Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT70YOF2)

• DOT Name: THAP domain-containing protein 2 (THAP2)
• Gene Name: THAP2
• UniProt ID: THAP2_HUMAN
• PDB ID: 2D8R
• Pfam ID: PF05485
• Sequence:
  MPTNCAAAGCATTYNKHINISFHRFPLDPKRRKEWVRLVRRKNFVPGKHTFLCSKHFEAS
  CFDLTGQTRRLKMDAVPTIFDFCTHIKSMKLKSRNLLKKNNSCSPAGPSNLKSNISSQQV
  LLEHSYAFRNPMEAKKRIIKLEKEIASLRRKMKTCLQKERRATRRWIKATCLVKNLEANS
  VLPKGTSEHMLPTALSSLPLEDFKILEQDQQDKTLLSLNLKQTKSTFI

Molecular Interaction Atlas (MIA) of This DOT

1 Drug(s) Affected the Post-Translational Modifications of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate decreases the methylation of THAP domain-containing protein 2 (THAP2).	[1]

12 Drug(s) Affected the Gene/Protein Processing of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate increases the expression of THAP domain-containing protein 2 (THAP2).	[2]
Cisplatin	DMRHGI9	Approved	Cisplatin decreases the expression of THAP domain-containing protein 2 (THAP2).	[3]
Estradiol	DMUNTE3	Approved	Estradiol decreases the expression of THAP domain-containing protein 2 (THAP2).	[4]
Quercetin	DM3NC4M	Approved	Quercetin increases the expression of THAP domain-containing protein 2 (THAP2).	[5]
Clorgyline	DMCEUJD	Approved	Clorgyline increases the expression of THAP domain-containing protein 2 (THAP2).	[6]
Urethane	DM7NSI0	Phase 4	Urethane increases the expression of THAP domain-containing protein 2 (THAP2).	[7]
SNDX-275	DMH7W9X	Phase 3	SNDX-275 decreases the expression of THAP domain-containing protein 2 (THAP2).	[8]
Epigallocatechin gallate	DMCGWBJ	Phase 3	Epigallocatechin gallate increases the expression of THAP domain-containing protein 2 (THAP2).	[9]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the expression of THAP domain-containing protein 2 (THAP2).	[10]
Trichostatin A	DM9C8NX	Investigative	Trichostatin A decreases the expression of THAP domain-containing protein 2 (THAP2).	[11]
Formaldehyde	DM7Q6M0	Investigative	Formaldehyde increases the expression of THAP domain-containing protein 2 (THAP2).	[12]
OXYQUINOLINE	DMZVS9Y	Investigative	OXYQUINOLINE increases the expression of THAP domain-containing protein 2 (THAP2).	[5]

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] Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
• [3] Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
• [4] 17-Estradiol Activates HSF1 via MAPK Signaling in ER-Positive Breast Cancer Cells. Cancers (Basel). 2019 Oct 11;11(10):1533. doi: 10.3390/cancers11101533.
• [5] Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
• [6] Anti-oncogenic and pro-differentiation effects of clorgyline, a monoamine oxidase A inhibitor, on high grade prostate cancer cells. BMC Med Genomics. 2009 Aug 20;2:55. doi: 10.1186/1755-8794-2-55.
• [7] Ethyl carbamate induces cell death through its effects on multiple metabolic pathways. Chem Biol Interact. 2017 Nov 1;277:21-32.
• [8] A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
• [9] Application of the adverse outcome pathway concept for investigating developmental neurotoxicity potential of Chinese herbal medicines by using human neural progenitor cells in vitro. Cell Biol Toxicol. 2023 Feb;39(1):319-343. doi: 10.1007/s10565-022-09730-4. Epub 2022 Jun 15.
• [10] Transcriptional signature of human macrophages exposed to the environmental contaminant benzo(a)pyrene. Toxicol Sci. 2010 Apr;114(2):247-59.
• [11] From transient transcriptome responses to disturbed neurodevelopment: role of histone acetylation and methylation as epigenetic switch between reversible and irreversible drug effects. Arch Toxicol. 2014 Jul;88(7):1451-68.
• [12] Gene expression changes in primary human nasal epithelial cells exposed to formaldehyde in vitro. Toxicol Lett. 2010 Oct 5;198(2):289-95.