m6A-centered Crosstalk Information

Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT00669
 [1], [2], [3], [4], [5]
m6A modification MIR20A MIR20A METTL3 Methylation : m6A sites Indirect Enhancement RNA modification MMP2 MMP2 DKC1 Methylation : modification sites
m6A Modification:
m6A Regulator Methyltransferase-like 3 (METTL3) WRITER
 Regulator Info 
m6A Target hsa-mir-20a
 Targert Gene 
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type RNA modification (RNAMod)  >> Pseudouridine
Epigenetic Regulator H/ACA ribonucleoprotein complex subunit DKC1 (DKC1) WRITER View Details
Regulated Target 72 kDa type IV collagenase (MMP2) View Details
Crosstalk Relationship m6A  →  Pseudouridine Enhancement
Crosstalk Mechanism m6A modification indirectly impacts RNA modification through downstream signaling pathways
Crosstalk Summary METTL3 interacts with hsa-mir-20a, increasing its m6A level and promoting its physical interaction with 72 kDa type IV collagenase (MMP2), which was regulated by DKC1-mediated Pseudouridine modification.
In-vitro Model
 786-O Renal cell carcinoma Homo sapiens CVCL_1051
ACHN Papillary renal cell carcinoma Homo sapiens CVCL_1067
U-87MG ATCC Glioblastoma Homo sapiens CVCL_0022
U-251MG Astrocytoma Homo sapiens CVCL_0021
MKN45 Gastric adenocarcinoma Homo sapiens CVCL_0434
Eca-109 Esophageal squamous cell carcinoma Homo sapiens CVCL_6898
TE1
 N.A. Mus musculus CVCL_C6K3
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
72 kDa type IV collagenase (MMP2) 56 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Prinomastat Approved [6]
Synonyms
AG-3354; AG-3362; Prinomastat (USAN/INN); (3S)-N-hydroxy-2,2-dimethyl-4-(4-pyridin-4-yloxyphenyl)sulfonylthiomorpholine-3-carboxamide
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.05 nM
External Link
CID: 466151
TTD: D00MDP
DrugBank: DB05100
 Compound Name Marimastat Phase 3 [7]
Synonyms
Marimastat [USAN]; BB 2516; BB-2516; Marimastat (USAN/INN); (2R,3S)-N-[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-N',3-dihydroxy-2-(2-methylpropyl)butanediamide; (2S,3R)-3-(((1S)-2,2-Dimethyl-1-(methylcarbamoxy)propyl)carboyl)-2-hydroxy-5-methylhexanohydroxamic acid; (2S,3R)-3-(((1S)-2,2-Dimethyl-1-(methylcarbamoyl)propyl)carbamoyl)-2-hydroxy-5-methylhexanohydroxamic acid; (2S,3R)-N(4)-[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-N(1),2-dihydroxy-3-(2-methylpropyl)butanediamide
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.43 nM
External Link
CID: 119031
TTD: D05VZE
DrugBank: DB00786
 Compound Name Epigallocatechin gallate Phase 3 [8]
Synonyms
(-)-Epigallocatechin gallate; EGCG; 989-51-5; Epigallocatechin 3-gallate; Epigallocatechin-3-gallate; Tea catechin; (-)-Epigallocatechin-3-o-gallate; Teavigo; Epigallocatechin-3-monogallate; (-)-Epigallocatechol gallate; (2R,3R)-5,7-Dihydroxy-2-(3,4,5-trihydroxyphenyl)chroman-3-yl 3,4,5-trihydroxybenzoate; Catechin deriv; UNII-BQM438CTEL; Green tea extract; CCRIS 3729; (-)-epigallocatechin 3-gallate; C22H18O11; BQM438CTEL; (2R,3R)-5,7-dihydroxy-2-(3,4,5-trihydroxyphenyl)-3,4-dihydro-2H-chromen-3-yl; EGCG analogs; EGCG, Anagen; Epigallocatechin gallate analogs, Anagen; Epigallocatechin gallate, Anagen; GTPs,Anagen; Green tea polyphenols, Anagen; EPIGALOCATECHIN GALLATE
