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Screening of the National Cancer Institute Chemical Diversity Set for Potential SPM‐1 Metallo‐β‐Lactamase Inhibitors
Author(s) -
Hickman Lauren,
Toney Jeffrey,
Thomas Janice
Publication year - 2006
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.20.4.a462-d
Subject(s) - diversity (politics) , cancer , set (abstract data type) , computational biology , chemistry , medicine , biology , computer science , political science , law , programming language
Carbapenem resistance in bacteria is increasing in the clinic due to several mechanisms, including class B or metallo‐ß‐lactamases (MBLs). While several chemical classes of MBL inhibitors have been identified that can reverse carbapenem resistance in clinical pathogens, we are searching for a novel chemical class of MBL inhibitors exhibiting greater broad spectrum activity. The National Cancer Institute Chemical Diversity Set was screened for SPM‐1 metallo‐ß‐Lactamase inhibition. Out of approximately 2000 compounds, up to18 were identified as having greater than fifty percent SPM‐1 inhibition at 40mM. These actives are currently being studied in further detail for specificity against SPM‐1.