Water-soluble prodrugs of cyclosporine A with tailored conversion rates
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The preparation of oligoribonucleotides is of great interest for structural and functional investigations in biomolecular chemistry and biology. Relevant RNAs are relatively long and contain often modifications. Two methods for their preparation are curren ...
Some nonenzymic epoxide-initiated polyolefin cyclisations are reported. The presented molecules are partially constrained analogues of (3S)-oxidosqualene, the natural substrate to many important cyclase enzymes. These model compounds feature a preformed C- ...
The activity of penicillin acylase has been studied in aq. and org. solvents, as free enzyme as well as immobilized within the membrane of liq.-core capsules. The activity of the enzyme is inhibited by the accumulation of the products of the hydrolysis rea ...
We present a new antibody-directed enzyme prodrug therapy strategy (ADEPT) based on a post-proline cleaving endopeptidase and prodrugs, in which cytotoxic moieties are linked to a proline-contg. peptide. Human prolyl endopeptidase was expressed in Escheric ...
Cyclosporins are a family of hydrophobic cyclic undecapeptides produced by the fungus Tolypocladium niveum. The main metabolite cyclosporin A (CsA, see Scheme, R = R' = H) is the first line drug currently used to prevent rejection of organ transplants. Its ...
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 ...
A new route for the preparation of four new indolizidines, (1R,2S,6S,7S,8aS)- and (1R,2S,6R,7R,8aS)-1,2,6,7-tetrahydroxyindolizidine (30 and 32) and (1S,2R,7S,8S,8a-R)- and (1S,2R,7R,8R,8a-R)1,2,7,8-tetrahydroxyindolizidine (44 and 46), is reported. The sy ...
Combinatorial mutagenesis was used to investigate the role of three key residues in cytochrome c peroxidase (CCP) from Saccharomyces cerevisiae, Arg48, Trp51, and Trp191, in control of the reactivity and selectivity of the heme-contg. enzyme. Libraries wer ...
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 ...
A symposium report. We report on the synthesis of TASP (template assembled synthetic proteins) mols. able to bind to neurotensin Y and angiotensin II receptors, in which a-cyclodextrin is used as template. [on SciFinder (R)] ...