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 9600 nM
External Link
CID: 65064
TTD: D0U2BH
DrugBank: DB12116
 Compound Name Metastat Phase 1 [9]
MOA Inhibitor
External Link
CID: 54678924
TTD: D0IJ7O
DrugBank: DB11647
 Compound Name Neovastat Phase 1 [10]
MOA Inhibitor
External Link
TTD: D0T4BL
 Compound Name PMID29130358-Compound-Figure16(9b) Patented [11]
MOA Inhibitor
Activity IC50 = 510 nM
External Link
TTD: D0A9ZW
 Compound Name PMID29130358-Compound-SB-3CT Patented [11]
MOA Inhibitor
Activity IC50 = 14 nM
External Link
TTD: D0DB0Z
 Compound Name PMID29130358-Compound-Figure16(9a) Patented [11]
MOA Inhibitor
Activity IC50 = 53 nM
External Link
CID: 58107501
TTD: D0LS4Y
 Compound Name PMID29130358-Compound-Figure18(14) Patented [11]
MOA Inhibitor
External Link
TTD: D0O8RQ
 Compound Name PMID29130358-Compound-Figure13(4) Patented [11]
MOA Inhibitor
External Link
TTD: D0Q4QB
 Compound Name PMID29130358-Compound-Figure16(9c) Patented [11]
MOA Inhibitor
Activity IC50 = 140 nM
External Link
TTD: D0S3PN
 Compound Name PMID29130358-Compound-LonimacranthoideVII Patented [11]
MOA Inhibitor
Activity IC50 = 6200 nM
External Link
TTD: D0W7HO
 Compound Name PMID29130358-Compound-Figure11(3) Patented [11]
MOA Inhibitor
External Link
TTD: D0Y1LO
 Compound Name PMID29130358-Compound-Figure10(2a) Patented [11]
MOA Inhibitor
External Link
TTD: D05GAP
 Compound Name PMID29130358-Compound-Figure18(14a) Patented [11]
MOA Inhibitor
Activity IC50 = 2500 nM
External Link
TTD: D0X6GG
 Compound Name Tanomastat Discontinued in Phase 3 [12]
Synonyms
Tanomastat (USAN/INN); (2S)-4-[4-(4-chlorophenyl)phenyl]-4-oxo-2-(phenylsulfanylmethyl)butanoic acid
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 11 nM
External Link
CID: 6918336
TTD: D0Q1CD
DrugBank: DB06276
 Compound Name BMS 275291 Discontinued in Phase 3 [13]
Synonyms
D 2163; N-((2S)-2-Mercapto-1-oxo-4-(3,4,4-trimethyl-2,5-dioxo-1-imidazolidinyl)butyl)-L-leucyl-N,3-dimethyl-L-valinamide; (2S)-N-[(2S)-3,3-dimethyl-2-(methylamino)butanoyl]-4-methyl-2-[[(2S)-2-sulfanyl-4-(3,4,4-trimethyl-2,5-dioxoimidazolidin-1-yl)butanoyl]amino]pentanamide
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 148203
TTD: D01EUF
 Compound Name Galarubicin Discontinued in Phase 2 [14]
Synonyms
DA-125; Metalloprotease inhibitors (cancer), Dong-A
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 114759
TTD: D05WTZ
 Compound Name RS-130830 Discontinued in Phase 2 [15]
Synonyms
CTS-1027; 193022-04-7; UNII-2QD3F58224; CHEMBL440498; 2QD3F58224; 4-[4-(4-CHLORO-PHENOXY)-BENZENESULFONYLMETHYL]-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HYDROXYAMIDE; 4-[[[4-(4-Chlorophenoxy)phenyl]sulfonyl]methyl]tetrahydro-N-hydroxy-2H-pyran-4-carboxamide; 4-(4-(4-Chloro-phenoxy)-benzenesulfonylmethyl)-tetrahydro-pyran-4-carboxylic acid hydroxyamide; Ro-1130830; AC1MOE9A; SCHEMBL2381112; BDBM11863; DTXSID90172907; 830c; CTS 1027; ZINC1488366; BCP13018; 3563AH; alpha-tetrahydropyran beta-sulfone 1B; AKOS030526690
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 0.22 nM
External Link
CID: 3342298
TTD: D03BOZ
DrugBank: DB08490
