MersV1, Main, Exploration, bibRecord, 002D55

A peptide inhibitor of MurA UDP-N-acetylglucosamine enolpyruvyl transferase: the first committed step in peptidoglycan biosynthesis.

Identifieur interne : 002D55 ( Main/Exploration ); précédent : 002D54; suivant : 002D56

A peptide inhibitor of MurA UDP-N-acetylglucosamine enolpyruvyl transferase: the first committed step in peptidoglycan biosynthesis.

Auteurs : José Molina-L Pez [Mexique] ; François Sanschagrin ; Roger C. Levesque

Source :

Peptides [ 0196-9781 ] ; 2006.

RBID : pubmed:17030076

Descripteurs français

KwdFr :
- Alkyl et aryl transferases (antagonistes et inhibiteurs), Alkyl et aryl transferases (métabolisme), Données de séquences moléculaires, Peptides (physiologie), Peptidoglycane (biosynthèse), Pseudomonas aeruginosa (enzymologie), Séquence d'acides aminés, Uridine diphosphate ose (métabolisme).
MESH :
- antagonistes et inhibiteurs : Alkyl et aryl transferases.
- biosynthèse : Peptidoglycane.
- enzymologie : Pseudomonas aeruginosa.
- métabolisme : Alkyl et aryl transferases, Uridine diphosphate ose.
- physiologie : Peptides.
- Données de séquences moléculaires, Séquence d'acides aminés.

English descriptors

KwdEn :
- Alkyl and Aryl Transferases (antagonists & inhibitors), Alkyl and Aryl Transferases (metabolism), Amino Acid Sequence, Molecular Sequence Data, Peptides (physiology), Peptidoglycan (biosynthesis), Pseudomonas aeruginosa (enzymology), Uridine Diphosphate Sugars (metabolism).
MESH :
- chemical , antagonists & inhibitors : Alkyl and Aryl Transferases.
- chemical , biosynthesis : Peptidoglycan.
- chemical , metabolism : Alkyl and Aryl Transferases, Uridine Diphosphate Sugars.
- chemical , physiology : Peptides.
- enzymology : Pseudomonas aeruginosa.
- Amino Acid Sequence, Molecular Sequence Data.

Abstract

The MurA enzyme from Pseudomonas aeruginosa was purified to homogeneity and found to be biologically active as a UDP-N-acetylglucosamine (UNAG) enolpyruvyl transferase in a coupled enzyme assay where ATPase activity was measured by the release of inorganic phosphate. A microtiter plate assay coupled to competitive biopanning using the UDP-N-acetylglucosamine was used to screen 10(9) C-7-C and 12-mers peptides from phage display libraries. From 60 phage-encoded peptides identified after the fourth round of biopanning, deduced amino acid sequences were aligned and two peptides were synthesized and tested for inhibition of the MurA-catalyzed reaction. The PEP 1354 peptide inhibited the ATPase activity of MurA with an IC(50) value of 200muM and was found to be a competitive inhibitor of UNAG. The pre-incubation of MurA with inhibitor indicated a time-independent inhibition. This time-dependent inhibition is the first report of peptide inhibitors of MurA, which represent the scaffold for the synthesis of inhibitory peptidomimetic molecules.

DOI: 10.1016/j.peptides.2006.08.023
PubMed: 17030076

Affiliations:

Mexique

Le document en format XML

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<term>Peptides (physiologie)</term>
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<front><div type="abstract" xml:lang="en">The MurA enzyme from Pseudomonas aeruginosa was purified to homogeneity and found to be biologically active as a UDP-N-acetylglucosamine (UNAG) enolpyruvyl transferase in a coupled enzyme assay where ATPase activity was measured by the release of inorganic phosphate. A microtiter plate assay coupled to competitive biopanning using the UDP-N-acetylglucosamine was used to screen 10(9) C-7-C and 12-mers peptides from phage display libraries. From 60 phage-encoded peptides identified after the fourth round of biopanning, deduced amino acid sequences were aligned and two peptides were synthesized and tested for inhibition of the MurA-catalyzed reaction. The PEP 1354 peptide inhibited the ATPase activity of MurA with an IC(50) value of 200muM and was found to be a competitive inhibitor of UNAG. The pre-incubation of MurA with inhibitor indicated a time-independent inhibition. This time-dependent inhibition is the first report of peptide inhibitors of MurA, which represent the scaffold for the synthesis of inhibitory peptidomimetic molecules.</div>
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<country name="Mexique"><noRegion><name sortKey="Molina L Pez, Jose" sort="Molina L Pez, Jose" uniqKey="Molina L Pez J" first="José" last="Molina-L Pez">José Molina-L Pez</name>
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A peptide inhibitor of MurA UDP-N-acetylglucosamine enolpyruvyl transferase: the first committed step in peptidoglycan biosynthesis.

A peptide inhibitor of MurA UDP-N-acetylglucosamine enolpyruvyl transferase: the first committed step in peptidoglycan biosynthesis.

Source :

Descripteurs français

English descriptors

Abstract

Links toward previous steps (curation, corpus...)

Le document en format XML

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