Details of Drug Off-Target (DOT)

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

DOT Name Prostate-specific antigen (KLK3)
Synonyms PSA; EC 3.4.21.77; Gamma-seminoprotein; Seminin; Kallikrein-3; P-30 antigen; Semenogelase
Gene Name KLK3
UniProt ID
KLK3_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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PDB ID
2ZCH; 2ZCK; 2ZCL; 3QUM
EC Number
3.4.21.77
Pfam ID
PF00089
Sequence
MWVPVVFLTLSVTWIGAAPLILSRIVGGWECEKHSQPWQVLVASRGRAVCGGVLVHPQWV
LTAAHCIRNKSVILLGRHSLFHPEDTGQVFQVSHSFPHPLYDMSLLKNRFLRPGDDSSHD
LMLLRLSEPAELTDAVKVMDLPTQEPALGTTCYASGWGSIEPEEFLTPKKLQCVDLHVIS
NDVCAQVHPQKVTKFMLCAGRWTGGKSTCSGDSGGPLVCNGVLQGITSWGSEPCALPERP
SLYTKVVHYRKWIKDTIVANP
Function Hydrolyzes semenogelin-1 thus leading to the liquefaction of the seminal coagulum.
KEGG Pathway
Pathways in cancer (hsa05200 )
Prostate cancer (hsa05215 )
Reactome Pathway
Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3 (R-HSA-5625886 )
Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs) (R-HSA-381426 )

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Drug Response of 1 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Cisplatin DMRHGI9 Approved Prostate-specific antigen (KLK3) affects the response to substance of Cisplatin. [61]
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1 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate increases the methylation of Prostate-specific antigen (KLK3). [1]
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64 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Estradiol DMUNTE3 Approved Estradiol increases the expression of Prostate-specific antigen (KLK3). [2]
Quercetin DM3NC4M Approved Quercetin decreases the expression of Prostate-specific antigen (KLK3). [3]
Calcitriol DM8ZVJ7 Approved Calcitriol increases the expression of Prostate-specific antigen (KLK3). [4]
Vorinostat DMWMPD4 Approved Vorinostat decreases the expression of Prostate-specific antigen (KLK3). [5]
Testosterone DM7HUNW Approved Testosterone increases the expression of Prostate-specific antigen (KLK3). [6]
Decitabine DMQL8XJ Approved Decitabine increases the expression of Prostate-specific antigen (KLK3). [7]
Selenium DM25CGV Approved Selenium decreases the expression of Prostate-specific antigen (KLK3). [8]
Fulvestrant DM0YZC6 Approved Fulvestrant decreases the expression of Prostate-specific antigen (KLK3). [9]
Folic acid DMEMBJC Approved Folic acid decreases the expression of Prostate-specific antigen (KLK3). [10]
Niclosamide DMJAGXQ Approved Niclosamide decreases the expression of Prostate-specific antigen (KLK3). [11]
Troglitazone DM3VFPD Approved Troglitazone decreases the expression of Prostate-specific antigen (KLK3). [12]
Diethylstilbestrol DMN3UXQ Approved Diethylstilbestrol decreases the expression of Prostate-specific antigen (KLK3). [13]
Azacitidine DMTA5OE Approved Azacitidine increases the expression of Prostate-specific antigen (KLK3). [14]
Clorgyline DMCEUJD Approved Clorgyline increases the expression of Prostate-specific antigen (KLK3). [15]
Thalidomide DM70BU5 Approved Thalidomide decreases the expression of Prostate-specific antigen (KLK3). [16]
Lindane DMB8CNL Approved Lindane increases the expression of Prostate-specific antigen (KLK3). [17]
Bicalutamide DMZMSPF Approved Bicalutamide decreases the expression of Prostate-specific antigen (KLK3). [18]
Enzalutamide DMGL19D Approved Enzalutamide decreases the expression of Prostate-specific antigen (KLK3). [19]
Hydrocortisone DMGEMB7 Approved Hydrocortisone increases the expression of Prostate-specific antigen (KLK3). [20]
Docetaxel DMDI269 Approved Docetaxel decreases the expression of Prostate-specific antigen (KLK3). [21]
Nevirapine DM6HX9B Approved Nevirapine increases the expression of Prostate-specific antigen (KLK3). [22]
Prasterone DM67VKL Approved Prasterone increases the expression of Prostate-specific antigen (KLK3). [23]
