Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTHE657)

• DTT Name: Bromodomain-containing protein 3 (BRD3)
• Synonyms: RING3like protein; RING3L; RING3-like protein; KIAA0043
• Gene Name: BRD3
• DTT Type: Clinical trial target; [1]
• BioChemical Class: Bromodomain
• UniProt ID: BRD3_HUMAN
• TTD ID: T42048
• Sequence:
  MSTATTVAPAGIPATPGPVNPPPPEVSNPSKPGRKTNQLQYMQNVVVKTLWKHQFAWPFY
  QPVDAIKLNLPDYHKIIKNPMDMGTIKKRLENNYYWSASECMQDFNTMFTNCYIYNKPTD
  DIVLMAQALEKIFLQKVAQMPQEEVELLPPAPKGKGRKPAAGAQSAGTQQVAAVSSVSPA
  TPFQSVPPTVSQTPVIAATPVPTITANVTSVPVPPAAAPPPPATPIVPVVPPTPPVVKKK
  GVKRKADTTTPTTSAITASRSESPPPLSDPKQAKVVARRESGGRPIKPPKKDLEDGEVPQ
  HAGKKGKLSEHLRYCDSILREMLSKKHAAYAWPFYKPVDAEALELHDYHDIIKHPMDLST
  VKRKMDGREYPDAQGFAADVRLMFSNCYKYNPPDHEVVAMARKLQDVFEMRFAKMPDEPV
  EAPALPAPAAPMVSKGAESSRSSEESSSDSGSSDSEEERATRLAELQEQLKAVHEQLAAL
  SQAPVNKPKKKKEKKEKEKKKKDKEKEKEKHKVKAEEEKKAKVAPPAKQAQQKKAPAKKA
  NSTTTAGRQLKKGGKQASASYDSEEEEEGLPMSYDEKRQLSLDINRLPGEKLGRVVHIIQ
  SREPSLRDSNPDEIEIDFETLKPTTLRELERYVKSCLQKKQRKPFSASGKKQAAKSKEEL
  AQEKKKELEKRLQDVSGQLSSSKKPARKEKPGSAPSGGPSRLSSSSSSESGSSSSSGSSS
  DSSDSE
• Function: Regulates transcription by promoting the binding of the transcription factor GATA1 to its targets. Chromatin reader that recognizes and binds hyperacetylated chromatin and plays a role in the regulation of transcription, probably by chromatin remodeling and interaction with transcription factors.

Molecular Interaction Atlas (MIA) of This DTT

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ABBV-744	DMTEA9C	Acute myeloid leukaemia	2A60	Phase 1	[1]

5 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID26924192-Compound-102	DMEJ107	N. A.	N. A.	Patented	[2]
PMID26924192-Compound-103	DMWOCP7	N. A.	N. A.	Patented	[2]
PMID26924192-Compound-104	DM346EU	N. A.	N. A.	Patented	[2]
PMID26924192-Compound-105	DMAWLGI	N. A.	N. A.	Patented	[2]
Pyrrolo-pyrrolone derivative 1	DMN4SE5	N. A.	N. A.	Patented	[2]

5 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
GW841819X	DMRL9IN	Discovery agent	N.A.	Investigative	[3]
I-BET151	DMYRUH2	Discovery agent	N.A.	Investigative	[4]
PMID24000170C36	DMHUWZS	Discovery agent	N.A.	Investigative	[5]
PMID24000170C38	DMOLRIY	Discovery agent	N.A.	Investigative	[5]
XD14	DMUMACD	Discovery agent	N.A.	Investigative	[6]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Myelodysplastic syndrome	2C82	Bone marrow	8.51E-01	-0.03	-0.13

References

• [1] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [2] BET inhibitors in cancer therapeutics: a patent review.Expert Opin Ther Pat. 2016;26(4):505-22.
• [3] Discovery and characterization of small molecule inhibitors of the BET family bromodomains. J Med Chem. 2011 Jun 9;54(11):3827-38.
• [4] Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature. 2011 Oct 2;478(7370):529-33.
• [5] Naphthyridines as novel BET family bromodomain inhibitors. ChemMedChem. 2014 Mar;9(3):580-9.
• [6] 4-Acyl pyrroles: mimicking acetylated lysines in histone code reading. Angew Chem Int Ed Engl. 2013 Dec 23;52(52):14055-9.