General Information of Drug Combination (ID: DCVLGBA)

Drug Combination Name
Bafilomycin A1 GDC-0077
Indication
Disease Entry Status REF
DD2 Investigative [1]
Component Drugs Bafilomycin A1   DMUNK59 GDC-0077   DMY6WUV
Small molecular drug N.A.
2D MOL 2D MOL
3D MOL 3D MOL
High-throughput Screening Result Testing Cell Line: DD2
Zero Interaction Potency (ZIP) Score: 10.281
Bliss Independence Score: 1.519
Loewe Additivity Score: 3.932
LHighest Single Agent (HSA) Score: 0.034

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Bafilomycin A1
Disease Entry ICD 11 Status REF
B-cell acute lymphoblastic leukaemia 2B33.3 Investigative [2]
Bafilomycin A1 Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Vacuolar-type proton ATPase (v-ATPase) TTTK3BH NOUNIPROTAC Inhibitor [6]
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Bafilomycin A1 Interacts with 24 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Apoptotic protease-activating factor 1 (APAF1) OTJWIVY0 APAF_HUMAN Increases Expression [7]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Increases Expression [7]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Increases Expression [7]
Steroidogenic factor 1 (NR5A1) OTOULYR4 STF1_HUMAN Decreases Expression [8]
Nuclear factor erythroid 2-related factor 2 (NFE2L2) OT0HENJ5 NF2L2_HUMAN Increases Expression [9]
Zinc finger protein SNAI1 (SNAI1) OTDPYAMC SNAI1_HUMAN Increases Expression [5]
Albumin (ALB) OTVMM513 ALBU_HUMAN Decreases Uptake [10]
Cathepsin D (CTSD) OTQZ36F3 CATD_HUMAN Decreases Cleavage [11]
Procathepsin L (CTSL) OTYTUW29 CATL1_HUMAN Decreases Cleavage [11]
Heme oxygenase 1 (HMOX1) OTC1W6UX HMOX1_HUMAN Decreases Expression [12]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [13]
Gap junction alpha-1 protein (GJA1) OTT94MKL CXA1_HUMAN Increases Expression [14]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Decreases Activity [15]
Caspase-4 (CASP4) OTVQTV1L CASP4_HUMAN Increases Activity [16]
Microsomal triglyceride transfer protein large subunit (MTTP) OTNUVSDT MTP_HUMAN Increases Expression [17]
Caspase-7 (CASP7) OTAPJ040 CASP7_HUMAN Decreases Activity [15]
BH3-interacting domain death agonist (BID) OTOSHSHU BID_HUMAN Increases Cleavage [18]
BCL2/adenovirus E1B 19 kDa protein-interacting protein 3 (BNIP3) OT4SO7J4 BNIP3_HUMAN Increases Expression [15]
Sequestosome-1 (SQSTM1) OTGY5D5J SQSTM_HUMAN Increases Expression [19]
Hypoxia-inducible factor 1-alpha (HIF1A) OTADSC03 HIF1A_HUMAN Increases Expression [15]
NACHT, LRR and PYD domains-containing protein 3 (NLRP3) OTZM6MHU NLRP3_HUMAN Increases Expression [5]
Microtubule-associated proteins 1A/1B light chain 3B (MAP1LC3B) OTUYHB84 MLP3B_HUMAN Increases Cleavage [20]
Microtubule-associated proteins 1A/1B light chain 3A (MAP1LC3A) OTPMGIU4 MLP3A_HUMAN Increases Expression [21]
Leucine-rich repeat serine/threonine-protein kinase 2 (LRRK2) OTLS7C99 LRRK2_HUMAN Increases Response To Substance [22]
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⏷ Show the Full List of 24 DOT(s)
Indication(s) of GDC-0077
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Phase 2 [3]
Breast cancer 2C60-2C65 Phase 1 [4]
GDC-0077 Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
PI3-kinase gamma (PIK3CG) TTHBTOP PK3CG_HUMAN Inhibitor [4]
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References

