123729-66-8Relevant academic research and scientific papers
Targeting the Src Homology 2 (SH2) Domain of Signal Transducer and Activator of Transcription 6 (STAT6) with Cell-Permeable, Phosphatase-Stable Phosphopeptide Mimics Potently Inhibits Tyr641 Phosphorylation and Transcriptional Activity
Mandal, Pijus K.,Morlacchi, Pietro,Knight, J. Morgan,Link, Todd M.,Lee, Gilbert R.,Nurieva, Roza,Singh, Divyendu,Dhanik, Ankur,Kavraki, Lydia,Corry, David B.,Ladbury, John E.,McMurray, John S.
, p. 8970 - 8984 (2015/12/09)
Signal transducer and activator of transcription 6 (STAT6) transmits signals from cytokines IL-4 and IL-13 and is activated in allergic airway disease. We are developing phosphopeptide mimetics targeting the SH2 domain of STAT6 to block recruitment to phosphotyrosine residues on IL-4 or IL-13 receptors and subsequent Tyr641 phosphorylation to inhibit the expression of genes contributing to asthma. Structure-affinity relationship studies showed that phosphopeptides based on Tyr631 from IL-4Rα bind with weak affinity to STAT6, whereas replacing the pY+3 residue with simple aryl and alkyl amides resulted in affinities in the mid to low nM range. A set of phosphatase-stable, cell-permeable prodrug analogues inhibited cytokine-stimulated STAT6 phosphorylation in both Beas-2B human airway cells and primary mouse T-lymphocytes at concentrations as low as 100 nM. IL-13-stimulated expression of CCL26 (eotaxin-3) was inhibited in a dose-dependent manner, demonstrating that targeting the SH2 domain blocks both phosphorylation and transcriptional activity of STAT6.
Synthesis and catalytic activities of (S)-1-formylpyrrolidine-2-carboxylic acid derivatives for the enantioselective reductions of both a ketone and a ketimine
Chen, Zhenfei,Zhang, Anjiang,Zhang, Lixue,Zhang, Jing,Lei, Xinxiang
experimental part, p. 266 - 269 (2009/04/10)
A series of (S)-1-formylpyrrolidine-2-carboxylic acid derivatives (6a-t) have been synthesised and examined as chiral organocatalysts in the asymmetric reduction of both ketone 2 and ketimine 3. These organic activators afforded good to moderate enantiose
DI- AND TRIPEPTIDE N-ALKYL- AND N-ARALKYL AMIDES AS CHYMOTRYPSIN INHIBITORS
Kasafirek, Evzen,Sutiakova, Irena,Bartik, Michal,Sturc, Antonin
, p. 2877 - 2883 (2007/10/02)
Two competitive inhibitors of chymotrypsin, Glt-Ala-Ala-Leu-EtPh and Glt-Ala-Ala-Pro-NH-EtPh, were synthesized and their inhibition constants Ki were determined.The Ki-determination was carried also with a set of peptides of type X-(