 Compound Name GM6001 Discontinued in Phase 2 [16]
Synonyms
Ilomastat; Galardin; 142880-36-2; GM 6001; Illomastat; CS 610; GM-6001; UNII-I0403ML141; CHEMBL19611; Ilomastat (GM6001, Galardin); I0403ML141; NCGC00163450-02; 3-(N-HYDROXYCARBOXAMIDO)-2-ISOBUTYLPROPANOYL-TRP-METHYLAMIDE; (R)-N4-Hydroxy-N1-[(S)-2-(1H-indol-3-yl)-1-methylcarbamoyl-ethyl]-2-isobutyl-succinamide; N-[(2R)-2-(Hydroxamidocarbonylmethyl)-4-methylpentanoyl]-L-tryptophan Methylamide; (R)-N(sup 1)-Hydroxy-N-((S)-2-indol-3-yl-1-(methylcarbamoyl)ethyl)-2-isobutylsuccinamide; (S-(R*,S*))-N(sup 4)-Hydroxy-N(sup
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 0.104 nM
External Link
CID: 132519
TTD: D0T9HG
DrugBank: DB02255
 Compound Name RO-26-2853 Preclinical [17]
MOA Inhibitor
External Link
TTD: D0C0ME
 Compound Name CDP-845 Terminated [18]
MOA Modulator
External Link
TTD: D02GYD
 Compound Name L-696418 Terminated [19]
Synonyms
CHEMBL8494; BDBM50057083; (R)-2-[(S)-1-(3-Methyl-1-phenylcarbamoyl-butylcarbamoyl)-3-phenyl-propylamino]-propionic acid; (R)-2-((S)-1-((S)-4-methyl-1-oxo-1-(phenylamino)pentan-2-ylamino)-1-oxo-4-phenylbutan-2-ylamino)propanoic acid; (R)-2-[(S)-1-((S)-3-Methyl-1-phenylcarbamoyl-butylcarbamoyl)-3-phenyl-propylamino]-propionic acid
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 200 nM
External Link
CID: 10478364
TTD: D08CEE
 Compound Name BB-3644 Terminated [20]
Synonyms
SCHEMBL609641
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 9822724
TTD: D08WBF
 Compound Name BB-1101 Terminated [21]
Synonyms
CHEMBL432079; SCHEMBL1844243; BDBM50070453
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1.8 nM
External Link
CID: 9908389
TTD: D05VNG
 Compound Name SC-44463 Terminated [22]
Synonyms
CHEMBL45483; n-[3-(n'-hydroxycarboxamido)-2-(2-methylpropyl)-propanoyl]-o-tyrosine-n-methylamide; 104408-38-0; Ihp-tyr-menh2; HTA; AC1L2U0O; SCHEMBL9284838; sc44463; BDBM50104969; DB07926; N-(2-Isobutyl-3-(N'-hydroxycarbonylamido)propanoyl)-O-methyltyrosinemethylamide; N*4*-Hydroxy-2-isobutyl-N*1*-[2-(4-methoxy-phenyl)-1-methylcarbamoyl-ethyl]-succinamide; (2R)-N-hydroxy-N'-[(1S)-2-(4-methoxyphenyl)-1-(methylcarbamoyl)ethyl]-2-(2-methylpropyl)butanediamide; Butanediamide, N4-hydroxy-N1-(1-((4-methoxyphenyl)meth
    Click to Show/Hide
MOA Inhibitor
Activity Ki < 1 nM
External Link
CID: 128564
TTD: D0Y1XT
DrugBank: DB07926
 Compound Name Lithospermic acid Investigative [23]
Synonyms
28831-65-4; UNII-100IP83JAC; CHEMBL518243; 100IP83JAC; Lithospermic-acid; AC1O5VFB; 4-(3-(1-Carboxy-2-(3,4-dihydroxyphenyl)ethoxy)-3-oxo-1-propenyl)-2-(3,4-dihydroxyphenyl)-2,3-dihydro-7-hydroxy-3-benzofurancarboxylic acid; SCHEMBL13284084; MolPort-020-005-934; ZINC4097774; BDBM50250808; AKOS026674259; 4-{(E)-2-[1-Carboxy-2-(3,4-dihydroxy-phenyl)-ethoxycarbonyl]-vinyl}-2-(3,4-dihydroxy-phenyl)-7-hydroxy-2,3-dihydro-benzofuran-3-carboxylic acid; 3-Benzofurancarboxylic acid, 4-(3-(1-carboxy-2-(3,4-dihydr
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 6441498
TTD: D06ALC
 Compound Name SC-74020 Investigative [24]
Synonyms
