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. 2022 Jul 8;12(7):959. doi: 10.3390/biom12070959

Table 2.

Some drugs and inhibitors of ADAMTS (TBD: to be determined).

ADAMTS Endogenous Inhibitor Synthetic Inhibitor Reference
1 Material Category Action type Molecular target Material Category Action type Molecular target [27]
TIMP-2 Tissue inhibitor of metalloproteinase Binding inhibition 3N-terminal globular domain of aggrecan (G1) 1,10-phenanthroline Organic small molecule Binding inhibition Urin recognition site (RX(K/R)R) (33, 34)
TIMP-3 EDTA
BB-94
2 TIMP-3 Tissue inhibitor of metalloproteinase Binding inhibition Sulfated glycosaminoglycans associated with ECM and cell surfaces TBD [216,217,218,219]
Cu2+ Metal ion Bound zinc blinding zone
α−2 macroglobulin Enzyme
Paplin Protein Non-competitive inhibition
3 TIMP-3 Tissue inhibitor of metalloproteinase Binding inhibition Sulfated glycosaminoglycans associated with ECM and cell surfaces TBD [218]
Cu2+ Metal ion Bound zinc blinding zone
4 TIMP-3 Tissue inhibitor of metalloproteinase Binding inhibition Glu1480–Gly1481 bond Cis-1(S)2(R)-amino-2-indanol-based Organic small molecule Selective action Water bridging, ring rigidity, pocket size, and shape [217,220,221]
α−2 macroglobulin Enzyme 691GRGHAR Metformin
PTH1-34 Hormone IGF/IGFBP Losartan Signal conditioning TGF-β1
β-Ecdysone FOXO1/ADAMTS-4/5
4,5-Dicaffeoylquinic Acid NF-κB
Matrix protein CCN1 Protein TGF-β/CCN1
5 Matrix protein CCN1 Protein Binding inhibition TGF-β/CCN1 Cis-1(S)2(R)-amino-2-indanol-based Organic small molecule Selective action Water bridging, ring rigidity, pocket size, and shape [217,220,221,222,223,224,225,226]
TIMP-3 Tissue inhibitor of metalloproteinase Glu1480–Gly1481 bond Metformin
α−2 macroglobulin Enzyme YESDVM690 4,5-Dicaffeoylquinic Acid Organic acid Signal conditioning NF-κB
PTH1-34 Hormone IGF/IGFBP Glycoconjugated arylsulfonamide Binding inhibition Exosite
Losartan Signal conditioning TGF-β1
β-Ecdysone FOXO1/ADAMTS-4/5
5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors Binding inhibition MicroM
7 TIMP-4 Tissue inhibitor of metalloproteinase Binding inhibition Active site zinc Granulin-epithelin precursor Protein Binding inhibition
Binding inhibition
Carboxy-terminal TSR motifs of ADAMTS7 and 12 [76,217,227,228]
GEP Protein C-terminal thrombospondin motifs JG23 Organic acid IC, cut
EDV33 Combined with zinc ion
8 TBD LIPUS Pulse Electrotherapy ZNT-9 [229,230,231]
12 TIMP-4 Tissue inhibitor of metalloproteinase Binding inhibition Active site zinc Granulin-epithelin precursor Protein Binding inhibition Carboxy-terminal TSR motifs of ADAMTS7 and 12 [76,217,227,228]
α2-M Enzyme
GEP Protein C-terminal thrombospondin motifs
14 TIMP-3 Tissue inhibitor of metalloproteinase Binding inhibition Sulfated glycosaminoglycans associated with ECM and cell surfaces TBD [218]
Cu2+ Metal ion Bound zinc blinding zone