138849-01-1Relevant articles and documents
SULFOXONIUM YLIDE DERIVATIVES AS PROBES FOR CYSTEINE PROTEASE
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Paragraph 0451; 0455-0457; 0461-0463, (2020/07/14)
The present invention relates to compounds of formula I bearing a sulfoxonium ylide moiety as warhead, or salts thereof. Such compounds can be used as activity-based probes for cysteine proteases such as cathepsin X, in methods of detecting cysteine protease activity and in related diagnostic or therapeutic methods.
Expanding the scope of PNA-encoded libraries: divergent synthesis of libraries targeting cysteine, serine and metallo-proteases as well as tyrosine phosphatases
Debaene, Fran?ois,Da Silva, Julien A.,Pianowski, Zbigniew,Duran, Fernando J.,Winssinger, Nicolas
, p. 6577 - 6586 (2008/02/05)
Seven PNA-encoded combinatorial libraries targeting proteases and phosphatases with covalent reversible and irreversible mechanism-based inhibitors were prepared. The libraries were synthesized using modified PNA monomers, which dramatically increase the water solubility of the libraries in biologically relevant buffers. The libraries were shown to selectively inhibit targeted enzymes.
Oral Bioavailability of a New Class of μ-Opioid Receptor Agonists Containing 3,6-Bis[Dmt-NH(CH2)n]-2(1H)-pyrazinone with Central-Mediated Analgesia
Jinsmaa, Yunden,Miyazaki, Anna,Fujita, Yoshio,Li, Tingyou,Fujisawa, Yutaka,Shiotani, Kimitaka,Tsuda, Yuko,Yokoi, Toshio,Ambo, Akihiro,Sasaki, Yusuke,Bryant, Sharon D.,Lazarus, Lawrence H.,Okada, Yoshio
, p. 2599 - 2610 (2007/10/03)
The inability of opioid peptides to be transported through epithelial membranes in the gastrointestinal tract and pass the blood-brain barrier limits their effectiveness for oral application in an antinociceptive treatment regime. To overcome this limitat
FunctionaIized erythro N-protected α-amino epoxides. Stereocontrolled synthesis and biological activity
Albeck, Amnon,Estreicher, Gary I.
, p. 5325 - 5338 (2007/10/03)
Erythro N-protected α-amino epoxides, derived from α-amino acids bearing functionalized side chains, were synthesized. The key synthetic step is a stereoselective reduction of the corresponding haloketone either to the halohydrin or directly to the epoxid