CHEMBL1233506; N-{4-[(1-HYDROXYCARBAMOYL-2-METHYL-PROPYL)-(2-MORPHOLIN-4-YL-ETHYL)-SULFAMOYL]-4-PENTYL-BENZAMIDE; I52; SC 74020; AC1NRBR8; BDBM50026872; DB01630; SC74020; N-(4-{[(1R)-1-(hydroxycarbamoyl)-2-methylpropyl](2-morpholin-4-ylethyl)sulfamoyl}phenyl)-4-pentylbenzamide; N-(4-{[(1R)-1-(hydroxycarbamoyl)-2-methylpropyl][2-(morpholin-4-yl)ethyl]sulfamoyl}phenyl)-4-pentylbenzamide
    Click to Show/Hide
MOA Inhibitor
Activity IC50 < 0.1 nM
External Link
CID: 5288596
TTD: D08NSS
DrugBank: DB01630
 Compound Name Clinopodic acid C Investigative [23]
Synonyms
CHEMBL1080779; BDBM50310832; (R)-3-(3,4-Dihydroxyphenyl)-2-[3-[2beta-(3,4-dihydroxyphenyl)-3beta-carboxy-2,3-dihydro-1,4-benzodioxin-6-yl]propenoyloxy]propionic acid
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 44254596
TTD: D0H9BL
 Compound Name Cis-2-aminocyclohexylcarbamoylphosphonic acid Investigative [25]
Synonyms
cis-ACCP; 777075-44-2; CHEMBL270083; SCHEMBL569075; C7H15N2O4P; CTK8E9417; MolPort-039-139-066; BDBM50234465; 1683AH; ZINC29134634
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 4000 nM
External Link
CID: 44457233
TTD: D0T1FR
 Compound Name Methotrexate gamma-L-proline-hydroxamic acid Investigative [26]
Synonyms
CHEMBL388879
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 44428667
TTD: D01HKU
 Compound Name PD-169469 Investigative [27]
Synonyms
CHEMBL42420; SCHEMBL7404078; BDBM12074; alpha-arylsulfonylamino carboxylate 2R; (2R)-2-{[4-(4-bromophenyl)benzene]sulfonamido}-3-methylbutanoic acid
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 5 nM
External Link
CID: 10549609
TTD: D02EFQ
 Compound Name 4-(4-(dec-1-ynyl)phenyl)-4-oxobutanoic acid Investigative [28]
Synonyms
CHEMBL373275; BDBM50180608
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3070 nM
External Link
CID: 44406790
TTD: D05JPV
 Compound Name 5-(4-Phenoxy-phenyl)-pyrimidine-2,4,6-trione Investigative [29]
Synonyms
CHEMBL176517; 219311-20-3; 2,4,6(1H,3H,5H)-Pyrimidinetrione, 5-(4-phenoxyphenyl)-; SCHEMBL6380971; CTK0J6997; DTXSID60470422; NNRYJLARUIVRRO-UHFFFAOYSA-N; 5-(4'-phenoxyphenyl)barbituric acid; 5-(4-phenoxyphenyl)pyrimidine-2,4,6-trione
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 53742316
TTD: D07LTB
 Compound Name Methotrexate gamma-hydroxamic acid Investigative [26]
Synonyms
CHEMBL244883
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 44428664
TTD: D0B0UI
 Compound Name 2-(4'-chloro-biphenyl-4-sulfonyl)-pentanoic acid Investigative [30]
Synonyms
CHEMBL378740; BDBM50185874; 2-(4''-chloro-biphenyl-4-sulfonyl)-pentanoic acid
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 792 nM
External Link
CID: 44411812
TTD: D0E5MB
 Compound Name PNU-107859 Investigative [31]
Synonyms
2-[3-(5-MERCAPTO-[1,3,4]THIADIAZOL-2-YL)-UREIDO]-N-METHYL-3-PHENYL-PROPIONAMIDE; CHEMBL249847; ATT; 3usn; AC1N9ZM9; SCHEMBL6954588; RKWXKADYTDWZIJ-VIFPVBQESA-N; ZINC6379443; BDBM50241372; DB07390; N-methyl-Nalpha-[(5-sulfanyl-1,3,4-thiadiazol-2-yl)carbamoyl]-L-phenylalaninamide; (2S)-N-methyl-3-phenyl-2-{[(5-sulfanyl-1,3,4-thiadiazol-2-yl)carbamoyl]amino}propanamide; (S)-1-(1-(methylamino)-1-oxo-3-phenylpropan-2-yl)-3-(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)urea
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 3000 nM
External Link
CID: 4369084
TTD: D0F7BE
