Details of the Drug Combination

General Information of Drug Combination (ID: DCQH7NC)

Drug Combination Name
NVP-AUY922 BIX-01294
Indication
Disease Entry Status REF
Hepatoblastoma Investigative [1]
Component Drugs NVP-AUY922   DMTYXQF BIX-01294   DM5CBNY
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL is unavailable
High-throughput Screening Result Testing Cell Line: HB3
Zero Interaction Potency (ZIP) Score: 1.958
Bliss Independence Score: 2.056
Loewe Additivity Score: 0.055
LHighest Single Agent (HSA) Score: 1.016

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of NVP-AUY922
Disease Entry ICD 11 Status REF
Multiple myeloma 2A83 Phase 2 [2]
Solid tumour/cancer 2A00-2F9Z Phase 2 [3]
NVP-AUY922 Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Heat shock protein 90 alpha (HSP90A) TT78R5H HS90A_HUMAN Inhibitor [6]
------------------------------------------------------------------------------------
NVP-AUY922 Interacts with 35 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Anterior gradient protein 2 homolog (AGR2) OTRRZT7W AGR2_HUMAN Increases Expression [5]
Epidermal growth factor receptor (EGFR) OTAPLO1S EGFR_HUMAN Decreases Expression [7]
Fibroblast growth factor 1 (FGF1) OT8I64X8 FGF1_HUMAN Decreases Expression [5]
ATP synthase subunit beta, mitochondrial (ATP5F1B) OTLFZUQK ATPB_HUMAN Decreases Expression [5]
Insulin-like growth factor 1 receptor (IGF1R) OTXJIF13 IGF1R_HUMAN Decreases Expression [7]
Hepatocyte growth factor receptor (MET) OT7K55MU MET_HUMAN Decreases Expression [7]
Platelet-derived growth factor receptor beta (PDGFRB) OTYSNK9Q PGFRB_HUMAN Decreases Expression [7]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [7]
Heat shock 70 kDa protein 1A (HSPA1A) OTKGIE76 HS71A_HUMAN Increases Expression [5]
Mast/stem cell growth factor receptor Kit (KIT) OTHUY3VZ KIT_HUMAN Decreases Expression [7]
S-formylglutathione hydrolase (ESD) OTUSIBPS ESTD_HUMAN Increases Expression [5]
Elongation factor 2 (EEF2) OTZ7SZ39 EF2_HUMAN Increases Expression [5]
Pyruvate kinase PKM (PKM) OTLHHMC2 KPYM_HUMAN Decreases Expression [5]
Serine/threonine-protein kinase B-raf (BRAF) OT7S81XQ BRAF_HUMAN Decreases Expression [7]
NAD(P)H dehydrogenase 1 (NQO1) OTZGGIVK NQO1_HUMAN Decreases Expression [5]
Intron Large complex component GCFC2 (GCFC2) OTC7FRXL GCFC2_HUMAN Increases Expression [5]
Proteasome subunit alpha type-1 (PSMA1) OTNBVM2U PSA1_HUMAN Increases Expression [5]
NF-kappa-B inhibitor alpha (NFKBIA) OTFT924M IKBA_HUMAN Affects Phosphorylation [7]
M-phase inducer phosphatase 3 (CDC25C) OTPQI71S MPIP3_HUMAN Decreases Expression [7]
RAC-alpha serine/threonine-protein kinase (AKT1) OT8H2YY7 AKT1_HUMAN Decreases Expression [7]
Radixin (RDX) OTNSYUN6 RADI_HUMAN Increases Expression [5]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Increases Cleavage [7]
Serpin H1 (SERPINH1) OTKGI7BS SERPH_HUMAN Decreases Expression [5]
Small ubiquitin-related modifier 3 (SUMO3) OTTUJQJ1 SUMO3_HUMAN Decreases Expression [5]
Peptidyl-prolyl cis-trans isomerase A (PPIA) OTHJMWQQ PPIA_HUMAN Increases Expression [5]
Echinoderm microtubule-associated protein-like 5 (EML5) OT0EFCPB EMAL5_HUMAN Increases Expression [5]
Interleukin enhancer-binding factor 3 (ILF3) OTKMZ5K5 ILF3_HUMAN Decreases Expression [5]
Eukaryotic translation initiation factor 3 subunit I (EIF3I) OTE07WND EIF3I_HUMAN Decreases Expression [5]
3-hydroxyacyl-CoA dehydrogenase type-2 (HSD17B10) OT7RJON4 HCD2_HUMAN Decreases Expression [5]
Phenylalanine--tRNA ligase beta subunit (FARSB) OT8N9TT5 SYFB_HUMAN Increases Expression [5]
Protein PALS2 (PALS2) OTV12NKE PALS2_HUMAN Increases Expression [5]
Cingulin (CGN) OTBCQ8AQ CING_HUMAN Decreases Expression [5]
Poly polymerase 2 (PARP2) OTYL81ZI PARP2_HUMAN Increases Expression [5]
Hypoxia up-regulated protein 1 (HYOU1) OTBGBSOV HYOU1_HUMAN Decreases Expression [5]
Phosphoserine aminotransferase (PSAT1) OTVV1YV9 SERC_HUMAN Increases Expression [5]
------------------------------------------------------------------------------------
⏷ Show the Full List of 35 DOT(s)
Indication(s) of BIX-01294
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Preclinical [4]
BIX-01294 Interacts with 2 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Euchromatic histone-lysine N-methyltransferase 1 (EHMT1) TTOFXD7 EHMT1_HUMAN Inhibitor [8]
Histone-lysine N-methyltransferase EHMT2 (EHMT2) TTS6RZT EHMT2_HUMAN Inhibitor [8]
------------------------------------------------------------------------------------
BIX-01294 Interacts with 2 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Interferon alpha-2 (IFNA2) OT4GII73 IFNA2_HUMAN Increases Response To Substance [9]
Interferon regulatory factor 7 (IRF7) OTC1A2PQ IRF7_HUMAN Increases Expression [9]
------------------------------------------------------------------------------------

References

1 Loss of function mutations in VARS encoding cytoplasmic valyl-tRNA synthetase cause microcephaly, seizures, and progressive cerebral atrophy.Hum Genet. 2018 Apr;137(4):293-303. doi: 10.1007/s00439-018-1882-3. Epub 2018 Apr 24.
2 ClinicalTrials.gov (NCT01854034) Phase 2 Study of AUY922 in NSCLC Patients With Exon 20 Insertion Mutations in EGFR. U.S. National Institutes of Health.
3 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027019)
4 Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease. Nat Rev Drug Discov. 2021 Apr;20(4):265-286.
5 Impact of Heat Shock Protein 90 Inhibition on the Proteomic Profile of Lung Adenocarcinoma as Measured by Two-Dimensional Electrophoresis Coupled with Mass Spectrometry. Cells. 2019 Jul 31;8(8):806. doi: 10.3390/cells8080806.
6 Recent advances in Hsp90 inhibitors as antitumor agents. Anticancer Agents Med Chem. 2008 Oct;8(7):761-82.
7 Gene expression-based chemical genomics identifies heat-shock protein 90 inhibitors as potential therapeutic drugs in cholangiocarcinoma. Cancer. 2013 Jan 15;119(2):293-303. doi: 10.1002/cncr.27743. Epub 2012 Jul 18.
8 Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol Cell. 2007 Feb 9;25(3):473-81.
9 Inhibition of euchromatic histone methyltransferase 1 and 2 sensitizes chronic myeloid leukemia cells to interferon treatment. PLoS One. 2014 Jul 31;9(7):e103915. doi: 10.1371/journal.pone.0103915. eCollection 2014.