Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T66665 Target Info
Target Name Prostaglandin G/H synthase 2 (COX-2)
Synonyms
Prostaglandin-endoperoxide synthase 2; Prostaglandin H2 synthase 2; PHS II; PGHS-2; PGH synthase 2; Cyclooxygenase-2; COX2; COX-2
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Target Type Successful Target
Gene Name PTGS2
Biochemical Class Paired donor oxygen oxidoreductase
UniProt ID
PGH2_HUMAN
Co-Targets of This Target  Top
Co-Target Name Androgen receptor (AR) Successful Target
UniProt ID ANDR_HUMAN
Gene Name AR
Synonyms
Testosterone receptor; Nuclear receptor subfamily 3 group C member 4; NR3C4; Dihydrotestosterone receptor; DHTR
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Representative Drug(s) Indomethacin Drug Info EC50 = 0.14 nM [1]
Co-Target Name Prostaglandin G/H synthase 1 (COX-1) Successful Target
UniProt ID PGH1_HUMAN
Gene Name PTGS1
Synonyms
Prostaglandin-endoperoxide synthase 1; Prostaglandin H2 synthase 1; PHS 1; PGHS-1; PGH synthase 1; Cyclooxygenase-1; COX1; COX-1
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Representative Drug(s) Drug Info IC50 = 2 nM Click to Show More [2]
2 Indomethacin Drug Info IC50 = 2 nM [3]
3 Lumiracoxib Drug Info IC50 = 7 nM [4]
4 Flurbiprofen Drug Info IC50 = 10 nM [5]
5 Celecoxib Drug Info IC50 = 50 nM [11]
6 Ibuprofen Drug Info IC50 = 290 nM [16]
7 Naproxen Drug Info IC50 = 350 nM [18]
8 Darbufelone Drug Info IC50 = 600 nM [20]
Co-Target Name Carbonic anhydrase XII (CA-XII) Successful Target
UniProt ID CAH12_HUMAN
Gene Name CA12
Synonyms
Tumor antigen HOM-RCC-3.1.3; Carbonic anhydrase 12; Carbonate dehydratase XII
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Representative Drug(s) Valdecoxib Drug Info Ki = 13 nM Click to Show More [6]
2 Celecoxib Drug Info Ki = 18 nM [7]
Co-Target Name Carbonic anhydrase II (CA-II) Successful Target
UniProt ID CAH2_HUMAN
Gene Name CA2
Synonyms
Carbonic anhydrase C; Carbonic anhydrase 2; Carbonate dehydratase II; CAC
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Representative Drug(s) Celecoxib Drug Info IC50 = 21 nM Click to Show More [8]
2 Valdecoxib Drug Info IC50 = 43 nM [9]
Co-Target Name Interleukin-8 (IL8) Successful Target
UniProt ID IL8_HUMAN
Gene Name CXCL8
Synonyms
T-cell chemotactic factor; Protein 3-10C; Neutrophil-activating protein 1; NAP-1; Monocyte-derived neutrophil-activating peptide; Monocyte-derived neutrophil chemotactic factor; MONAP; MDNCF; IL8; IL-8; Granulocyte chemotactic protein 1; GCP-1; Emoctakin; Chemokine (C-X-C motif) ligand 8; C-X-C motif chemokine 8
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Representative Drug(s) Indomethacin Drug Info IC50 = 50 nM Click to Show More [10]
2 Tolmetin Drug Info IC50 = 90 nM [10]
Co-Target Name Dihydrodiol dehydrogenase type I (AKR1C3) Successful Target
UniProt ID AK1C3_HUMAN
Gene Name AKR1C3
Synonyms
Trans-1,2-dihydrobenzene-1,2-diol dehydrogenase; Testosterone 17-beta-dehydrogenase 5; Prostaglandin F synthase; PGFS; KIAA0119; Indanol dehydrogenase; HSD17B5; HA1753; Dihydrodiol dehydrogenase 3; DDH1; DD3; DD-3; Chlordecone reductase homolog HAKRb; Aldo-keto reductase family 1 member C3; 3-alpha-hydroxysteroid dehydrogenase type 2; 3-alpha-HSD type II, brain; 3-alpha-HSD type 2; 17-beta-hydroxysteroid dehydrogenase type 5; 17-beta-HSD 5
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Representative Drug(s) Flufenamic Acid Drug Info IC50 = 50 nM Click to Show More [12]
