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| [[Image:2gqn.jpg|left|200px]] | | {{Seed}} |
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| {{STRUCTURE_2gqn| PDB=2gqn | SCENE= }} | | {{STRUCTURE_2gqn| PDB=2gqn | SCENE= }} |
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| '''Cystathionine Beta-Lyase (CBL) from Escherichia Coli in complex with N-Hydrazinocarbonylmethyl-2-Nitro-Benzamide'''
| | ===Cystathionine Beta-Lyase (CBL) from Escherichia Coli in complex with N-Hydrazinocarbonylmethyl-2-Nitro-Benzamide=== |
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| ==Overview==
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| The biosynthesis of methionine is an attractive antibiotic target given its importance in protein and DNA metabolism and its absence in mammals. We have performed a high-throughput screen of the methionine biosynthesis enzyme cystathionine beta-lyase (CBL) against a library of 50 000 small molecules and have identified several compounds that inhibit CBL enzyme activity in vitro. These hit molecules were of two classes: those that blocked CBL activity with mixed steady-state inhibition and those that covalently interacted with the enzyme at the active site pyridoxal phosphate cofactor with slow-binding inhibition kinetics. We determined the crystal structure of one of the slow-binding inhibitors in complex with CBL and used this structure as a guide in the synthesis of a small, focused library of analogues, some of which had improved enzyme inhibition properties. These studies provide the first lead molecules for antimicrobial agents that target cystathionine beta-lyase in methionine biosynthesis. | | The line below this paragraph, {{ABSTRACT_PUBMED_17300162}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 17300162 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_17300162}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Plp cofactor covalently bount to blp inhibitor]] | | [[Category: Plp cofactor covalently bount to blp inhibitor]] |
| [[Category: Protein-inhibitor complex]] | | [[Category: Protein-inhibitor complex]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:24:41 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 03:45:11 2008'' |