DrugBank: DB07390
 Compound Name 5-Hexyl-5-phenyl-pyrimidine-2,4,6-trione Investigative [29]
Synonyms
5-Hexyl-5-phenylbarbituric acid; BRN 0297956; BARBITURIC ACID, 5-HEXYL-5-PHENYL-; 67051-21-2; CHEMBL173075; AC1L2LKK; 4-24-00-02103 (Beilstein Handbook Reference); CTK8J9653; DTXSID20217355; 5-hexyl-5-phenyl barbituric acid; BDBM50099125; LS-24512
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1300 nM
External Link
CID: 49292
TTD: D0K4TI
 Compound Name 5-Biphenyl-4-yl-5-hexyl-pyrimidine-2,4,6-trione Investigative [29]
Synonyms
CHEMBL175282; BDBM50099116
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 868 nM
External Link
CID: 44385624
TTD: D0Q9LC
 Compound Name Roche 28-2653 Investigative [32]
MOA Inhibitor
External Link
CID: 56603788
TTD: D0U7CD
 Compound Name Folate gamma-L-proline-hydroxamic acid Investigative [26]
Synonyms
CHEMBL388878
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 44428663
TTD: D0ZB6O
 Compound Name N-hydroxy-3-(2-oxo-2H-chromen-3-yl)propanamide Investigative [33]
Synonyms
CHEMBL252674; 2H-1-Benzopyran-3-propanamide, N-hydroxy-2-oxo-; BDBM50224963
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 200 nM
External Link
CID: 44446270
TTD: D00RNA
 Compound Name N-hydroxy-3-(6-methoxy-2-oxo-2H-chromen-3-yl) Investigative [33]
Synonyms
CHEMBL402990
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 590 nM
External Link
CID: 44446277
TTD: D08ICI
 Compound Name 3-(4-Phenylethynylbenzoyl)nonanoic acid Investigative [28]
Synonyms
CHEMBL201298
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1660 nM
External Link
CID: 11581319
TTD: D0A5MV
 Compound Name Folate gamma-hydroxamic acid Investigative [26]
MOA Inhibitor
External Link
CID: 136177317
TTD: D0P8EY
 Compound Name 5-Biphenyl-4-yl-5-ethyl-pyrimidine-2,4,6-trione Investigative [29]
Synonyms
CHEMBL367524; 94209-48-0; 2,4,6(1H,3H,5H)-Pyrimidinetrione, 5-[1,1'-biphenyl]-4-yl-5-ethyl-; ACMC-20lyhc; AC1M3WRE; Oprea1_691960; MLS001000776; NIOSH/CQ0532020; CTK3G9325; DTXSID20367041; MolPort-002-095-507; HMS2827O03; BDBM50099119; ZINC96299878; STK760260; AKOS005616072; MCULE-2406616532; Acido 5-etil 5-(p-difenilil)barbiturici; NCGC00245692-01; 5-(4-Biphenylyl)-5-ethylbarbituric acid; SMR000498104; LS-23825; M.G. 3419; CQ05320200; Barbituric acid, 5-(4-biphenylyl)-5-ethyl-
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 898 nM
External Link
CID: 2220392
TTD: D0Y7NV
 Compound Name (+/-)5-(biphenyl-4-yl)-3-hydroxypentanoic acid Investigative [34]
Synonyms
CHEMBL572982; SCHEMBL5613354; ILGSIIFHQGOKKV-UHFFFAOYSA-N; BDBM50300465; 5-biphenyl-4-yl-3-hydroxy-pentanoic acid; 5-(biphenyl-4-yl)-3-hydroxypentanoic acid
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 4520 nM
External Link
CID: 11391583
TTD: D0G3YZ
 Compound Name 3-(4-(2-phenylethynyl)benzoyl)pentanoic acid Investigative [28]
Synonyms
CHEMBL202875
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 440 nM
External Link
CID: 11609208
TTD: D0L4EO
 Compound Name UK-356618 Investigative [22]
Synonyms
