66831-16-1Relevant articles and documents
Labeled molecular imaging agents and methods of use
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Page/Page column 20; 21, (2016/11/09)
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
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
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)
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.
