Chemical Modifications of Peptide Sequences via S-Alkylation Reaction
摘要:
A chemoselective, convenient, and mild synthetic strategy to modify peptides on a cysteine sulfhydryl group is described. It simply requires activated molecular sieves to selectively promote S-alkylation in the presence of peptide nucleophilic functionalities. The procedure is easy to perform, fast, and provides high yields even in the case of poor electrophilic groups. Moreover, the method allows an efficient one-pot poly alkylation, proving that the sulfhydryl reactivity does not rely on its specific position within the peptide sequence.
[EN] BENZODIOXEPINE AND BENZODIOXINE COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN FOR THE TREATMENT OF DIABETES<br/>[FR] BENZODIOXÉPINE ET COMPOSÉS DE BENZODIOXINE QUI INTERAGISSENT AVEC LA PROTÉINE RÉGULATRICE DE LA GLUCOKINASE POUR LE TRAITEMENT DU DIABÈTE
申请人:AMGEN INC
公开号:WO2012138776A1
公开(公告)日:2012-10-11
The present invention relates to compounds of formula I or II, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
The invention relates to a method for labeling and fragmenting a single- or double-stranded deoxyribonucleic acid (DNA) comprising the following steps:
chemically fragmenting the DNA by creating at least one abasic site on said DNA,
attaching a marker to at least one of the fragments by means of a labeling reagent, said reagent covalently and predominantly coupling to at least one phosphate of said fragment.
The invention finds a preferred application in the field of diagnosis.
[EN] METHODS TO DETERMINE KDM1A TARGET ENGAGEMENT AND CHEMOPROBES USEFUL THEREFOR<br/>[FR] PROCÉDÉS DE DÉTERMINATION DE L'ENGAGEMENT D'UNE CIBLE KDM1A ET CHIMIOSONDES UTILES CORRESPONDANTES
申请人:ORYZON GENOMICS SA
公开号:WO2017158136A1
公开(公告)日:2017-09-21
The invention relates to methods to determine KDM1A target engagement and chemoprobes useful therefor. In particular, the invention relates to non-peptidic KDM1A chemoprobes carrying a tag or label that can be used to assess KDM1A target engagement in cells and tissues. These chemoprobes can also be used to identify KDM1A interacting factors and analyze expression levels of KDM1A.
CHEMOSENSOR AND A METHOD OF DETECTING PALLADIUM IONS
申请人:King Fahd University of Petroleum and Minerals
公开号:US20200392148A1
公开(公告)日:2020-12-17
A palladium selective chemosensor based on a fluorescein-allyloxy benzene scaffold and a method of detecting palladium ions in a fluid sample with the chemosensor, whereby the fluid sample is contacted with a solution that includes water and the chemosensor to form a mixture. An ultraviolet visible absorption profile and/or a fluorescence emission profile of the mixture is measured to determine a presence or absence of palladium ions in the fluid sample, wherein the chemosensor has an ultraviolet visible absorption peak at 315 to 325 nm and a fluorescence emissions peak at 380 to 400 nm in the solution, and wherein a bathochromic shift in the ultraviolet visible absorption peak to 338 to 342 nm in the mixture and/or a bathochromic shift in the fluorescence emissions peak to 530 to 550 nm in the mixture indicates the presence of palladium ions in the fluid sample.
Methods are provided for detecting formation of oligomeric complexes of molecules on the surface of cell membranes. These methods employ pairs of tagged probes and cleaving probes, each of which binds specificly to a cell surface molecule. The tagged probe includes a molecular tag that is linked to a first binding compound through a cleavable linkage, and the cleaving probe includes a second binding agent and a cleavage-inducing moiety that can cleave the linkage when within a defined proximity thereto. Binding of the two probes to cell surface molecules that have formed an oligomeric complex results in release of the molecular tag from the binding compound, providing a measure of formation of the complex.