Flutamide DMK0O7U Approved Flutamide decreases the expression of Prostate-specific antigen (KLK3). [24]
Dutasteride DMQ4TJK Approved Dutasteride decreases the expression of Prostate-specific antigen (KLK3). [25]
Fludrocortisone DMUDIR8 Approved Fludrocortisone increases the expression of Prostate-specific antigen (KLK3). [20]
Riluzole DMECBWN Approved Riluzole decreases the expression of Prostate-specific antigen (KLK3). [26]
Hydroxyflutamide DMGIZF5 Approved Hydroxyflutamide decreases the expression of Prostate-specific antigen (KLK3). [27]
Levonorgestrel DM1DP7T Approved Levonorgestrel increases the expression of Prostate-specific antigen (KLK3). [28]
Finasteride DMWV3TZ Approved Finasteride decreases the expression of Prostate-specific antigen (KLK3). [31]
Dihydrotestosterone DM3S8XC Phase 4 Dihydrotestosterone decreases the expression of Prostate-specific antigen (KLK3). [32]
Isoflavone DM7U58J Phase 4 Isoflavone decreases the expression of Prostate-specific antigen (KLK3). [33]
Beclomethasone dipropionate DM5NW1E Phase 4 Beclomethasone dipropionate increases the expression of Prostate-specific antigen (KLK3). [34]
Cyproterone acetate DMLMOIJ Phase 4 Cyproterone acetate decreases the expression of Prostate-specific antigen (KLK3). [35]
Resveratrol DM3RWXL Phase 3 Resveratrol decreases the expression of Prostate-specific antigen (KLK3). [36]
Curcumin DMQPH29 Phase 3 Curcumin decreases the expression of Prostate-specific antigen (KLK3). [37]
EXISULIND DMBY56U Phase 3 EXISULIND decreases the expression of Prostate-specific antigen (KLK3). [38]
Genistein DM0JETC Phase 2/3 Genistein decreases the expression of Prostate-specific antigen (KLK3). [39]
ACYLINE DM9GRTK Phase 2 ACYLINE decreases the expression of Prostate-specific antigen (KLK3). [40]
Netoglitazone DM8H7OA Phase 2 Netoglitazone decreases the expression of Prostate-specific antigen (KLK3). [41]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene increases the expression of Prostate-specific antigen (KLK3). [42]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the expression of Prostate-specific antigen (KLK3). [43]
GSK2816126 DMJDVW4 Phase 1 GSK2816126 decreases the expression of Prostate-specific antigen (KLK3). [44]
KENPAULLONE DMAGVXW Patented KENPAULLONE increases the expression of Prostate-specific antigen (KLK3). [45]
PMID27841045-Compound-129 DME2IHD Patented PMID27841045-Compound-129 decreases the expression of Prostate-specific antigen (KLK3). [46]
THAPSIGARGIN DMDMQIE Preclinical THAPSIGARGIN decreases the expression of Prostate-specific antigen (KLK3). [26]
Bisphenol A DM2ZLD7 Investigative Bisphenol A increases the expression of Prostate-specific antigen (KLK3). [47]
Trichostatin A DM9C8NX Investigative Trichostatin A decreases the expression of Prostate-specific antigen (KLK3). [48]
Sulforaphane DMQY3L0 Investigative Sulforaphane decreases the expression of Prostate-specific antigen (KLK3). [48]
[3H]methyltrienolone DMTSGOW Investigative [3H]methyltrienolone decreases the expression of Prostate-specific antigen (KLK3). [32]
Butanoic acid DMTAJP7 Investigative Butanoic acid decreases the expression of Prostate-specific antigen (KLK3). [49]
Forskolin DM6ITNG Investigative Forskolin increases the expression of Prostate-specific antigen (KLK3). [50]
Rapamycin Immunosuppressant Drug DM678IB Investigative Rapamycin Immunosuppressant Drug increases the expression of Prostate-specific antigen (KLK3). [51]
ELLAGIC ACID DMX8BS5 Investigative ELLAGIC ACID decreases the expression of Prostate-specific antigen (KLK3). [52]
Daidzein DMRFTJX Investigative Daidzein decreases the expression of Prostate-specific antigen (KLK3). [53]
3,7,3',4'-TETRAHYDROXYFLAVONE DMES906 Investigative 3,7,3',4'-TETRAHYDROXYFLAVONE decreases the expression of Prostate-specific antigen (KLK3). [54]
EPZ-004777 DMLN4V5 Investigative EPZ-004777 decreases the expression of Prostate-specific antigen (KLK3). [55]
