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Pyrimidine dicarboxamides are highly selective MMP-13 inhibitors. In the S1’ pocket of MMP-13 is an S1’ side pocket that is unique to the matrix metalloproteiase. Pyrimidine dicarboxamides bind to this side pocket, which increases the selectivity. The role of MMP-13 is cleaving fibrillar collagen at neutral pH and higher mRNA levels of MMP ...
[5] [6] It is a member of the matrix metalloproteinase (MMP) family. Like most MMPs, it is secreted as an inactive pro-form. [7] MMP-13 has a predicted molecular weight around 54 kDa. [8] It is activated once the pro-domain is cleaved, leaving an active enzyme composed of the catalytic domain and the hemopexin-like domain . Although the actual ...
A matrix metalloproteinase inhibitor (INN stem –mastat [1]) inhibits matrix metalloproteinases.Because they inhibit cell migration, they have antiangiogenic effects. They are endogenous or exogenous.
MMP-11 shows more similarity to the MT-MMPs, is convertase-activatable and is secreted therefore usually associated to convertase-activatable MMPs. Substrates include Col IV, fibronectin, laminin, aggrecan MMP12: Macrophage metalloelastase: HME, ME, MME, MMP-12: secreted: Substrates include elastin, fibronectin, Col IV MMP13: Collagenase 3 ...
ADAMTS13 (a disintegrin and metalloproteinase with a thrombospondin type 1 motif, member 13)—also known as von Willebrand factor-cleaving protease (VWFCP)—is a zinc-containing metalloprotease enzyme that cleaves von Willebrand factor (vWf), a large protein involved in blood clotting.
Cenobamate induces the enzymes CYP3A4 and CYP2B6 and can therefore decrease blood concentrations of drugs that are metabolized by these enzymes (for example midazolam and bupropion, respectively). Conversely, it inhibits the enzyme CYP2C19, potentially increasing concentrations of drugs metabolized by this enzyme (for example omeprazole). [13] [14]
Ubenimex (), also known more commonly as bestatin, is a competitive, reversible protease inhibitor.It is an inhibitor of arginyl aminopeptidase (aminopeptidase B), [3] leukotriene A 4 hydrolase (a zinc metalloprotease that displays both epoxide hydrolase and aminopeptidase activities), [4] alanyl aminopeptidase (aminopeptidase M/N), [5] leucyl/cystinyl aminopeptidase (oxytocinase ...
Dutasteride is sometimes used as a component of hormone therapy for transgender women in combination with an estrogen and/or another antiandrogen such as spironolactone. [7] It may be useful for preventing and treating scalp hair loss and can also be used as a general antiandrogen for in those who have issues tolerating spironolactone, though as a α-reductase inhibitor it has limited effects ...