Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMXSYTA)

• Drug Name: CPI-203 Drug Info
• Synonyms: CPI203; CPI 203

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 71291068
  ChEBI ID: CHEMBL4303293
  TTD Drug ID: DMXSYTA

Molecule-Related Drug Atlas

Drug(s) Targeting Bromodomain-containing protein 4 (BRD4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CPI-0610	DMPXOYJ	Myelofibrosis	2A20.2	Phase 3	[4]
OTX-015	DMI8RG1	Acute myeloid leukaemia	2A60	Phase 1/2	[4]
PLX2853	DMX168L	Acute myeloid leukaemia	2A60	Phase 1/2	[5]
RVX-208	DM1LO8K	Alzheimer disease	8A20	Phase 1/2	[4]
INCB57643	DMBGU7V	Advanced malignancy	2A00-2F9Z	Phase 1/2	[5]
ABBV-744	DMTEA9C	Acute myeloid leukaemia	2A60	Phase 1	[5]
(+)-JQ1	DM1CZSJ	Testicular cancer	2C80	Phase 1	[6]
GSK525762	DMPAWBN	Haematological malignancy	2B33.Y	Phase 1	[4]
TEN010	DM4UOY5	Advanced solid tumour	2A00-2F9Z	Phase 1	[4]
AZD5153	DMW4GM2	Solid tumour/cancer	2A00-2F9Z	Phase 1	[5]

Drug(s) Affected By Heat shock factor protein 1 (HSF1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[7]
SPI-1005	DM6XFHS	Reperfusion injury	ND56.Z	Approved	[3]
Imipramine	DM2NUH3	Depression	6A70-6A7Z	Approved	[3]
Sulindac	DM2QHZU	Acute myelogenous leukaemia	2A41	Approved	[8]
Simvastatin	DM30SGU	Arteriosclerosis	BD40	Approved	[9]
Ceftazidime	DM41GRA	Bacteremia	1A73	Approved	[3]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[10]
Chlorpheniramine	DM5URA2	Allergic rhinitis	CA08.0	Approved	[3]
Ethacrynic acid	DM60QMR	Edema	MG29	Approved	[3]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[3]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Bromodomain-containing protein 4 (BRD4)	TTRA6BO	BRD4_HUMAN	Inhibitor	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Heat shock factor protein 1 (HSF1)	OTYNJ4KP	HSF1_HUMAN	Gene/Protein Processing	[3]

References

• [1] 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. (Ligand id: 7513).
• [2] BRD4 is an atypical kinase that phosphorylates serine2 of the RNA polymerase II carboxy-terminal domain. Proc Natl Acad Sci U S A. 2012 May 1;109(18):6927-32.
• [3] 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.
• [4] Targeting bromodomains: epigenetic readers of lysine acetylation.Nat Rev Drug Discov.2014 May;13(5):337-56.
• [5] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [6] Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73.
• [7] NRF2 transcriptionally activates the heat shock factor 1 promoter under oxidative stress and affects survival and migration potential of MCF7 cells. J Biol Chem. 2018 Dec 14;293(50):19303-19316. doi: 10.1074/jbc.RA118.003376. Epub 2018 Oct 11.
• [8] Non-steroidal anti-inflammatory drugs inhibit the expression of cytokines and induce HSP70 in human monocytes. Cytokine. 1999 May;11(5):347-58. doi: 10.1006/cyto.1998.0437.
• [9] Simvastatin induces heat shock factor 1 in vascular endothelial cells. Atherosclerosis. 2006 Oct;188(2):265-73. doi: 10.1016/j.atherosclerosis.2005.10.045. Epub 2005 Dec 20.
• [10] Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.