2 Indomethacin Drug Info IC50 = 100 nM [1]
3 Naproxen Drug Info IC50 = 180 nM [14]
4 Mefenamic acid Drug Info Ki = 300 nM [17]
Co-Target Name Carbonic anhydrase VI (CA-VI) Successful Target
UniProt ID CAH6_HUMAN
Gene Name CA6
Synonyms
Secreted carbonic anhydrase; Salivary carbonic anhydrase; Carbonic anhydrase 6; Carbonate dehydratase VI
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Representative Drug(s) Celecoxib Drug Info Ki = 94 nM Click to Show More [13]
2 Valdecoxib Drug Info Ki = 572 nM [19]
Co-Target Name Carbonic anhydrase XIV (CA-XIV) Successful Target
UniProt ID CAH14_HUMAN
Gene Name CA14
Synonyms
UNQ690/PRO1335; Carbonic anhydrase 14; Carbonate dehydratase XIV
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Representative Drug(s) Valdecoxib Drug Info Ki = 107 nM Click to Show More [6]
2 Celecoxib Drug Info Ki = 689 nM [13]
Co-Target Name Carbonic anhydrase IV (CA-IV) Successful Target
UniProt ID CAH4_HUMAN
Gene Name CA4
Synonyms
Carbonic anhydrase 4; Carbonate dehydratase IV; CAIV
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Representative Drug(s) Celecoxib Drug Info Ki = 290 nM [15]
Co-Target Name Amyloid beta A4 protein (APP) Successful Target
UniProt ID A4_HUMAN
Gene Name APP
Synonyms
Protease nexin-II; PreA4; PN-II; Cerebral vascular amyloid peptide; CVAP; Amyloid-beta precursor protein; Amyloid-beta A4 protein; Alzheimer disease amyloid protein; APPI; APP; AD1; ABPP; A4
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Representative Drug(s) Curcumin Drug Info IC50 = 630 nM [21]
Co-Target Name Monoamine oxidase type A (MAO-A) Successful Target
UniProt ID AOFA_HUMAN
Gene Name MAOA
Synonyms
Monoamine oxidase A; Amine oxidase [flavin-containing] A
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Representative Drug(s) Curcumin Drug Info Ki = 710 nM [22]
Co-Target Name Lactoylglutathione lyase (GLO1) Clinical trial Target
UniProt ID LGUL_HUMAN
Gene Name GLO1
Synonyms
S-D-lactoylglutathione methylglyoxal lyase; Methylglyoxalase; Ketone-aldehyde mutase; Glyoxalase I; GlxI; Glx I; GLO1; Aldoketomutase
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Representative Drug(s) Curcumin Drug Info Ki = 5 nM [23]
Co-Target Name Tissue factor (F3) Successful Target
UniProt ID TF_HUMAN
Gene Name F3
Synonyms
Thromboplastin; TF; F3; Coagulation factor III; CD142 antigen
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Representative Drug(s) Curcumin Drug Info IC50 = 13.16 nM [24]
Co-Target Name Carbonic anhydrase IX (CA-IX) Clinical trial Target
UniProt ID CAH9_HUMAN
Gene Name CA9
Synonyms
Renal cell carcinoma-associated antigen G250; RCC-associated antigen G250; PMW1; P54/58N; Membrane antigen MN; MN; G250 antigen (MN/CA IX/G250); G250; Carbonic anhydrase 9; Carbonate dehydratase IX; CAIX
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Representative Drug(s) Celecoxib Drug Info IC50 = 16 nM Click to Show More [8]
2 Valdecoxib Drug Info IC50 = 27 nM [8]
Co-Target Name Prostaglandin D2 receptor 2 (PTGDR2) Clinical trial Target
UniProt ID PD2R2_HUMAN
Gene Name PTGDR2
Synonyms
PTGDR2; Chemoattractant receptor-homologous molecule expressed on Th2 cells; CD294
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Representative Drug(s) Indomethacin Drug Info Ki = 50 nM [25]
Co-Target Name Thromboxane-A synthase (TBXAS1) Clinical trial Target