UK 356618; 230961-08-7; CHEMBL117225; UK-356,618; SCHEMBL6437730; GTPL6528; CHEBI:94305; DTXSID50438778; MolPort-023-277-089; ZINC3924338; BDBM50097263; AKOS024458021; FT-0675728; PF 03890101; PF-03890101; UK-356618, &gt; J-014983; BRD-K57011718-001-01-5; (R)-N*1*-[(S)-2,2-Dimethyl-1-((R)-1-phenyl-ethylcarbamoyl)-propyl]-N*4*-hydroxy-2-[3-(2-methyl-biphenyl-4-yl)-propyl]-succinamide
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1790 nM
External Link
CID: 10370504
TTD: D0NP8A
 Compound Name Ro-37-9790 Investigative [35]
Synonyms
CHEMBL306412; BDBM50290086
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 44313734
TTD: D0XL8K
 Compound Name 2-(Biphenyl-4-ylsulfonyl)N-hydroxybenzamide Investigative [36]
Synonyms
CHEMBL574589
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1300 nM
External Link
CID: 44478925
TTD: D05THD
 Compound Name [2-(Biphenyl-4-sulfonyl)phenyl]acetic Acid Investigative [36]
Synonyms
CHEMBL573935
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 510 nM
External Link
CID: 44479701
TTD: D07MJD
 Compound Name N-Hydroxy-2-(4-phenoxy-benzenesulfonyl)benzamide Investigative [36]
Synonyms
CHEMBL575896
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1200 nM
External Link
CID: 10155934
TTD: D0S9OL
 Compound Name SR-973 Investigative [37]
Synonyms
CHEMBL204357; SCHEMBL4486832; ZINC34801833; BDBM50182403; (2S,3R)-N1-hydroxy-3-isobutyl-N4-((S)-2-oxo-1-(3-phenoxybenzyl)azepan-3-yl)-2-propylsuccinamide; (2R,3S)-N'-Hydroxy-N-[1-(3-phenoxybenzyl)-2,3,4,5,6,7-hexahydro-2-oxo-1H-azepine-3beta-yl]-2-isobutyl-3-propylbutanediamide
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 7 nM
External Link
CID: 9849669
TTD: D03AMR
 Compound Name IK-862 Investigative [38]
Synonyms
YDMIPBHQKFOFQW-NSYGIPOTSA-N; (2R)-N-HYDROXY-2-[(3S)-3-METHYL-3-{4-[(2-METHYLQUINOLIN-4-YL)METHOXY]PHENYL}-2-OXOPYRROLIDIN-1-YL]PROPANAMIDE; CHEMBL148169; CHEBI:40083; (2R)-N-hydroxy-2-[(3S)-3-methyl-3-[4-[(2-methylquinolin-4-yl)methoxy]phenyl]-2-oxopyrrolidin-1-yl]propanamide; IK862; 2fv5; AC1OCAC0; BMCL181958 Compound 1; GTPL8680; SCHEMBL5966106; BDBM26526; IK682; DB07145; C468787000; (R)-2-[(3S)-2-Oxo-3alpha-[4-(2-methyl-4-quinolinylmethoxy)phenyl]-3-methylpyrrolizino]propanehydroximic; IK 862; compound 32; IK-682
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 2050 nM
External Link
CID: 6914621
TTD: D0W2UK
DrugBank: DB07145
 Compound Name MMI270 Investigative [39]
Synonyms
CGS-27023A; CGS-27023; UNII-80AXY59IT2; 80AXY59IT2; N-HYDROXY-2(R)-[[(4-METHOXYPHENYL)SULFONYL](3-PICOLYL)AMINO]-3-METHYLBUTANAMIDE HYDROCHLORIDE; CHEMBL514138; (2R)-N-hydroxy-2-[(4-methoxyphenyl)sulfonyl-(pyridin-3-ylmethyl)amino]-3-methylbutanamide; CGS; 1eub; MMI270B free base; hydroxamate analogue 1; 2w0d; 1bm6; MMI-270B free base; AC1L9JQY; 3MP-HAV-MSB; CGS-27023A free base; BMCL16311 Compound 1a; BDBM8465; SCHEMBL3468445; GTPL8846; CHEMBL267178; BSIZUMJRKYHEBR-QGZVFWFLSA-N; CGS 27023; BDBM50066658; DB07556; 161314-70-1
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3 nM
External Link
CID: 446504
TTD: D0A4TC
DrugBank: DB07556
References
Ref 1 DKC1 serves as a potential prognostic biomarker for human clear cell renal cell carcinoma and promotes its proliferation, migration and invasion via the NF?kappaB pathway. Oncol Rep. 2018 Aug;40(2):968-978. doi: 10.3892/or.2018.6484. Epub 2018 Jun 11.
