Synthesis and biological activity of 8-L-Ala-motilin and 8-D-Ala-motilin.
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Design, Synthesis, and Characterization of a High-Affinity Trivalent System Derived from Vancomycin and L-Lys-D-Ala-D-Ala
A trivalent derivative of vancomycin, tris(vancomycin carboxamide), [C6H3-1,3,5-(CONHC6H4-4CH2NHCOV)3 (RtV3; V ) vancomycin)], binds an analogous trivalent derivative of D-Ala-D-Ala, R′tL′3, (C6H31,3,5-[CON H(N-Ac)-L-Lys-D-Ala-D-Ala]3) in water with a dissociation constant that is approximately 4 × 10-17 M, as estimated by HPLC using a competitive assay against NR, -diacetyl-L-Lys-D-Ala-D-Ala (...
متن کاملMutational analysis of active-site residues of the enterococcal D-ala-D-Ala dipeptidase VanX and comparison with Escherichia coli D-ala-D-Ala ligase and D-ala-D-Ala carboxypeptidase VanY.
BACKGROUND Vancomycin-resistant enterococci are pathogenic bacteria that attenuate antibiotic sensitivity by producing peptidoglycan precursors that terminate in D-Ala-D-lactate rather than D-Ala-D-Ala. A key enzyme in effecting antibiotic resistance is the metallodipeptidase VanX, which reduces the cellular pool of the D-Ala-D-Ala dipeptide. RESULTS We constructed eleven mutants, using the r...
متن کاملTight Binding of a Dimeric Derivative of Vancomycin with Dimeric L-Lys-D-Ala-D-Ala
The ligand/receptor pair consisting of a synthetic dimeric derivative of vancomycin (V), linked at the C terminus by p-xylylenediamine (V-CONHCH2C6H4CH2NHCO-V), and a dimeric derivative of L-Lys-D-Ala-D-Ala, [CH2CON H(N-Ac)-L-Lys-D-Ala-D-Ala-CO2]2, provides a new system with which to study the influence of divalency on the strength of binding. A competitive assay using affinity capillary electr...
متن کاملDesign and synthesis of N-terminal cyclic motilin partial peptides: a novel pure motilin antagonist.
Motilin antagonist was designed and synthesized on the basis of the structure-activity relationship analysis of porcine motilin that we reported recently. The drug design was performed on a specific concept to reduce a flexibility of peptide conformation of porcine motilin partial peptide by its cyclization. The cyclic peptide was synthesized using Boc (tert-butyloxycarbonyl) solid phase method...
متن کاملChapter 771 Actinomadura R39 d-Ala d Ala Carboxypeptidase
bacterial penicillin-binding proteins and beta-lactamases. Antimicrob. Agents Chemother. 42(1), 1 17. [41] Davies, C., White, S.W., Nicholas, R.A. (2001). Crystal structure of a deacylation-defective mutant of penicillin-binding protein 5 at 2.3-Å resolution. J. Biol. Chem. 276(1), 616 623. [42] Nicola, G., Tomberg, J., Pratt, R.F., Nicholas, R.A., Davies, C. (2010). Crystal structures of coval...
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ژورنال
عنوان ژورنال: Chemical and Pharmaceutical Bulletin
سال: 1978
ISSN: 0009-2363,1347-5223
DOI: 10.1248/cpb.26.880