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2 Bafilomycin A1 targets both autophagy and apoptosis pathways in pediatric B-cell acute lymphoblastic leukemia. Haematologica. 2015 Mar;100(3):345-56.
3 ClinicalTrials.gov (NCT04632992) A Study Evaluating Targeted Therapies in Participants Who Have Advanced Solid Tumors With Genomic Alterations or Protein Expression Patterns Predictive of Response (MyTACTIC). U.S. National Institutes of Health.
4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
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6 Molecular basis of V-ATPase inhibition by bafilomycin A1. Nat Commun. 2021 Mar 19;12(1):1782.
7 Nano-sized iron particles may induce multiple pathways of cell death following generation of mistranscripted RNA in human corneal epithelial cells. Toxicol In Vitro. 2017 Aug;42:348-357.
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10 Chronic high glucose inhibits albumin reabsorption by lysosomal alkalinization in cultured porcine proximal tubular epithelial cells (LLC-PK1). Diabetes Res Clin Pract. 2006 Jun;72(3):223-30. doi: 10.1016/j.diabres.2005.10.019. Epub 2005 Nov 28.
11 Berbamine Hydrochloride inhibits lysosomal acidification by activating Nox2 to potentiate chemotherapy-induced apoptosis via the ROS-MAPK pathway in human lung carcinoma cells. Cell Biol Toxicol. 2023 Aug;39(4):1297-1317. doi: 10.1007/s10565-022-09756-8. Epub 2022 Sep 7.
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14 GJA1 reverses arsenic-induced EMT via modulating MAPK/ERK signaling pathway. Toxicol Appl Pharmacol. 2022 Sep 1;450:116138. doi: 10.1016/j.taap.2022.116138. Epub 2022 Jun 21.
15 Combined effects of EGFR tyrosine kinase inhibitors and vATPase inhibitors in NSCLC cells. Toxicol Appl Pharmacol. 2015 Aug 15;287(1):17-25. doi: 10.1016/j.taap.2015.05.001. Epub 2015 May 14.
16 Autophagy induction by capsaicin in malignant human breast cells is modulated by p38 and extracellular signal-regulated mitogen-activated protein kinases and retards cell death by suppressing endoplasmic reticulum stress-mediated apoptosis. Mol Pharmacol. 2010 Jul;78(1):114-25. doi: 10.1124/mol.110.063495. Epub 2010 Apr 6.
17 Cadmium induces triglyceride levels via microsomal triglyceride transfer protein (MTTP) accumulation caused by lysosomal deacidification regulated by endoplasmic reticulum (ER) Ca(2+) homeostasis. Chem Biol Interact. 2021 Oct 1;348:109649. doi: 10.1016/j.cbi.2021.109649. Epub 2021 Sep 10.
18 Inhibition of cholesterol metabolism underlies synergy between mTOR pathway inhibition and chloroquine in bladder cancer cells. Oncogene. 2016 Aug 25;35(34):4518-28. doi: 10.1038/onc.2015.511. Epub 2016 Feb 8.
19 Resveratrol-activated AMPK/SIRT1/autophagy in cellular models of Parkinson's disease. Neurosignals. 2011;19(3):163-74. doi: 10.1159/000328516. Epub 2011 Jul 22.
20 LncRNA UCA1 attenuates autophagy-dependent cell death through blocking autophagic flux under arsenic stress. Toxicol Lett. 2018 Mar 1;284:195-204. doi: 10.1016/j.toxlet.2017.12.009. Epub 2017 Dec 15.
21 Transcriptomic Landscape of Cisplatin-Resistant Neuroblastoma Cells. Cells. 2019 Mar 12;8(3):235. doi: 10.3390/cells8030235.
22 G2019S LRRK2 mutant fibroblasts from Parkinson's disease patients show increased sensitivity to neurotoxin 1-methyl-4-phenylpyridinium dependent of autophagy. Toxicology. 2014 Oct 3;324:1-9. doi: 10.1016/j.tox.2014.07.001. Epub 2014 Jul 10.