Ref 2 Increased DKC1 expression in glioma and its significance in tumor cell proliferation, migration and invasion. Invest New Drugs. 2019 Dec;37(6):1177-1186. doi: 10.1007/s10637-019-00748-w. Epub 2019 Mar 7.
Ref 3 N(6)-methyladenosine-dependent pri-miR-17-92 maturation suppresses PTEN/TMEM127 and promotes sensitivity to everolimus in gastric cancer. Cell Death Dis. 2020 Oct 9;11(10):836. doi: 10.1038/s41419-020-03049-w.
Ref 4 Mechanism of methyltransferase like 3 in epithelial-mesenchymal transition process, invasion, and metastasis in esophageal cancer. Bioengineered. 2021 Dec;12(2):10023-10036. doi: 10.1080/21655979.2021.1994721.
Ref 5 Post-transcriptional regulation of MMP2 mRNA by its interaction with miR-20a and Nucleolin in breast cancer cell lines. Mol Biol Rep. 2021 Mar;48(3):2315-2324. doi: 10.1007/s11033-021-06261-9. Epub 2021 Mar 31.
Ref 6 AG-3340 (Agouron Pharmaceuticals Inc). IDrugs. 2000 Mar;3(3):336-45.
Ref 7 Metalloelastase (MMP-12) induced inflammatory response in mice airways: effects of dexamethasone, rolipram and marimastat. Eur J Pharmacol. 2007 Mar 15;559(1):75-81. doi: 10.1016/j.ejphar.2006.11.070. Epub 2006 Dec 12.
Ref 8 Regioselective synthesis of methylated epigallocatechin gallate via nitrobenzenesulfonyl (Ns) protecting group. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4171-4. doi: 10.1016/j.bmcl.2009.05.111. Epub 2009 Jun 2.
Ref 9 Strategies for MMP inhibition in cancer: innovations for the post-trial era. Nat Rev Cancer. 2002 Sep;2(9):657-72. doi: 10.1038/nrc884.
Ref 10 Neovastat, a naturally occurring multifunctional antiangiogenic drug, in phase III clinical trials. Semin Oncol. 2001 Dec;28(6):620-5. doi: 10.1016/s0093-7754(01)90035-1.
Ref 11 Gelatinase inhibitors: a patent review (2011-2017). Expert Opin Ther Pat. 2018 Jan;28(1):31-46. doi: 10.1080/13543776.2018.1397132. Epub 2017 Nov 12.
Ref 12 Radiation therapy and biological compounds for consolidation therapy in advanced ovarian cancer. Int J Gynecol Cancer. 2008 Mar-Apr;18 Suppl 1:44-6. doi: 10.1111/j.1525-1438.2007.01105.x.
Ref 13 Phase 1/2 trial of BMS-275291 in patients with human immunodeficiency virus-related Kaposi sarcoma: a multicenter trial of the AIDS Malignancy Consortium. Cancer. 2008 Mar 1;112(5):1083-8. doi: 10.1002/cncr.23108.
Ref 14 Inhibitory effect of DA-125, a new anthracyclin analog antitumor agent, on the invasion of human fibrosarcoma cells by down-regulating the matrix metalloproteinases. Biochem Pharmacol. 2005 Dec 19;71(1-2):21-31. doi: 10.1016/j.bcp.2005.10.007. Epub 2005 Nov 2.
Ref 15 Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13). Bioorg Med Chem Lett. 2005 Feb 15;15(4):1101-6. doi: 10.1016/j.bmcl.2004.12.016.
Ref 16 Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase B (MMP-9) inhibitors with improved selectivity. Bioorg Med Chem. 2008 Sep 15;16(18):8745-59. doi: 10.1016/j.bmc.2008.07.041. Epub 2008 Jul 20.
Ref 17 Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52.
