Details of Drug Off-Target (DOT)

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

DOT Name Regulator of G-protein signaling 16 (RGS16)
Synonyms RGS16; A28-RGS14P; Retinal-specific RGS; RGS-r; hRGS-r; Retinally abundant regulator of G-protein signaling
Gene Name RGS16
UniProt ID
RGS16_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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PDB ID
2BT2; 2IK8
Pfam ID
PF00615
Sequence
MCRTLAAFPTTCLERAKEFKTRLGIFLHKSELGCDTGSTGKFEWGSKHSKENRNFSEDVL
GWRESFDLLLSSKNGVAAFHAFLKTEFSEENLEFWLACEEFKKIRSATKLASRAHQIFEE
FICSEAPKEVNIDHETHELTRMNLQTATATCFDAAQGKTRTLMEKDSYPRFLKSPAYRDL
AAQASAASATLSSCSLDEPSHT
Function
Regulates G protein-coupled receptor signaling cascades. Inhibits signal transduction by increasing the GTPase activity of G protein alpha subunits, thereby driving them into their inactive GDP-bound form. Plays an important role in the phototransduction cascade by regulating the lifetime and effective concentration of activated transducin alpha. May regulate extra and intracellular mitogenic signals.
Tissue Specificity Abundantly expressed in retina with lower levels of expression in most other tissues.
Reactome Pathway
G alpha (i) signalling events (R-HSA-418594 )
G alpha (z) signalling events (R-HSA-418597 )
G alpha (q) signalling events (R-HSA-416476 )

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
32 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate increases the expression of Regulator of G-protein signaling 16 (RGS16). [1]
Ciclosporin DMAZJFX Approved Ciclosporin decreases the expression of Regulator of G-protein signaling 16 (RGS16). [2]
Tretinoin DM49DUI Approved Tretinoin decreases the expression of Regulator of G-protein signaling 16 (RGS16). [3]
Acetaminophen DMUIE76 Approved Acetaminophen increases the expression of Regulator of G-protein signaling 16 (RGS16). [4]
Doxorubicin DMVP5YE Approved Doxorubicin increases the expression of Regulator of G-protein signaling 16 (RGS16). [5]
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate increases the expression of Regulator of G-protein signaling 16 (RGS16). [6]
Cisplatin DMRHGI9 Approved Cisplatin increases the expression of Regulator of G-protein signaling 16 (RGS16). [7]
Estradiol DMUNTE3 Approved Estradiol increases the expression of Regulator of G-protein signaling 16 (RGS16). [8]
Hydrogen peroxide DM1NG5W Approved Hydrogen peroxide affects the expression of Regulator of G-protein signaling 16 (RGS16). [9]
Calcitriol DM8ZVJ7 Approved Calcitriol decreases the expression of Regulator of G-protein signaling 16 (RGS16). [10]
Marinol DM70IK5 Approved Marinol increases the expression of Regulator of G-protein signaling 16 (RGS16). [11]
Phenobarbital DMXZOCG Approved Phenobarbital affects the expression of Regulator of G-protein signaling 16 (RGS16). [12]
Menadione DMSJDTY Approved Menadione affects the expression of Regulator of G-protein signaling 16 (RGS16). [9]
Fluorouracil DMUM7HZ Approved Fluorouracil affects the expression of Regulator of G-protein signaling 16 (RGS16). [13]
Demecolcine DMCZQGK Approved Demecolcine increases the expression of Regulator of G-protein signaling 16 (RGS16). [14]
Mitomycin DMH0ZJE Approved Mitomycin decreases the expression of Regulator of G-protein signaling 16 (RGS16). [15]
Melphalan DMOLNHF Approved Melphalan increases the expression of Regulator of G-protein signaling 16 (RGS16). [16]
Colchicine DM2POTE Approved Colchicine decreases the expression of Regulator of G-protein signaling 16 (RGS16). [15]
Hydroxyurea DMOQVU9 Approved Hydroxyurea increases the expression of Regulator of G-protein signaling 16 (RGS16). [15]
Adenine DMZLHKJ Approved Adenine decreases the expression of Regulator of G-protein signaling 16 (RGS16). [15]
Tamibarotene DM3G74J Phase 3 Tamibarotene decreases the expression of Regulator of G-protein signaling 16 (RGS16). [3]
Curcumin DMQPH29 Phase 3 Curcumin increases the expression of Regulator of G-protein signaling 16 (RGS16). [17]
Genistein DM0JETC Phase 2/3 Genistein decreases the expression of Regulator of G-protein signaling 16 (RGS16). [18]
Afimoxifene DMFORDT Phase 2 Afimoxifene increases the expression of Regulator of G-protein signaling 16 (RGS16). [8]
phorbol 12-myristate 13-acetate DMJWD62 Phase 2 phorbol 12-myristate 13-acetate increases the expression of Regulator of G-protein signaling 16 (RGS16). [19]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene increases the expression of Regulator of G-protein signaling 16 (RGS16). [20]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 increases the expression of Regulator of G-protein signaling 16 (RGS16). [21]
PMID28870136-Compound-48 DMPIM9L Patented PMID28870136-Compound-48 increases the expression of Regulator of G-protein signaling 16 (RGS16). [22]
Bisphenol A DM2ZLD7 Investigative Bisphenol A decreases the expression of Regulator of G-protein signaling 16 (RGS16). [23]
Formaldehyde DM7Q6M0 Investigative Formaldehyde increases the expression of Regulator of G-protein signaling 16 (RGS16). [24]
Acetaldehyde DMJFKG4 Investigative Acetaldehyde increases the expression of Regulator of G-protein signaling 16 (RGS16). [25]
N-(3-METHYLBUT-2-EN-1-YL)-9H-PURIN-6-AMINE DM2D4KY Investigative N-(3-METHYLBUT-2-EN-1-YL)-9H-PURIN-6-AMINE decreases the expression of Regulator of G-protein signaling 16 (RGS16). [26]
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References

