Structural characterization of three novel hydroxamate-based zinc chelating inhibitors of the Clostridium botulinum serotype a neurotoxin light chain metalloprotease reveals a compact binding site resulting from 60/70 loop flexibility

Biochemistry

Volumn 50, Issue 19, 2011, Pages 4019-4028

  Thompson, Aaron A ^a   Jiao, Guan Sheng ^b   Kim, Seongjin ^b   Thai, April ^b   Cregar Hernandez, Lynne ^b   Margosiak, Stephen A ^b   Johnson, Alan T ^b   Han, Gye Won ^a   Omalley, Sean ^b   Stevens, Raymond C ^a  

^a SCRIPPS RESEARCH INSTITUTE   (United States)

^b PanThera Biopharma LLC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACTIVE SITE; ACTIVE SITE POCKET; CLOSTRIDIUM BOTULINUM; CONFORMATIONAL CHANGE; ETIOLOGICAL AGENT; INDUCED-FIT MECHANISM; LIGHT CHAIN; METALLO-PROTEASE; SEROTYPES; SMALL MOLECULE INHIBITOR; STRUCTURAL CHARACTERIZATION; STRUCTURE ACTIVITY RELATIONSHIPS; TOXIC PROTEINS; X RAY CRYSTAL STRUCTURES;

BIOSYNTHESIS; CRYSTAL STRUCTURE; ZINC;

CLOSTRIDIUM;

CHELATING AGENT; HYDROXAMIC ACID DERIVATIVE; METALLOPROTEINASE INHIBITOR; ZINC DERIVATIVE;

ARTICLE; BINDING SITE; CLOSTRIDIUM BOTULINUM; CONFORMATIONAL TRANSITION; CRYSTAL STRUCTURE; DRUG POTENCY; DRUG PROTEIN BINDING; ENZYME ACTIVE SITE; ENZYME INHIBITION; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

BINDING SITES; BOTULINUM TOXINS, TYPE A; CHELATING AGENTS; CLOSTRIDIUM BOTULINUM; CRYSTALLOGRAPHY, X-RAY; HYDROXAMIC ACIDS; LIGANDS; METALLOPROTEASES; NEUROTOXINS; PROTEIN BINDING; PROTEIN CONFORMATION; PROTEIN STRUCTURE, TERTIARY; ZINC;

CLOSTRIDIUM BOTULINUM;

EID: 79955851447     PISSN: 00062960     EISSN: 15204995     Source Type: Journal    
DOI: 10.1021/bi2001483     Document Type: Article

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