Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT7ETKPE)

DOT Name Peptidyl-prolyl cis-trans isomerase FKBP3 (FKBP3)
Synonyms PPIase FKBP3; EC 5.2.1.8; 25 kDa FK506-binding protein; 25 kDa FKBP; FKBP-25; FK506-binding protein 3; FKBP-3; Immunophilin FKBP25; Rapamycin-selective 25 kDa immunophilin; Rotamase
Gene Name FKBP3
Related Disease
Abscess ( )
Amyotrophic lateral sclerosis type 1 ( )
Colorectal carcinoma ( )
Gastric disease ( )
Non-small-cell lung cancer ( )
Osteoglophonic dwarfism ( )
Parkinson disease ( )
UniProt ID
FKBP3_HUMAN
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
PDB ID
1PBK; 2KFV; 2MPH; 5D75; 5GPG
EC Number
5.2.1.8
Pfam ID
PF18410 ; PF00254
Sequence
MAAAVPQRAWTVEQLRSEQLPKKDIIKFLQEHGSDSFLAEHKLLGNIKNVAKTANKDHLV
TAYNHLFETKRFKGTESISKVSEQVKNVKLNEDKPKETKSEETLDEGPPKYTKSVLKKGD
KTNFPKKGDVVHCWYTGTLQDGTVFDTNIQTSAKKKKNAKPLSFKVGVGKVIRGWDEALL
TMSKGEKARLEIEPEWAYGKKGQPDAKIPPNAKLTFEVELVDID
Function
FK506- and rapamycin-binding proteins (FKBPs) constitute a family of receptors for the two immunosuppressants which inhibit T-cell proliferation by arresting two distinct cytoplasmic signal transmission pathways. PPIases accelerate the folding of proteins.

Molecular Interaction Atlas (MIA) of This DOT

7 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
Abscess DISAP982 Strong Biomarker [1]
Amyotrophic lateral sclerosis type 1 DIS5A2M0 Strong Biomarker [2]
Colorectal carcinoma DIS5PYL0 Strong Altered Expression [3]
Gastric disease DISNZNTG Strong Biomarker [4]
Non-small-cell lung cancer DIS5Y6R9 Strong Biomarker [5]
Osteoglophonic dwarfism DISVSNPT Strong Biomarker [6]
Parkinson disease DISQVHKL Strong Biomarker [7]
------------------------------------------------------------------------------------
⏷ Show the Full List of 7 Disease(s)
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
3 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 Peptidyl-prolyl cis-trans isomerase FKBP3 (FKBP3). [8]
PMID28870136-Compound-52 DMFDERP Patented PMID28870136-Compound-52 decreases the phosphorylation of Peptidyl-prolyl cis-trans isomerase FKBP3 (FKBP3). [15]
Coumarin DM0N8ZM Investigative Coumarin increases the phosphorylation of Peptidyl-prolyl cis-trans isomerase FKBP3 (FKBP3). [15]
------------------------------------------------------------------------------------
8 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Ciclosporin DMAZJFX Approved Ciclosporin decreases the expression of Peptidyl-prolyl cis-trans isomerase FKBP3 (FKBP3). [9]
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate decreases the expression of Peptidyl-prolyl cis-trans isomerase FKBP3 (FKBP3). [10]
Estradiol DMUNTE3 Approved Estradiol decreases the expression of Peptidyl-prolyl cis-trans isomerase FKBP3 (FKBP3). [11]
Ivermectin DMDBX5F Approved Ivermectin decreases the expression of Peptidyl-prolyl cis-trans isomerase FKBP3 (FKBP3). [12]
Selenium DM25CGV Approved Selenium decreases the expression of Peptidyl-prolyl cis-trans isomerase FKBP3 (FKBP3). [13]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 decreases the expression of Peptidyl-prolyl cis-trans isomerase FKBP3 (FKBP3). [14]
Bisphenol A DM2ZLD7 Investigative Bisphenol A decreases the expression of Peptidyl-prolyl cis-trans isomerase FKBP3 (FKBP3). [16]
Milchsaure DM462BT Investigative Milchsaure decreases the expression of Peptidyl-prolyl cis-trans isomerase FKBP3 (FKBP3). [17]
------------------------------------------------------------------------------------
⏷ Show the Full List of 8 Drug(s)

References

1 Novel Regulation of Alpha-Toxin and the Phenol-Soluble Modulins by Peptidyl-Prolyl cis/trans Isomerase Enzymes in Staphylococcus aureus.Toxins (Basel). 2019 Jun 16;11(6):343. doi: 10.3390/toxins11060343.
2 The role of immunophilins in mutant superoxide dismutase-1linked familial amyotrophic lateral sclerosis.Proc Natl Acad Sci U S A. 1999 Mar 16;96(6):3251-6. doi: 10.1073/pnas.96.6.3251.
3 FKBP3 mediates oxaliplatin resistance in colorectal cancer cells by regulating HDAC2 expression.Oncol Rep. 2019 Oct;42(4):1404-1412. doi: 10.3892/or.2019.7259. Epub 2019 Aug 2.
4 Differential Proteomic Analysis Reveals Protein Networks and Pathways that May Contribute to Helicobacter pylori FKBP-Type PPIase-Associated Gastric Diseases.Proteomics Clin Appl. 2018 May;12(3):e1700127. doi: 10.1002/prca.201700127. Epub 2017 Dec 5.
5 FKBP3 Promotes Proliferation of Non-Small Cell Lung Cancer Cells through Regulating Sp1/HDAC2/p27.Theranostics. 2017 Jul 22;7(12):3078-3089. doi: 10.7150/thno.18067. eCollection 2017.
6 Elucidation of the FKBP25-60S Ribosomal Protein L7a Stress Response Signaling During Ischemic Injury.Cell Physiol Biochem. 2018;47(5):2018-2030. doi: 10.1159/000491470. Epub 2018 Jul 3.
7 The Molecular Basis of the Interaction of CyclophilinA with -Synuclein.Angew Chem Int Ed Engl. 2020 Mar 27;59(14):5643-5646. doi: 10.1002/anie.201914878. Epub 2020 Jan 29.
8 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.
9 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
10 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
11 Genistein and bisphenol A exposure cause estrogen receptor 1 to bind thousands of sites in a cell type-specific manner. Genome Res. 2012 Nov;22(11):2153-62.
12 Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
13 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
14 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.
15 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.
16 Bisphenol A induces DSB-ATM-p53 signaling leading to cell cycle arrest, senescence, autophagy, stress response, and estrogen release in human fetal lung fibroblasts. Arch Toxicol. 2018 Apr;92(4):1453-1469.
17 Transcriptional profiling of lactic acid treated reconstructed human epidermis reveals pathways underlying stinging and itch. Toxicol In Vitro. 2019 Jun;57:164-173.