Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTKZH9PO)

DOT Name Bromodomain-containing protein 9 (BRD9)
Synonyms Rhabdomyosarcoma antigen MU-RMS-40.8
Gene Name BRD9
UniProt ID
BRD9_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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PDB ID
3HME ; 4NQN ; 4UIT ; 4UIU ; 4UIV ; 4UIW ; 4XY8 ; 4YY4 ; 4YY6 ; 4YYD ; 4YYG ; 4YYH ; 4YYI ; 4YYJ ; 4YYK ; 4Z6H ; 4Z6I ; 5E9V ; 5EU1 ; 5F1H ; 5F1L ; 5F25 ; 5F2P ; 5I40 ; 5I7X ; 5I7Y ; 5IGM ; 5IGN ; 5JI8 ; 5MKY ; 5TWX ; 6BQA ; 6HM0 ; 6UZF ; 6V0S ; 6V0X ; 6V14 ; 6V1B ; 6Y7H ; 6Y7I ; 6Y7J ; 6Y7K ; 6Y7L ; 6YQR ; 6YQS ; 6YQW ; 8A7I ; 8AHC
Pfam ID
PF00439 ; PF12024
Sequence
MGKKHKKHKAEWRSSYEDYADKPLEKPLKLVLKVGGSEVTELSGSGHDSSYYDDRSDHER
ERHKEKKKKKKKKSEKEKHLDDEERRKRKEEKKRKREREHCDTEGEADDFDPGKKVEVEP
PPDRPVRACRTQPAENESTPIQQLLEHFLRQLQRKDPHGFFAFPVTDAIAPGYSMIIKHP
MDFGTMKDKIVANEYKSVTEFKADFKLMCDNAMTYNRPDTVYYKLAKKILHAGFKMMSKQ
AALLGNEDTAVEEPVPEVVPVQVETAKKSKKPSREVISCMFEPEGNACSLTDSTAEEHVL
ALVEHAADEARDRINRFLPGGKMGYLKRNGDGSLLYSVVNTAEPDADEEETHPVDLSSLS
SKLLPGFTTLGFKDERRNKVTFLSSATTALSMQNNSVFGDLKSDEMELLYSAYGDETGVQ
CALSLQEFVKDAGSYSKKVVDDLLDQITGGDHSRTLFQLKQRRNVPMKPPDEAKVGDTLG
DSSSSVLEFMSMKSYPDVSVDISMLSSLGKVKKELDPDDSHLNLDETTKLLQDLHEAQAE
RGGSRPSSNLSSLSNASERDQHHLGSPSRLSVGEQPDVTHDPYEFLQSPEPAASAKT
Function
Plays a role in chromatin remodeling and regulation of transcription. Acts as a chromatin reader that recognizes and binds acylated histones: binds histones that are acetylated and/or butyrylated. Component of SWI/SNF chromatin remodeling subcomplex GBAF that carries out key enzymatic activities, changing chromatin structure by altering DNA-histone contacts within a nucleosome in an ATP-dependent manner. Orchestrates also the RAD51-RAD54 complex formation and thereby plays a role in homologous recombination (HR).
KEGG Pathway
ATP-dependent chromatin remodeling (hsa03082 )

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
4 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate decreases the expression of Bromodomain-containing protein 9 (BRD9). [1]
Ciclosporin DMAZJFX Approved Ciclosporin increases the expression of Bromodomain-containing protein 9 (BRD9). [2]
Tretinoin DM49DUI Approved Tretinoin decreases the expression of Bromodomain-containing protein 9 (BRD9). [3]
Bisphenol A DM2ZLD7 Investigative Bisphenol A increases the expression of Bromodomain-containing protein 9 (BRD9). [6]
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3 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
TAK-243 DM4GKV2 Phase 1 TAK-243 increases the sumoylation of Bromodomain-containing protein 9 (BRD9). [4]
PMID28870136-Compound-52 DMFDERP Patented PMID28870136-Compound-52 decreases the phosphorylation of Bromodomain-containing protein 9 (BRD9). [5]
Coumarin DM0N8ZM Investigative Coumarin increases the phosphorylation of Bromodomain-containing protein 9 (BRD9). [5]
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References

1 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
2 Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
3 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.
4 Inhibiting ubiquitination causes an accumulation of SUMOylated newly synthesized nuclear proteins at PML bodies. J Biol Chem. 2019 Oct 18;294(42):15218-15234. doi: 10.1074/jbc.RA119.009147. Epub 2019 Jul 8.
5 Quantitative phosphoproteomics reveal cellular responses from caffeine, coumarin and quercetin in treated HepG2 cells. Toxicol Appl Pharmacol. 2022 Aug 15;449:116110. doi: 10.1016/j.taap.2022.116110. Epub 2022 Jun 7.
6 Isobaric tags for relative and absolute quantitation-based proteomics analysis of the effect of ginger oil on bisphenol A-induced breast cancer cell proliferation. Oncol Lett. 2021 Feb;21(2):101. doi: 10.3892/ol.2020.12362. Epub 2020 Dec 8.