Ref 18 Clinical potential of matrix metalloprotease inhibitors. Drugs R D. 1999 Feb;1(2):117-29. doi: 10.2165/00126839-199901020-00001.
Ref 19 Inhibition of matrix metalloproteinases by N-carboxyalkyl peptides containing extended alkyl residues At P1', Bioorg. Med. Chem. Lett. 5(6):539-542 (1995).
Ref 20 Tumour microenvironment - opinion: validating matrix metalloproteinases as drug targets and anti-targets for cancer therapy. Nat Rev Cancer. 2006 Mar;6(3):227-39. doi: 10.1038/nrc1821.
Ref 21 Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution. Bioorg Med Chem Lett. 1998 Jun 16;8(12):1443-8. doi: 10.1016/s0960-894x(98)00255-8.
Ref 22 A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers. J Med Chem. 2003 Jul 31;46(16):3514-25. doi: 10.1021/jm0308038.
Ref 23 Matrix metalloproteinase-2 inhibitors from Clinopodium chinense var. parviflorum. J Nat Prod. 2009 Aug;72(8):1379-84. doi: 10.1021/np800781t.
Ref 24 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 25 Carbamoylphosphonate matrix metalloproteinase inhibitors 6: cis-2-aminocyclohexylcarbamoylphosphonic acid, a novel orally active antimetastatic matrix metalloproteinase-2 selective inhibitor--synthesis and pharmacodynamic and pharmacokinetic analysis. J Med Chem. 2008 Mar 13;51(5):1406-14. doi: 10.1021/jm701087n. Epub 2008 Feb 8.
Ref 26 Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs. Bioorg Med Chem. 2007 Feb 1;15(3):1266-74. doi: 10.1016/j.bmc.2006.11.017. Epub 2006 Nov 14.
Ref 27 Structural insight into the stereoselective inhibition of MMP-8 by enantiomeric sulfonamide phosphonates. J Med Chem. 2006 Feb 9;49(3):923-31. doi: 10.1021/jm050787+.
Ref 28 Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids. J Med Chem. 2006 Jan 26;49(2):456-8. doi: 10.1021/jm051101g.
Ref 29 Novel 5,5-disubstitutedpyrimidine-2,4,6-triones as selective MMP inhibitors. Bioorg Med Chem Lett. 2001 Apr 23;11(8):969-72. doi: 10.1016/s0960-894x(01)00104-4.
Ref 30 Synthesis and SAR of alpha-sulfonylcarboxylic acids as potent matrix metalloproteinase inhibitors. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3096-100. doi: 10.1016/j.bmcl.2006.03.065. Epub 2006 May 2.
Ref 31 A molecular basis for the selectivity of thiadiazole urea inhibitors with stromelysin-1 and gelatinase-A from generalized born molecular dynamics simulations. J Med Chem. 2004 Jun 3;47(12):3065-74. doi: 10.1021/jm030570k.
Ref 32 The new synthetic matrix metalloproteinase inhibitor (Roche 28-2653) reduces tumor growth and prolongs survival in a prostate cancer standard rat model. Oncogene. 2002 Mar 27;21(13):2089-96. doi: 10.1038/sj.onc.1205267.
Ref 33 Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation. Bioorg Med Chem. 2008 Jan 1;16(1):530-5. doi: 10.1016/j.bmc.2007.09.014. Epub 2007 Sep 14.
Ref 34 The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5760-3. doi: 10.1016/j.bmcl.2009.07.155. Epub 2009 Aug 6.
Ref 35 11,21-Bisphenyl-19-norpregnane derivatives are selective antiglucocorticoids, Bioorg. Med. Chem. Lett. 7(17):2299-2302 (1997).
Ref 36 Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors. J Med Chem. 2009 Oct 22;52(20):6347-61. doi: 10.1021/jm900335a.
Ref 37 Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. doi: 10.1016/j.bmcl.2006.01.055. Epub 2006 Feb 10.
Ref 38 Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships. J Med Chem. 2002 Nov 7;45(23):4954-7. doi: 10.1021/jm0255670.
Ref 39 Picking the S1, S1' and S2' pockets of matrix metalloproteinases. A niche for potent acyclic sulfonamide inhibitors. Bioorg Med Chem Lett. 1999 Jun 21;9(12):1691-6. doi: 10.1016/s0960-894x(99)00259-0.