CYCLOPAMINE DMEM2SW Investigative CYCLOPAMINE decreases the expression of Prostate-specific antigen (KLK3). [56]
Aniline DMLCAR9 Investigative Aniline decreases the expression of Prostate-specific antigen (KLK3). [57]
Indirubin-3'-monoxime DMLRQH0 Investigative Indirubin-3'-monoxime increases the expression of Prostate-specific antigen (KLK3). [45]
1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane DMDJYHK Investigative 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane increases the expression of Prostate-specific antigen (KLK3). [58]
EPI-001 DMYWV81 Investigative EPI-001 decreases the expression of Prostate-specific antigen (KLK3). [12]
[3H]mibolerone DM6HDKQ Investigative [3H]mibolerone increases the expression of Prostate-specific antigen (KLK3). [59]
9-Nitropaullone DM8LUYM Investigative 9-Nitropaullone increases the expression of Prostate-specific antigen (KLK3). [45]
CH-4933468 DM1ZF3Y Investigative CH-4933468 increases the expression of Prostate-specific antigen (KLK3). [60]
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⏷ Show the Full List of 64 Drug(s)
3 Drug(s) Affected the Protein Interaction/Cellular Processes of This DOT
Drug Name Drug ID Highest Status Interaction REF
Goserelin DMAT8CG Approved Goserelin decreases the secretion of Prostate-specific antigen (KLK3). [29]
Methyltestosterone DMWLFGO Approved Methyltestosterone increases the secretion of Prostate-specific antigen (KLK3). [30]
Dibutyl phthalate DMEDGKO Investigative Dibutyl phthalate increases the secretion of Prostate-specific antigen (KLK3). [30]
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References

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2 The mutant androgen receptor T877A mediates the proliferative but not the cytotoxic dose-dependent effects of genistein and quercetin on human LNCaP prostate cancer cells. Mol Pharmacol. 2002 Nov;62(5):1027-35. doi: 10.1124/mol.62.5.1027.
3 Quercetin inhibits the expression and function of the androgen receptor in LNCaP prostate cancer cells. Carcinogenesis. 2001 Mar;22(3):409-14. doi: 10.1093/carcin/22.3.409.
4 Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
5 Suberoylanilide hydroxamic acid (vorinostat) represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer cell proliferation. Mol Cancer Ther. 2007 Jan;6(1):51-60. doi: 10.1158/1535-7163.MCT-06-0144. Epub 2007 Jan 11.
6 Inhibition of 5alpha-reductase enhances testosterone-induced expression of U19/Eaf2 tumor suppressor during the regrowth of LNCaP xenograft tumor in nude mice. Prostate. 2010 Oct 1;70(14):1575-85. doi: 10.1002/pros.21193.
7 A role for DNA methylation in regulating the growth suppressor PMEPA1 gene in prostate cancer. Epigenetics. 2007 Apr-Jun;2(2):100-9.
8 Prostate specific antigen expression is down-regulated by selenium through disruption of androgen receptor signaling. Cancer Res. 2004 Jan 1;64(1):19-22. doi: 10.1158/0008-5472.can-03-2789.
9 Arsenite and cadmium promote the development of mammary tumors. Carcinogenesis. 2020 Jul 14;41(7):1005-1014. doi: 10.1093/carcin/bgz176.
10 Folic acid supplementation dysregulates gene expression in lymphoblastoid cells--implications in nutrition. Biochem Biophys Res Commun. 2011 Sep 9;412(4):688-92. doi: 10.1016/j.bbrc.2011.08.027. Epub 2011 Aug 16.
11 Niclosamide and Bicalutamide Combination Treatment Overcomes Enzalutamide- and Bicalutamide-Resistant Prostate Cancer. Mol Cancer Ther. 2017 Aug;16(8):1521-1530. doi: 10.1158/1535-7163.MCT-16-0912. Epub 2017 May 12.
12 EPI-001 is a selective peroxisome proliferator-activated receptor-gamma modulator with inhibitory effects on androgen receptor expression and activity in prostate cancer. Oncotarget. 2015 Feb 28;6(6):3811-24.
13 Insulin-like growth factor binding protein-6 inhibits prostate cancer cell proliferation: implication for anticancer effect of diethylstilbestrol in hormone refractory prostate cancer. Br J Cancer. 2005 Apr 25;92(8):1538-44. doi: 10.1038/sj.bjc.6602520.
