Discovery of Potent and Selective Inhibitors against Protein-Derived Electrophilic Cofactors
作者:Xie Wang、Zongtao Lin、Katelyn A. Bustin、Nate R. McKnight、William H. Parsons、Megan L. Matthews
DOI:10.1021/jacs.1c12748
日期:2022.3.30
they have remained blind spots in traditional activity-based protein profiling (ABPP) approaches that target nucleophiles. More recently, reverse-polarity (RP)-ABPP usinghydrazineprobes identified an electrophilic N-terminal glyoxylyl (Glox) group for the first time in secernin-3 (SCRN3). The biological function(s) of both the protein and Glox as a cofactor has not yet been pharmacologically validated
CHEMOPROTEOMIC PROFILING OF PROTEIN ELECTROPHILIC AND OXIDATIVE POST-TRANSLATIONAL MODIFICATIONS
申请人:Zenagem, LLC
公开号:US20190204336A1
公开(公告)日:2019-07-04
Chemoproteomic methods for detecting and profiling electrophilic post-translational modifications (PTMs) and oxidative PTMs in proteins are described. The methods including contacting a proteomic mixture with a probe having hydrazine and alkyne moieties or oxyamine and alkyne moieties to form a covalent linkage between the hydrazine or oxyamine moiety of the probe and the electrophilic PTM or oxidative PTM of the protein. The resulting alkyne-derivatized proteins are labelled with an azide modified tag via a click chemistry reaction. The labelled proteins can then be detected or profiled using techniques such as, for example, fluorescence imaging or mass spectrometry. Also described are protein conjugates having a covalent linkage formed by reaction of a hydrazine or oxyamine moiety of a probe with an electrophilic or oxidative PTM of a protein.
[EN] USE OF CSE INHIBITORS FOR THE TREATMENT OF CUTANEOUS INJURIES OR CONDITIONS AND SLEEP-RELATED BREATHING DISORDERS<br/>[FR] UTILISATION D'INHIBITEURS DE CSE POUR LE TRAITEMENT DE LÉSIONS OU D'AFFECTIONS CUTANÉES ET DE TROUBLES RESPIRATOIRES DU SOMMEIL
申请人:SOVA PHARMACEUTICALS INC
公开号:WO2014018571A2
公开(公告)日:2014-01-30
HYDRAZIDE COMPOUND AND HARMFUL ARTHROPOD-CONTROLLING AGENT CONTAINING THE SAME
申请人:Sumitomo Chemical Company, Limited
公开号:EP2143721B1
公开(公告)日:2012-08-15
[EN] CYSTATHIONINE-Upsilon-LYASE (CSE) INHIBITORS<br/>[FR] INHIBITEURS DE LA CYSTATHIONINE- Gamma -LYASE (CSE)
申请人:SOVA PHARMACEUTICALS INC
公开号:WO2014018570A1
公开(公告)日:2014-01-30
Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit cystathionine -γ-lyase (CSE). Also described herein are methods for using such CSE inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from CSE inhibition.