- Design and synthesis of macrocyclic peptidyl hydroxamates as peptide deformylase inhibitors
[作者:Shen, G; Zhu, J; Simpson, AM; Pei, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3060-3063 , 文章类型: Proceedings Paper,,卷期:2008年18-10]
- Macrocyclic peptidyl hydroxamates were designed, synthesized, and evaluated as peptide deformylase (PDF) inhibitors. The most potent compound exhibited tight, slow-binding inhibition of Escherichia coli PDF (K-I* = 4.4 n...
- Conformational analyses of thiirane-based gelatinase inhibitors
[作者:Lee, M; Hesek, D; Shi, Q; Noll, BC; Fisher, JF; Chang, M; Mobashery, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3064-3067 , 文章类型: Proceedings Paper,,卷期:2008年18-10]
- SB-3CT is a thiirane-containing inhibitor of the gelatinase class of matrix metalloprotease enzymes. In support of the mechanistic study of this inhibition, the conformational analyses of SB-3CT (and of two methyl-substi...
- Synthetic ligands that activate and inhibit a quorum-sensing regulator in Pseudomonas aeruginosa
[作者:Mattmann, ME; Geske, GD; Worzalla, GA; Chandler, JR; Sappington, KJ; Greenberg, EP; Blackwell, HE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3072-3075 , 文章类型: Proceedings Paper,,卷期:2008年18-10]
- The transcription factor QscR is a regulator of quorum sensing in Pseudomonas aeruginosa and plays a role in controlling virulence in this prevalent opportunistic pathogen. This study outlines the discovery of a set of s...
- New insights into the first oxidative phenol coupling reaction during vancomycin biosynthesis
[作者:Geib, N; Woithe, K; Zerbe, K; Li, DB; Robinson, JA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3081-3084 , 文章类型: Proceedings Paper,,卷期:2008年18-10]
- OxyB catalyzes the first oxidative phenol coupling reaction in vancomycin biosynthesis. OxyB is a P450 hemoprotein whose activity is strictly dependent upon the presence of molecular oxygen. Here, it was shown that label...
- Substrate specificity and diastereoselectivity of strictosidine glucosidase, a key enzyme in monoterpene indole alkaloid biosynthesis
[作者:Yerkes, N; Wu, JX; McCoy, E; Galan, MC; Chen, S; O'Connor, SE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3095-3098 , 文章类型: Proceedings Paper,,卷期:2008年18-10]
- Strictosidine glucosidase (SGD) from Catharanthus roseus catalyzes the deglycosylation of strictosidine, an intermediate from which thousands of monoterpene indole alkaloids are derived. The steady-state kinetics of SGD ...
- Design and characterization of mechanism-based inhibitors for the tyrosine aminomutase SgTAM
[作者:Montavon, TJ; Christianson, CV; Festin, GM; Shen, B; Bruner, SD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3099-3102 , 文章类型: Proceedings Paper,,卷期:2008年18-10]
- The synthesis and evaluation of two classes of inhibitors for SgTAM, a 4-methylideneimidazole-5-one (MIO) containing tyrosine aminomutase, are described. A mechanism-based strategy was used to design analogs that mimic t...
- Top-down mass spectrometry on low-resolution instruments: Characterization of phosphopantetheinylated carrier domains in polyketide and non-ribosomal biosynthetic pathways
[作者:Meluzzi, D; Zheng, WH; Hensler, M; Nizet, V; Dorrestein, PC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3107-3111 , 文章类型: Proceedings Paper,,卷期:2008年18-10]
- Mass spectrometry (MS) is an important tool for studying non-ribosomal peptide, polyketide, and fatty acid biosynthesis. Here we describe a new approach using multi-stage tandem MS on a common ion trap instrument to obta...
- Functionalization of the 4,4-difluoro-4-bora-3a, 4a-diaza-s-indacene (BODIPY) core
[作者:Li, L; Nguyen, B; Burgess, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3112-3116 , 文章类型: Proceedings Paper,,卷期:2008年18-10]
- The new BODIPY systems 1 and 2 were prepared and then used as substrates to explore SNAr and F-B displacement reactions. Chloride was easily displaced from 1 by a piperidine/ester, methylmagnesium bromide selectively dis...
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