14 Chronic azacitidine treatment results in differentiating effects, sensitizes against bicalutamide in androgen-independent prostate cancer cells. Prostate. 2008 May 15;68(7):793-801. doi: 10.1002/pros.20748.
15 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.
16 An open-label phase II study of low-dose thalidomide in androgen-independent prostate cancer. Br J Cancer. 2003 Mar 24;88(6):822-7. doi: 10.1038/sj.bjc.6600817.
17 -Hexachlorocyclohexane: A Small Molecule with a Big Impact on Human Cellular Biochemistry. Biomedicines. 2020 Nov 16;8(11):505. doi: 10.3390/biomedicines8110505.
18 Microarray analysis of bicalutamide action on telomerase activity, p53 pathway and viability of prostate carcinoma cell lines. J Pharm Pharmacol. 2005 Jan;57(1):83-92.
19 Inhibition of the erythropoietin-producing receptor EPHB4 antagonizes androgen receptor overexpression and reduces enzalutamide resistance. J Biol Chem. 2020 Apr 17;295(16):5470-5483. doi: 10.1074/jbc.RA119.011385. Epub 2020 Mar 17.
20 A glucocorticoid-responsive mutant androgen receptor exhibits unique ligand specificity: therapeutic implications for androgen-independent prostate cancer. Endocrinology. 2002 May;143(5):1889-900. doi: 10.1210/endo.143.5.8778.
21 Tubulin-targeting chemotherapy impairs androgen receptor activity in prostate cancer. Cancer Res. 2010 Oct 15;70(20):7992-8002. doi: 10.1158/0008-5472.CAN-10-0585. Epub 2010 Aug 31.
22 Nevirapine restores androgen signaling in hormone-refractory human prostate carcinoma cells both in vitro and in vivo. Prostate. 2009 May 15;69(7):744-54. doi: 10.1002/pros.20923.
23 Androgen receptor or estrogen receptor-beta blockade alters DHEA-, DHT-, and E(2)-induced proliferation and PSA production in human prostate cancer cells. Prostate. 2007 Aug 1;67(11):1152-62. doi: 10.1002/pros.20585.
24 Identification of a group of brominated flame retardants as novel androgen receptor antagonists and potential neuronal and endocrine disrupters. Environ Int. 2015 Jan;74:60-70.
25 Effects of dutasteride on the expression of genes related to androgen metabolism and related pathway in human prostate cancer cell lines. Invest New Drugs. 2007 Oct;25(5):491-7.
26 Riluzole induces AR degradation via endoplasmic reticulum stress pathway in androgen-dependent and castration-resistant prostate cancer cells. Prostate. 2019 Feb;79(2):140-150. doi: 10.1002/pros.23719. Epub 2018 Oct 2.
27 Androgen receptor modulation following combination exposure to brominated flame-retardants. Sci Rep. 2018 Mar 19;8(1):4843. doi: 10.1038/s41598-018-23181-0.
28 Effects of natural products and nutraceuticals on steroid hormone-regulated gene expression. Clin Chim Acta. 2001 Oct;312(1-2):213-9. doi: 10.1016/s0009-8981(01)00626-x.
29 Prostate specific antigen expression does not necessarily correlate with prostate cancer cell growth. J Urol. 2006 Jul;176(1):354-60. doi: 10.1016/S0022-5347(06)00516-7.
30 Cell viability and PSA secretion assays in LNCaP cells: a tiered in vitro approach to screen chemicals with a prostate-mediated effect on male reproduction within the ReProTect project. Reprod Toxicol. 2010 Aug;30(1):25-35. doi: 10.1016/j.reprotox.2010.03.008. Epub 2010 Apr 2.
31 Antiandrogenic effects of novel androgen synthesis inhibitors on hormone-dependent prostate cancer. Cancer Res. 2000 Dec 1;60(23):6630-40.
32 Characterisation of gene expression patterns in 22RV1 cells for determination of environmental androgenic/antiandrogenic compounds. J Steroid Biochem Mol Biol. 2003 Feb;84(2-3):231-8. doi: 10.1016/s0960-0760(03)00033-5.
33 Soy isoflavones exert differential effects on androgen responsive genes in LNCaP human prostate cancer cells. J Nutr. 2007 Apr;137(4):964-72.
