Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT2P0XNK)

• DOT Name: Integral membrane protein GPR180 (GPR180)
• Synonyms: Intimal thickness-related receptor
• Gene Name: GPR180
• Related Disease:
  leukaemia
  Leukemia
  Osteogenesis imperfecta
  Promyelocytic leukaemia
  Lung adenocarcinoma
  Lung cancer
  Lung carcinoma
• UniProt ID: GP180_HUMAN
• Pfam ID: PF10192
• Sequence:
  MGGLRLLAVALTCCWWPQGSQGKTLRGSFSSTAAQDAQGQRIGHFEFHGDHALLCVRINN
  IAVAVGKEAKLYLFQAQEWLKLQQSSHGYSCSEKLSKAQLTMTMNQTEHNLTVSQIPSPQ
  TWHVFYADKYTCQDDKENSQVEDIPFEMVLLNPDAEGNPFDHFSAGESGLHEFFFLLVLV
  YFVIACIYAQSLWQAIKKGGPMHMILKVLTTALLLQAGSALANYIHFSSYSKDGIGVPFM
  GSLAEFFDIASQIQMLYLLLSLCMGWTIVRMKKSQSRPLQWDSTPASTGIAVFIVMTQSV
  LLLWEQFEDISHHSYHSHHNLAGILLIVLRICLALSLGCGLYQIITVERSTLKREFYITF
  AKGCILWFLCHPVLACISVIFSDYQRDKVITIGVILCQSVSMVILYRLFLSHSLYWEVSS
  LSSVTLPLTISSGHKSRPHF

Molecular Interaction Atlas (MIA) of This DOT

7 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
leukaemia	DISS7D1V	Strong	Biomarker	[1]
Leukemia	DISNAKFL	Strong	Biomarker	[1]
Osteogenesis imperfecta	DIS7XQSD	Strong	Biomarker	[2]
Promyelocytic leukaemia	DISYGG13	moderate	Biomarker	[1]
Lung adenocarcinoma	DISD51WR	Limited	Biomarker	[3]
Lung cancer	DISCM4YA	Limited	Biomarker	[3]
Lung carcinoma	DISTR26C	Limited	Biomarker	[3]

8 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 Integral membrane protein GPR180 (GPR180).	[4]
Doxorubicin	DMVP5YE	Approved	Doxorubicin decreases the expression of Integral membrane protein GPR180 (GPR180).	[5]
Temozolomide	DMKECZD	Approved	Temozolomide decreases the expression of Integral membrane protein GPR180 (GPR180).	[7]
Vorinostat	DMWMPD4	Approved	Vorinostat increases the expression of Integral membrane protein GPR180 (GPR180).	[8]
Demecolcine	DMCZQGK	Approved	Demecolcine decreases the expression of Integral membrane protein GPR180 (GPR180).	[9]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene decreases the expression of Integral membrane protein GPR180 (GPR180).	[10]
PMID28460551-Compound-2	DM4DOUB	Patented	PMID28460551-Compound-2 increases the expression of Integral membrane protein GPR180 (GPR180).	[11]
Formaldehyde	DM7Q6M0	Investigative	Formaldehyde decreases the expression of Integral membrane protein GPR180 (GPR180).	[9]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Arsenic	DMTL2Y1	Approved	Arsenic affects the methylation of Integral membrane protein GPR180 (GPR180).	[6]

References

• [1] ITR?84 modulates cell differentiation in human chronic myelogenous leukemia K562 cells.Oncol Rep. 2018 Jan;39(1):383-391. doi: 10.3892/or.2017.6090. Epub 2017 Nov 9.
• [2] Dual Interlocking Telescopic Rod Provides Effective Tibial Stabilization in Children With Osteogenesis Imperfecta.Clin Orthop Relat Res. 2018 Nov;476(11):2238-2246. doi: 10.1097/CORR.0000000000000429.
• [3] Carboxamide analog ITR-284 evokes apoptosis and inhibits migration ability in human lung adenocarcinoma A549 cells.Oncol Rep. 2017 Mar;37(3):1786-1792. doi: 10.3892/or.2017.5374. Epub 2017 Jan 16.
• [4] Stem cell transcriptome responses and corresponding biomarkers that indicate the transition from adaptive responses to cytotoxicity. Chem Res Toxicol. 2017 Apr 17;30(4):905-922.
• [5] Bringing in vitro analysis closer to in vivo: studying doxorubicin toxicity and associated mechanisms in 3D human microtissues with PBPK-based dose modelling. Toxicol Lett. 2018 Sep 15;294:184-192.
• [6] Prenatal arsenic exposure and the epigenome: identifying sites of 5-methylcytosine alterations that predict functional changes in gene expression in newborn cord blood and subsequent birth outcomes. Toxicol Sci. 2015 Jan;143(1):97-106. doi: 10.1093/toxsci/kfu210. Epub 2014 Oct 10.
• [7] Temozolomide induces activation of Wnt/-catenin signaling in glioma cells via PI3K/Akt pathway: implications in glioma therapy. Cell Biol Toxicol. 2020 Jun;36(3):273-278. doi: 10.1007/s10565-019-09502-7. Epub 2019 Nov 22.
• [8] Definition of transcriptome-based indices for quantitative characterization of chemically disturbed stem cell development: introduction of the STOP-Toxukn and STOP-Toxukk tests. Arch Toxicol. 2017 Feb;91(2):839-864.
• [9] Characterization of formaldehyde's genotoxic mode of action by gene expression analysis in TK6 cells. Arch Toxicol. 2013 Nov;87(11):1999-2012.
• [10] Transcriptional signature of human macrophages exposed to the environmental contaminant benzo(a)pyrene. Toxicol Sci. 2010 Apr;114(2):247-59.
• [11] Cell-based two-dimensional morphological assessment system to predict cancer drug-induced cardiotoxicity using human induced pluripotent stem cell-derived cardiomyocytes. Toxicol Appl Pharmacol. 2019 Nov 15;383:114761. doi: 10.1016/j.taap.2019.114761. Epub 2019 Sep 15.