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Metallo protease inhibitors

Protease 3D structural models matrix metallo protease-inhibitor complexes... [Pg.612]

Very recently, (3-lactam antibiotics have been shown to offer neuroprotection by increasing glutamate transporters expression via gene activation [15] in addition, the discoveries of new biologically active (3-lactams such as cholesterol acyl transferase inhibitors [16-18], thrombin inhibitors [19], human cytomegalovirus protease inhibitors [20], matrix-metallo protease inhibitors [21], inhibitors of human leukocyte elastase (HLE) [22, 23] and cysteine protease [24, 25], and apoptosis inductors [26, 27] have provided much needed motivation for continuous development of new (3-lactam systems. [Pg.52]

Various solid-phase syntheses have been reported including the phosphinic acid dipeptide analogues 209 which were constructed by coupling the appropriate Wang Resin-bound amino acid to the phosphinate carboxylic acid 210 using Fmoc chemistry. Similar phosphinate carboxylic acid derivatives (211) protected at phosphorus as their 1-adamanyl esters have also been used in solid-phase synthesis directed towards zinc metallo protease inhibitors. ... [Pg.126]

Reported bioanalytical applications that use SS-LLE products include both tlie cartridge (tube) format and the microplate format. Some of these applications include the determination of mexiletine [44], amiodarone [45] and other antiarrhythmic drugs [46], proxyphylline [47], 16(3-hydroxystanozolol [48], dextromethorphan [49], and simvastatin [50] from biological fluids. Microplate applications for SS-LLE include a crude purification of crude combinatorial library samples [51], carboxylic acid-based matrix metallo-protease inhibitors [52], and a p3-adrenergic receptor agonist [53]. [Pg.487]

Combinatorial chemists at Merck described the synthesis of a mechanism-based library (1.25) of matrix metallo-protease inhibitors combining both mix and split and indexed combinatorial techniques [10]. The results found in the study were consistent with the known SAR for this class of inhibitor. [Pg.100]

There are numerous examples of the application of rhodium and ruthenium catalysed hydrogenation of functionalised alkenes to the synthesis of pharmaceuticals. One such example is the hydrogenation of itaconate 3 in the synthesis of MMP-3 (Matrix Metallo Protease) inhibitor 5 (Scheme 14.3). Both rhodium and ruthenium catalysts were screened for the reduction of the free acid and carbojgrlate salts. It was found that rhodium catalysts performed well in the reduction of the free acid conversely the ruthenium catalysts were effective for the reduction of salts. Despite... [Pg.162]

Januario AH, Simone LS, Silvana M, et al. Neo-clerodane diterpenoid, a new metallo-protease snake venom inhibitor from Baccharis trimera (Asteraceae) anti-proteolytic and anti-hemorrhagic properties. Chem Biol Interact 2002 150 243-251. [Pg.64]

Based on their sequence homology, disulfide connectivity, and cysteine location within the sequence and chemistry of the reactive site. Pis can be assigned to distinct families, as classified by Laskowski and Kato. Kunitz-type, Bowman—Birk-type, Potato type I and type II, and squash inhibitors are members of these families shown in Table 3. For inhibitors not falling into these classifications more families have been proposed. Pis can also be classified by their target/mode of action. Plants have been found to express Pis that target serine proteinases, cysteine proteinases, aspartic proteinases, and metallo-proteinases. Serine and cysteine protease inhibitors are the best-studied PIs. ... [Pg.271]

Peterson JT, Li H, Dillon L, Bryant JW. Evolution of metallo-protease and tissue inhibitor expression during heart failure progression in the infarcted heart, Cardiovasc Res 2000 46 307-315. [Pg.369]

Numerous reversible inhibitors have been developed for metallo-proteases and some have therapeutic applications. [Pg.359]

Figure 1.12 The arylsulfonylhydroxamate scaffold (top) served as template structure for compounds active on various members of the matrix metallo-protease family, as well as of phosphodiesterase 4. By variation of the molecular periphery (R-groups, X top), discriminating compounds (bottom left, bottom middle), as well as dual inhibitors (bottom right) were obtained [61, 62]. Figure 1.12 The arylsulfonylhydroxamate scaffold (top) served as template structure for compounds active on various members of the matrix metallo-protease family, as well as of phosphodiesterase 4. By variation of the molecular periphery (R-groups, X top), discriminating compounds (bottom left, bottom middle), as well as dual inhibitors (bottom right) were obtained [61, 62].
ADAM. A Disintesrin And MetalloProteinase family of proteins. Disintegrins, as the name implies, are proteins which interfere with interactions of cells with proteins in the extracellular matrix. An example are the inhibitors of the interaction of blood platelets with fibrinogen. Disintegrins are found in snake venom. Metalloproteinases are a family of proteases which need a bivalent cation for catalysis. MMP s are matrix metallo-proteases. They are associated with the extracellular matrix. [Pg.303]

Classical TSA inhibitors of cysteine and serine proteases differ from the metallo- and aspartic protease inhibitors in that they mimic the tet-... [Pg.652]

Fig. 2. Silicon diol proteases inhibitors, 1 (angiotensin-converting enzyme (metallo) inhibitor) and 2 (HIV protease (aspartyl) inhibitor). Fig. 2. Silicon diol proteases inhibitors, 1 (angiotensin-converting enzyme (metallo) inhibitor) and 2 (HIV protease (aspartyl) inhibitor).
The most conserved segment of the L chain of CNTs is a central region that contains a His-Glu-Xaa-Xaa-His zinc-binding motif characteristic of zinc-endopeptidases, thus suggesting that TeTx and the BoNTs may inhibit neuroexocytosis through a zinc-endopeptidase activity. This hypothesis was confirmed with two experimental approaches in Aply-sia neurons. First, the lack of toxicity of the apo-TeTx L chain demonstrated the essential role of the metal atom in toxin activity (Schiavo et ai, 1992 a, b). Second, phosphoramidon, a very specific inhibitor of zinc-endopeptidases, was shown to inhibit TeTx-induced blockade of ACh release (Schiavo ef ai, 1992 b). These results were the first clear evidence that the L chain of TeTx was acting via a metallo-protease activity. [Pg.176]

Peptidylphosphonates have been demonstrated to mimic effectively the transition state involved in the enzymatic hydrolysis of the peptide bond, and are commonly used as inhibitors of peptidases, and in particular of metallo-proteases [146], A solid-phase method for the introduction of the (/[P0(0Me)0] motif exploits a modified Mitsunobu reaction (Scheme 7.11) [147]. [Pg.285]


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See also in sourсe #XX -- [ Pg.193 ]




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