UniProt ID THAS_HUMAN
Gene Name TBXAS1
Synonyms
Thromboxane A2 synthase; TXS; TXA synthase; Cytochrome P450 5A1; CYP5A1; CYP5
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Representative Drug(s) Indomethacin Drug Info IC50 = 100 nM [26]
Co-Target Name Prostaglandin E synthase (PTGES) Clinical trial Target
UniProt ID PTGES_HUMAN
Gene Name PTGES
Synonyms
p53-induced gene 12 protein; PIG12; PGES; PGE synthase; P53-induced apoptosis protein 12; Microsomal prostaglandin E synthase 1; Microsomal glutathione S-transferase 1-like 1; MPGES1; MPGES-1; MGST1L1; MGST1-L1
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Representative Drug(s) Curcumin Drug Info IC50 = 200 nM Click to Show More [27]
2 Celecoxib Drug Info IC50 = 425 nM [28]
Co-Target Name Stress-activated protein kinase 2a (p38 alpha) Clinical trial Target
UniProt ID MK14_HUMAN
Gene Name MAPK14
Synonyms
SAPK2A; P38 mitogen activatedprotein kinase; P38 Mitogen-activatedprotein kinase alpha; Mitogen-activated protein kinase p38 alpha; Mitogen-activated protein kinase 14; MXI2; MAX-interacting protein 2; MAPK 14; MAP kinase p38alpha; MAP kinase p38 alpha; MAP kinase MXI2; MAP kinase 14; Cytokine suppressive anti-inflammatory drug-binding protein; Cytokine suppressive anti-inflammatory drug binding protein; CSPB1; CSBP2; CSBP1; CSBP; CSAID-binding protein; CSAID binding protein; CRK1
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Representative Drug(s) Etoricoxib Drug Info IC50 = 530 nM Click to Show More [29]
2 Celecoxib Drug Info IC50 = 810 nM [29]
3 RWJ-67657 Drug Info IC50 = 1000 nM [33]
Co-Target Name Histone deacetylase 6 (HDAC6) Clinical trial Target
UniProt ID HDAC6_HUMAN
Gene Name HDAC6
Synonyms
KIAA0901; JM21; HD6
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Representative Drug(s) Celecoxib Drug Info IC50 = 643 nM [30]
Co-Target Name Myeloperoxidase (MPO) Clinical trial Target
UniProt ID PERM_HUMAN
Gene Name MPO
Synonyms
MPO
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Representative Drug(s) Mefenamic acid Drug Info IC50 = 980 nM [31]
Co-Target Name Soluble epoxide hydrolase (EPHX2) Clinical trial Target
UniProt ID HYES_HUMAN
Gene Name EPHX2
Synonyms
Bifunctional epoxide hydrolase 2
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Representative Drug(s) Celecoxib Drug Info IC50 ~ 1000 nM Click to Show More [32]
2 Rofecoxib Drug Info IC50 ~ 1000 nM [32]
3 Indomethacin Drug Info IC50 ~ 1000 nM [32]
Co-Target Name Cytochrome c oxidase subunit 2 (MT-CO2) Co-Target
UniProt ID COX2_HUMAN
Gene Name MT-CO2
Synonyms
Cytochrome c oxidase polypeptide II
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Representative Drug(s) Rofecoxib Drug Info IC50 = 20 nM Click to Show More [34]
2 Celecoxib Drug Info IC50 = 293 nM [34]
3 Indomethacin Drug Info IC50 = 610 nM [36]
Co-Target Name Carbonic anhydrase VB (CA5B) Co-Target
UniProt ID CAH5B_HUMAN
Gene Name CA5B
Synonyms
Carbonic anhydrase 5B, mitochondrial; Carbonate dehydratase VB; Carbonic anhydrase VB; CA-VB
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Representative Drug(s) Valdecoxib Drug Info Ki = 88 nM Click to Show More [6]
2 Celecoxib Drug Info Ki = 93 nM [6]
Co-Target Name Carbonic anhydrase XIII (CA13) Co-Target
UniProt ID CAH13_HUMAN
Gene Name CA13
Synonyms
Carbonic anhydrase 13; Carbonate dehydratase XIII; CA-XIII
