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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 ...
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 ...
The most notorious endogenous metalloproteinases are tissue inhibitors of metalloproteinases, followed by cartilage-derived angiogenesis inhibitors. Exogenous matrix metalloproteinase inhibitors were developed as anticancer drugs. [2] Examples include: Batimastat; Cipemastat; Ilomastat; Marimastat; Prinomastat; Rebimastat; Tanomastat
Class of antihypertensives that bind to and inhibit the angiotensin II receptor type 1 and thereby block the arteriolar contraction and sodium retention effects of renin–angiotensin system. Azilsartan medoxomil
In addition, many drugs are small molecule enzyme inhibitors that target either disease-modifying enzymes in the patient [1]: 5 or enzymes in pathogens which are required for the growth and reproduction of the pathogen. [5] In addition to small molecules, some proteins act as enzyme inhibitors.
Antihypertensive agents comprise multiple classes of compounds that are intended to manage hypertension (high blood pressure). Antihypertensive therapy aims to maintain a blood pressure goal of <140/90 mmHg in all patients, as well as to prevent the progression or recurrence of cardiovascular diseases (CVD) in hypertensive patients with established CVD. [2]
Metalloproteinase inhibitors are found in numerous marine organisms, including fish, cephalopods, mollusks, algae and bacteria. [5] Members of the M50 metallopeptidase family include: mammalian sterol-regulatory element binding protein (SREBP) site 2 protease and Escherichia coli protease EcfE, stage IV sporulation protein FB.