Labeled molecular imaging agents and methods of use
Imaging agents are described that comprise labeled substrates capable of being introduced into cells via the cystine/glutamate antiporter. The substrates may be used for imaging or detecting oxidative stress in cells by introducing the labeled agents into
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Page/Page column 20; 21
(2016/11/09)
Novel elastase inhibitors
This invention relates to compounds which are inhibitors of elastase, particularly human neutrophil elastase. The inhibitors are short, synthetic peptides in which the P2 moiety is substituted with various nitrogen-containing heterocyclic group
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(2008/06/13)
Inhibition of human neutrophil elastase. 4. Design, synthesis, X-ray crystallographic analysis, and structure-activity relationships for a series of P2-modified, orally active peptidyl pentafluoroethyl ketones
A series of P2-modified, orally active peptidic inhibitors of human neutrophil elastase (HNE) are reported. These pentafluoroethyl ketone-based inhibitors were designed using pentafluoroethyl ketone 1 as a model. Rational structural modifications were made at the P3, P2, and activating group (A(G)) portions of 1 based on structure-activity relationships (SAR) developed from in vitro (measured K(i)) data and information provided by modeling studies that docked inhibitor 1 into the active site of HNE. The modeling-based design was corroborated with X-ray crystallographic analysis of the complex between 1 and porcine pancreatic elastase (PPE) and subsequently the complex between 1 and HNE.
Cregge, Robert J.,Durham, Sherrie L.,Farr, Robert A.,Gallion, Steven L.,Hare, C. Michelle,Hoffman, Robert V.,Janusz, Michael J.,Kim, Hwa-Ok,Koehl, Jack R.,Mehdi, Shujaath,Metz, William A.,Peet, Norton P.,Pelton, John T.,Schreuder, Herman A.,Sunder, Shyam,Tardif, Chantal
p. 2461 - 2480
(2007/10/03)
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