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Representative Drug(s) Celecoxib Drug Info Ki = 98 nM Click to Show More [13]
2 Valdecoxib Drug Info Ki = 425 nM [6]
Co-Target Name CDGSH iron-sulfur domain-containing protein 1 (CISD1_HUMAN) Co-Target
UniProt ID CISD1_HUMAN
Gene Name CISD1
Synonyms
MitoNEET
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Representative Drug(s) Curcumin Drug Info Ki = 101 nM [35]
Co-Target Name Aldo-keto reductase family 1 member C2 (AKR1C2) Co-Target
UniProt ID AK1C2_HUMAN
Gene Name AKR1C2
Synonyms
Dihydrodiol dehydrogenase 2; DD-2; DD2; 3-alpha-HSD3; Chlordecone reductase homolog HAKRD; Dihydrodiol dehydrogenase/bile acid-binding protein; DD/BABP; Type III 3-alpha-hydroxysteroid dehydrogenase
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Representative Drug(s) Mefenamic acid Drug Info Ki = 220 nM Click to Show More [17]
2 Flufenamic Acid Drug Info IC50 = 370 nM [12]
Co-Target Name Aldo-keto reductase family 1 member B10 (AKR1B10) Co-Target
UniProt ID AK1BA_HUMAN
Gene Name AKR1B10
Synonyms
ARL-1; Aldose reductase-like; Aldose reductase-related protein; ARP; hARP; Small intestine reductase; SI reductase
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Representative Drug(s) Flufenamic Acid Drug Info IC50 = 760 nM [37]
Co-Target Name Carbonic anhydrase VA (CA5A) Co-Target
UniProt ID CAH5A_HUMAN
Gene Name CA5A
Synonyms
Carbonic anhydrase 5A, mitochondrial; Carbonate dehydratase VA; CA-VA
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Representative Drug(s) Celecoxib Drug Info Ki = 794 nM Click to Show More [6]
2 Valdecoxib Drug Info Ki = 912 nM [6]
Co-Target Name Aldo-keto reductase family 1 member C1 (AK1C1_HUMAN) Co-Target
UniProt ID AK1C1_HUMAN
Gene Name AKR1C1
Synonyms
20-alpha-hydroxysteroid dehydrogenase; 20-alpha-HSD; Dihydrodiol dehydrogenase 1; DD1; Chlordecone reductase homolog HAKRC; High-affinity hepatic bile acid-binding protein; HBAB
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Representative Drug(s) Mefenamic acid Drug Info Ki = 810 nM [17]
References  Top
REF 1 Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer. J Med Chem. 2013 Mar 28;56(6):2429-46.
REF 2 Structure-based design of cyclooxygenase-2 selectivity into ketoprofen. Bioorg Med Chem Lett. 2002 Feb 25;12(4):533-7.
REF 3 Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles. J Med Chem. 2003 Jul 31;46(16):3463-75.
REF 4 Exploring activity cliffs in medicinal chemistry. J Med Chem. 2012 Apr 12;55(7):2932-42.
REF 5 Structural and functional basis of cyclooxygenase inhibition. J Med Chem. 2007 Apr 5;50(7):1425-41.
REF 6 Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit alpha- and beta-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms. J Med Chem. 2012 Nov 26;55(22):9619-29.
REF 7 Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, VII, IX and XII with benzene sulfonamides incorporating 4,5,6,7-tetrabromophthalimide moiety. Bioorg Med Chem. 2013 Oct 1;21(19):5973-82.
REF 8 Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition. J Med Chem. 2004 Jan 29;47(3):550-7.
REF 9 Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride. Bioorg Med Chem Lett. 2004 Jan 19;14(2):337-41.
REF 10 Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4026-30.
REF 11 3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1195-8.
REF 12 Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships. J Med Chem. 2012 Mar 8;55(5):2311-23.
