Investigation on the structure of the active site of monoamine oxidase-B by affinity labeling with the selective inhibitor lazabemide and by site-directed mutagenesis
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The determination of the protonation state of enzyme active sites may be crucial for the investigation of their mechanism of action. In the bizinc beta-lactamase family of enzymes, no consensus has been reached on the protonation state of a fully conserved ...
A series of organometallic compds. of general formula [(arene)M(PTA)nXm]Y (arene = η6-C10H14, η-C5Me5); (M = Ru(II), Os(II), Rh(III) and Ir(III); X = Cl, mPTA; Y = OTf, PF6) have been screened for their cytotoxicity and ability to inhibit cathepsin B in vi ...
Structure and dynamics of substrate binding (cefotaxime) to the catalytic pocket of the mononuclear zinc-beta-lactamase from Bacillus cereus are investigated by molecular dynamics simulations. The calculations, which are based on the hydrogen-bond pattern ...
In this contribution we explore a new and simple approach for immobilizing enzymes like glucose oxidase on SU-8 surfaces to develop a smart substrate integrated in microfluidics. SU-8 is a well known photoresist often used in microfluidic prototyping. Immo ...
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We describe two general methodologies, based on filter-sandwich assays, for isolating enzymic activities from a large repertoire of protein variants expressed in the cytoplasm of E. coli cells. The enzymes are released by the freezing and thawing of bacter ...
New pyrrolidine-3,4-diol derivatives were prepared from D-(-)- and L(+)-phenylglycinol and tested for their ability to inhibit 25 commercial glycosidases. The influence of the substitution of the lateral side chain and of the pyrrolidine ring on the enzyme ...
A 33-residue de novo designed peptide ligase is reported which catalyzes the template-directed condensation of suitably activated short peptides with catalytic efficiencies in excess of 105 ([kcat/Km]/kuncat). The ligase peptide, derived from natural and d ...
The authors have performed a computational study of different protomeric states of the methionine aminopeptidase active site using a combined quantum-mech./mol. mech. simulation approach. The aim of this study was to clarify the native protonation state of ...
The emergence of drug-resistant variants is a serious side effect assocd. with acquired immune deficiency syndrome therapies based on inhibition of human immunodeficiency virus type 1 protease (HIV-1 PR). In these variants, compensatory mutations, usually ...
Telomerase, a ribonucleoprotein acting as a reverse transcriptase, has been identified as a target for cancer drug discovery. The synthetic, non-nucleosidic compound, BIBR1532, is a potent and selective telomerase inhibitor capable of inducing senescence i ...
