptosis induced by the retinoid N-(4-hydroxyphenyl) retinamide and effect of deregulated bcl-2. Blood. 1995 Jan 15;85(2):359-67.
25 Fenretinide derivatives act as disrupters of interactions of serum retinol binding protein (sRBP) with transthyretin and the sRBP receptor. J Med Chem. 2011 Jul 14;54(13):4378-87. doi: 10.1021/jm200256g. Epub 2011 Jun 7.
26 Induction of apoptosis in primary meningioma cultures by fenretinide. Cancer Res. 2005 Feb 15;65(4):1547-53. doi: 10.1158/0008-5472.CAN-04-0786.
27 Identification of retinoid-modulated proteins in squamous carcinoma cells using high-throughput immunoblotting. Cancer Res. 2004 Apr 1;64(7):2439-48. doi: 10.1158/0008-5472.can-03-2643.
28 Novel retinoic acid metabolism blocking agents have potent inhibitory activities on human breast cancer cells and tumour growth. Br J Cancer. 2007 Apr 23;96(8):1204-15. doi: 10.1038/sj.bjc.6603705. Epub 2007 Mar 27.
29 N-(4-hydroxyphenyl)retinamide induces apoptosis in human retinal pigment epithelial cells: retinoic acid receptors regulate apoptosis, reactive oxygen species generation, and the expression of heme oxygenase-1 and Gadd153. J Cell Physiol. 2006 Dec;209(3):854-65. doi: 10.1002/jcp.20774.
30 Enrichment of Nur77 mediated by retinoic acid receptor leads to apoptosis of human hepatocellular carcinoma cells induced by fenretinide and histone deacetylase inhibitors. Hepatology. 2011 Mar;53(3):865-74. doi: 10.1002/hep.24101. Epub 2011 Feb 11.
31 Breast cancer progression in MCF10A series of cell lines is associated with alterations in retinoic acid and retinoid X receptors and with differential response to retinoids. Int J Oncol. 2004 Oct;25(4):961-71.
32 Expression of gastrointestinal glutathione peroxidase is inversely correlated to the presence of hepatitis C virus subgenomic RNA in human liver cells. J Biol Chem. 2005 Mar 11;280(10):8831-41. doi: 10.1074/jbc.M413730200. Epub 2004 Dec 28.
33 4-oxo-fenretinide, a recently identified fenretinide metabolite, induces marked G2-M cell cycle arrest and apoptosis in fenretinide-sensitive and fenretinide-resistant cell lines. Cancer Res. 2006 Mar 15;66(6):3238-47. doi: 10.1158/0008-5472.CAN-05-3362.
34 Induction and intracellular localization of Nur77 dictate fenretinide-induced apoptosis of human liver cancer cells. Biochem Pharmacol. 2010 Apr 1;79(7):948-54. doi: 10.1016/j.bcp.2009.11.004. Epub 2009 Nov 11.
35 N-(4-hydroxyphenyl)retinamide-induced apoptosis triggered by reactive oxygen species is mediated by activation of MAPKs in head and neck squamous carcinoma cells. Oncogene. 2006 May 4;25(19):2785-94. doi: 10.1038/sj.onc.1209303.
36 PPAR activation and decreased proliferation in oral carcinoma cells with 4-HPR. Otolaryngol Head Neck Surg. 2005 Nov;133(5):695-701. doi: 10.1016/j.otohns.2005.07.019.
37 Inhibitory effects of N-(4-hydrophenyl) retinamide on liver cancer and malignant melanoma cells. World J Gastroenterol. 2005 Oct 7;11(37):5763-9. doi: 10.3748/wjg.v11.i37.5763.
38 Mechanism of 4-HPR-induced apoptosis in glioma cells: evidences suggesting role of mitochondrial-mediated pathway and endoplasmic reticulum stress. Carcinogenesis. 2006 Oct;27(10):2047-58. doi: 10.1093/carcin/bgl051. Epub 2006 May 4.
39 A Gene Expression Biomarker Predicts Heat Shock Factor 1 Activation in a Gene Expression Compendium. Chem Res Toxicol. 2021 Jul 19;34(7):1721-1737. doi: 10.1021/acs.chemrestox.0c00510. Epub 2021 Jun 25.
40 Retinamide-induced apoptosis in glioblastomas is associated with down-regulation of Bcl-xL and Bcl-2 proteins. J Neurooncol. 2005 Sep;74(3):225-32. doi: 10.1007/s11060-005-7305-z.
41 Role of Noxa in p53-independent fenretinide-induced apoptosis of neuroectodermal tumours. Apoptosis. 2007 Mar;12(3):613-22. doi: 10.1007/s10495-006-0020-1.
42 BBC3 mediates fenretinide-induced cell death in neuroblastoma. Oncogene. 2005 Dec 1;24(54):7976-83. doi: 10.1038/sj.onc.1208947.
43 Phosphoinositide 3-kinase (PI3K) pathway alterations are associated with histologic subtypes and are predictive of sensitivity to PI3K inhibitors in lung cancer preclinical models. Clin Cancer Res. 2012 Dec 15;18(24):6771-83. doi: 10.1158/1078-0432.CCR-12-2347. Epub 2012 Nov 7.
44 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2109).
45 GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway. Mol Cancer Ther. 2011 Dec;10(12):2426-36.
46 Modulation of Akt/mTOR signaling overcomes sunitinib resistance in renal and prostate cancer cells. Mol Cancer Ther. 2012 Jul;11(7):1510-7. doi: 10.1158/1535-7163.MCT-11-0907. Epub 2012 Apr 24.