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2 Cyclosporine A--induced oxidative stress in human renal mesangial cells: a role for ERK 1/2 MAPK signaling. Toxicol Sci. 2012 Mar;126(1):101-13.
3 Differential modulation of PI3-kinase/Akt pathway during all-trans retinoic acid- and Am80-induced HL-60 cell differentiation revealed by DNA microarray analysis. Biochem Pharmacol. 2004 Dec 1;68(11):2177-86.
4 Gene expression analysis of precision-cut human liver slices indicates stable expression of ADME-Tox related genes. Toxicol Appl Pharmacol. 2011 May 15;253(1):57-69.
5 RNA sequence analysis of inducible pluripotent stem cell-derived cardiomyocytes reveals altered expression of DNA damage and cell cycle genes in response to doxorubicin. Toxicol Appl Pharmacol. 2018 Oct 1;356:44-53.
6 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
7 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
8 Estrogenic GPR30 signalling induces proliferation and migration of breast cancer cells through CTGF. EMBO J. 2009 Mar 4;28(5):523-32.
9 Global gene expression analysis reveals differences in cellular responses to hydroxyl- and superoxide anion radical-induced oxidative stress in caco-2 cells. Toxicol Sci. 2010 Apr;114(2):193-203. doi: 10.1093/toxsci/kfp309. Epub 2009 Dec 31.
10 Identification of vitamin D3 target genes in human breast cancer tissue. J Steroid Biochem Mol Biol. 2016 Nov;164:90-97.
11 Inhibiting Heat Shock Proteins Can Potentiate the Cytotoxic Effect of Cannabidiol in Human Glioma Cells. Anticancer Res. 2015 Nov;35(11):5827-37.
12 Reproducible chemical-induced changes in gene expression profiles in human hepatoma HepaRG cells under various experimental conditions. Toxicol In Vitro. 2009 Apr;23(3):466-75. doi: 10.1016/j.tiv.2008.12.018. Epub 2008 Dec 30.
13 Cell-type-specific responses to chemotherapeutics in breast cancer. Cancer Res. 2004 Jun 15;64(12):4218-26.
14 Characterization of formaldehyde's genotoxic mode of action by gene expression analysis in TK6 cells. Arch Toxicol. 2013 Nov;87(11):1999-2012.
15 Utilization of CDKN1A/p21 gene for class discrimination of DNA damage-induced clastogenicity. Toxicology. 2014 Jan 6;315:8-16. doi: 10.1016/j.tox.2013.10.009. Epub 2013 Nov 6.
16 Bone marrow osteoblast damage by chemotherapeutic agents. PLoS One. 2012;7(2):e30758. doi: 10.1371/journal.pone.0030758. Epub 2012 Feb 17.
17 Gene-expression profiling during curcumin-induced apoptosis reveals downregulation of CXCR4. Exp Hematol. 2007 Jan;35(1):84-95.
18 Regulation of gene expression and inhibition of experimental prostate cancer bone metastasis by dietary genistein. Neoplasia. 2004 Jul-Aug;6(4):354-63. doi: 10.1593/neo.03478.
19 Expression of endogenous retroviruses reflects increased usage of atypical enhancers in T cells. EMBO J. 2019 Jun 17;38(12):e101107. doi: 10.15252/embj.2018101107. Epub 2019 May 8.
20 Identification of a transcriptomic signature of food-relevant genotoxins in human HepaRG hepatocarcinoma cells. Food Chem Toxicol. 2020 Jun;140:111297. doi: 10.1016/j.fct.2020.111297. Epub 2020 Mar 28.
21 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.
22 Global expression profiling of theophylline response genes in macrophages: evidence of airway anti-inflammatory regulation. Respir Res. 2005 Aug 8;6(1):89. doi: 10.1186/1465-9921-6-89.
23 Bisphenol A and bisphenol S induce distinct transcriptional profiles in differentiating human primary preadipocytes. PLoS One. 2016 Sep 29;11(9):e0163318.
24 Identification of gene markers for formaldehyde exposure in humans. Environ Health Perspect. 2007 Oct;115(10):1460-6. doi: 10.1289/ehp.10180.
25 Transcriptome profile analysis of saturated aliphatic aldehydes reveals carbon number-specific molecules involved in pulmonary toxicity. Chem Res Toxicol. 2014 Aug 18;27(8):1362-70.
26 Immediate up-regulation of the calcium-binding protein S100P and its involvement in the cytokinin-induced differentiation of human myeloid leukemia cells. Biochim Biophys Acta. 2005 Sep 10;1745(2):156-65.