Details of the Drug Combination

General Information of Drug Combination (ID: DCTNSAI)

Drug Combination Name
Pepstatin PFK-158
Indication
Disease Entry Status REF
Chronic myelogenous leukemia Investigative [1]
Component Drugs Pepstatin   DM9S1EA PFK-158   DMIR21F
Small molecular drug N.A.
2D MOL 2D MOL
3D MOL is unavailable 3D MOL
High-throughput Screening Result Testing Cell Line: KBM-7
Zero Interaction Potency (ZIP) Score: 19.86
Bliss Independence Score: 19.86
Loewe Additivity Score: 30.82
LHighest Single Agent (HSA) Score: 30.82

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Pepstatin
Disease Entry ICD 11 Status REF
Malaria 1F40-1F45 Terminated [2]
Pepstatin Interacts with 4 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Plasmodium Cysteine protease falcipain-2 (Malaria CPF2) TT7EASG Q9N6S8_PLAFA Inhibitor [4]
Plasmodium Plasmepsin 2 (Malaria PLA2) TTXMNHO PLM2_PLAFA Inhibitor [5]
Plasmodium Plasmepsin 1 (Malaria PLA1) TTH9VL3 PLM1_PLAFA Inhibitor [5]
Plasmodium Cysteine protease falcipain (Malaria CPF) TTJNPTK NOUNIPROTAC Inhibitor [5]
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Pepstatin Interacts with 1 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Cathepsin D (CTSD) OTQZ36F3 CATD_HUMAN Decreases Activity [6]
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Indication(s) of PFK-158
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Phase 1 [3]
PFK-158 Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Renal carcinoma antigen NY-REN-56 (PFKFB3) TTTHMQJ F263_HUMAN Inhibitor [7]
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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 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004280)
3 ClinicalTrials.gov (NCT02044861) Phase 1 Safety Study of ACT-PFK-158, 2HCl in Patients With Advanced Solid Malignancies. U.S. National Institutes of Health.
4 Novel molecular targets for antimalarial drug development. Chem Biol Drug Des. 2008 Apr;71(4):287-97.
5 Novel molecular targets for antimalarial chemotherapy. Int J Antimicrob Agents. 2007 Jul;30(1):4-10.
6 Evidence of a lysosomal pathway for apoptosis induced by the synthetic retinoid CD437 in human leukemia HL-60 cells. Cell Death Differ. 2001 May;8(5):477-85. doi: 10.1038/sj.cdd.4400843.
7 Discovery of a PFKFB3 inhibitor for phase I trial testing that synergizes with the B-Raf inhibitor vemurafenib. Cancer Metab. 2014; 2(Suppl 1): P14.