Details of the Drug Combination

General Information of Drug Combination (ID: DCX9FPN)

• Drug Combination Name: (-)-englerin A + LY2523355
• Indication: Ewing sarcoma; Status: Investigative [1]
• Component Drugs:
  (-)-englerin A (DMPQBWY): Small molecular drug
  LY2523355 (DMCV602): Small molecular drug
• High-throughput Screening Result:
  Testing Cell Line: TC-71
  Zero Interaction Potency (ZIP) Score: 7.532
  Bliss Independence Score: 6.312
  Loewe Additivity Score: 3.298
  LHighest Single Agent (HSA) Score: 4.409

Molecular Interaction Atlas of This Drug Combination

Indication(s) of (-)-englerin A

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[2]

(-)-englerin A Interacts with 2 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Short transient receptor potential channel 5 (TRPC5)	TT32NQ1	TRPC5_HUMAN	Agonist	[4]
Short transient receptor potential channel 4 (TRPC4)	TTX0H5W	TRPC4_HUMAN	Agonist	[4]

Indication(s) of LY2523355

Disease Entry	ICD 11	Status	REF
Acute myeloid leukaemia	2A60	Phase 2	[3]

LY2523355 Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Kinesin-like protein KIF11 (KIF11)	TTTRP0H	KIF11_HUMAN	Modulator	[5]

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] Enantioselective synthesis of (-)-englerins A and B. Angew Chem Int Ed Engl. 2010 May 3;49(20):3517-9.
• [3] ClinicalTrials.gov (NCT01416389) A Study of LY2523355 in Patients With Breast Cancer. U.S. National Institutes of Health.
• [4] (-)-Englerin is a potent and selective activator of TRPC4 and TRPC5 calcium channels. Angew Chem Int Ed Engl. 2015 Mar 16;54(12):3787-91.
• [5] Kinesins and cancer. Nat Rev Cancer. 2012 Jul 24;12(8):527-39.