REF 13 Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a l... Bioorg Med Chem Lett. 2010 Aug 1;20(15):4376-81.
REF 14 Discovery of (R)-2-(6-Methoxynaphthalen-2-yl)butanoic Acid as a Potent and Selective Aldo-keto Reductase 1C3 Inhibitor. J Med Chem. 2016 Aug 25;59(16):7431-44.
REF 15 Synthesis of bulky-tailed sulfonamides incorporating pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-1(5H)-yl) moieties and evaluation of their carbonic anhydrases I, II, IV and IX inhibitory effects. Bioorg Med Chem. 2017 Apr 1;25(7):2210-7.
REF 16 Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors. J Med Chem. 2013 Jun 13;56(11):4277-99.
REF 17 Selective inhibitors of aldo-keto reductases AKR1C1 and AKR1C3 discovered by virtual screening of a fragment library. J Med Chem. 2012 Sep 13;55(17):7417-24.
REF 18 Syntheses and biological evaluation of two new naproxen analogs. Bioorg Med Chem Lett. 1996 Oct 8;6(19):2281-2.
REF 19 Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV. J Med Chem. 2009 Feb 12;52(3):646-54.
REF 20 Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series. J Med Chem. 1999 Apr 8;42(7):1151-60.
REF 21 Neuritogenic activity of bi-functional bis-tryptoline triazole. Bioorg Med Chem. 2017 Feb 1;25(3):1195-1201.
REF 22 Monoamine Oxidase Inhibitory Activity of Novel Pyrazoline Analogues: Curcumin Based Design and Synthesis. ACS Med Chem Lett. 2015 Dec 1;7(1):56-61.
REF 23 Recent advances in the discovery and development of glyoxalase I inhibitors. Bioorg Med Chem. 2020 Feb 15;28(4):115243.
REF 24 Microbial hydroxylation and glycosylation of pentacyclic triterpenes as inhibitors on tissue factor procoagulant activity. Bioorg Med Chem Lett. 2017 Feb 15;27(4):1026-30.
REF 25 Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2. J Med Chem. 2005 Oct 6;48(20):6174-7.
REF 26 3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists. J Med Chem. 1989 Aug;32(8):1842-60.
REF 27 Targeting microsomal prostaglandin E2 synthase-1 (mPGES-1): the development of inhibitors as an alternative to non-steroidal anti-inflammatory drugs (NSAIDs). Medchemcomm. 2015;6:2081-123.
REF 28 Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors. J Med Chem. 2016 Jan 14;59(1):194-205.
REF 29 The molecular basis for coxib inhibition of p38alpha MAP kinase. Bioorg Med Chem Lett. 2005 Aug 1;15(15):3506-9.
REF 30 Design, synthesis and biological evaluation of novel hydroxamic acid based histone deacetylase 6 selective inhibitors bearing phenylpyrazol scaffold as surface recognition motif. Bioorg Med Chem. 2018 May 1;26(8):1418-25.
REF 31 Discovery of Novel Potent Reversible and Irreversible Myeloperoxidase Inhibitors Using Virtual Screening Procedure. J Med Chem. 2017 Aug 10;60(15):6563-6586.
REF 32 Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase. J Med Chem. 2011 Apr 28;54(8):3037-50.
REF 33 Drugs designed to inhibit human p38 mitogen-activated protein kinase activation treat Toxoplasma gondii and Encephalitozoon cuniculi infection. Antimicrob Agents Chemother. 2007 Dec;51(12):4324-8.
REF 34 Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities. Eur J Med Chem. 2019 Nov 15;182:111601.
REF 35 Identification of small molecules that bind to the mitochondrial protein mitoNEET. Bioorg Med Chem Lett. 2016 Nov 1;26(21):5350-5353.
REF 36 Hydroxytriazole derivatives as potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors discovered by bioisosteric scaffold hopping approach. Eur J Med Chem. 2017 Oct 20;139:936-946.
REF 37 Flavones Inhibit the Activity of AKR1B10, a Promising Therapeutic Target for Cancer Treatment. J Nat Prod. 2015 Nov 25;78(11):2666-74.

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