34 Expression of the prostate specific antigen gene by lung tissue. Clin Cancer Res. 1997 Jul;3(7):1201-6.
35 Dramatic suppression of plasma and urinary prostate specific antigen and human glandular kallikrein by antiandrogens in male-to-female transsexuals. J Urol. 2000 Mar;163(3):802-5.
36 Differential expression of genes induced by resveratrol in LNCaP cells: P53-mediated molecular targets. Int J Cancer. 2003 Mar 20;104(2):204-12.
37 Curcumin blocks the activation of androgen and interlukin-6 on prostate-specific antigen expression in human prostatic carcinoma cells. J Androl. 2008 Nov-Dec;29(6):661-8. doi: 10.2164/jandrol.108.004911. Epub 2008 Jul 31.
38 Safety and efficacy of exisulind for treatment of recurrent prostate cancer after radical prostatectomy. J Urol. 2001 Sep;166(3):882-6.
39 Using DNA microarray analyses to elucidate the effects of genistein in androgen-responsive prostate cancer cells: identification of novel targets. Mol Carcinog. 2004 Oct;41(2):108-119.
40 Intraprostatic androgens and androgen-regulated gene expression persist after testosterone suppression: therapeutic implications for castration-resistant prostate cancer. Cancer Res. 2007 May 15;67(10):5033-41.
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42 Benzo[a]pyrene-induced changes in microRNA-mRNA networks. Chem Res Toxicol. 2012 Apr 16;25(4):838-49.
43 Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer. Nature. 2014 Jun 12;510(7504):278-82. doi: 10.1038/nature13229. Epub 2014 Apr 23.
44 Dual targeting of EZH2 and androgen receptor as a novel therapy for castration-resistant prostate cancer. Toxicol Appl Pharmacol. 2020 Oct 1;404:115200. doi: 10.1016/j.taap.2020.115200. Epub 2020 Aug 14.
45 Proliferative and androgenic effects of indirubin derivatives in LNCaP human prostate cancer cells at sub-apoptotic concentrations. Chem Biol Interact. 2011 Feb 1;189(3):177-85. doi: 10.1016/j.cbi.2010.11.008. Epub 2010 Nov 25.
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47 Unique bisphenol A transcriptome in prostate cancer: novel effects on ERbeta expression that correspond to androgen receptor mutation status. Environ Health Perspect. 2007 Nov;115(11):1646-53. doi: 10.1289/ehp.10283.
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54 A novel dietary flavonoid fisetin inhibits androgen receptor signaling and tumor growth in athymic nude mice. Cancer Res. 2008 Oct 15;68(20):8555-63. doi: 10.1158/0008-5472.CAN-08-0240.
55 Histone methyltransferase DOT1L coordinates AR and MYC stability in prostate cancer. Nat Commun. 2020 Aug 19;11(1):4153. doi: 10.1038/s41467-020-18013-7.
56 Mono-2-ethyhexyl phthalate advancing the progression of prostate cancer through activating the hedgehog pathway in LNCaP cells. Toxicol In Vitro. 2016 Apr;32:86-91. doi: 10.1016/j.tiv.2015.12.012. Epub 2015 Dec 19.
57 Designed modulation of sex steroid signaling inhibits telomerase activity and proliferation of human prostate cancer cells. Toxicol Appl Pharmacol. 2014 Oct 15;280(2):323-34. doi: 10.1016/j.taap.2014.08.002. Epub 2014 Aug 11.
58 The Effects of the Organic Flame-Retardant 1,2-Dibromo-4-(1,2-dibromoethyl) Cyclohexane (TBECH) on Androgen Signaling in Human Prostate Cancer Cell Lines. J Biochem Mol Toxicol. 2016 May;30(5):239-42. doi: 10.1002/jbt.21784. Epub 2016 Jan 5.
59 Resveratrol inhibits the expression and function of the androgen receptor in LNCaP prostate cancer cells. Cancer Res. 1999 Dec 1;59(23):5892-5.
60 Biological properties of androgen receptor pure antagonist for treatment of castration-resistant prostate cancer: optimization from lead compound to CH5137291. Prostate. 2011 Sep;71(12):1344-56. doi: 10.1002/pros.21351. Epub 2011 Feb 9.
61 Gene expression profiling of 30 cancer cell lines predicts resistance towards 11 anticancer drugs at clinically achieved concentrations. Int J Cancer. 2006 Apr 1;118(7):1699-712. doi: 10.1002/ijc.21570.