S-Adenosyl-Vinthionine and its Analogs as Tools for the Studies of S-Adenosyl-Methionine-Dependent Methyltransferases and Methylation
The AdoMet analog:ΓÇóHas minimal structural changes as compared to conventional analogsΓÇóIs effectively used for in-vivo labelingΓÇóForms a bi-substrate adduct with the substrate that can be easily dissociated and detectedΓÇóIn form of a bi-substrate adduct, acts as a potent selective inhibitorΓÇóContains hooks with customized reactivities to catch the substrate(s)ΓÇóHas an enhanced binding affinity to methyl-transferase as compared to conventional approachesΓÇóWould be commercially useful for the following applications:o Inhibitor leado Drug target discovery and validationo Off-target identificationo Methyl-transferase substrate identificationo Bio-conjugation
Many commonly used approaches such as mass spectrometry, immunoassays, selective tagging, and affinity enrichment have limited utility for proteomics analysis, including the assessment of methylation, which is an extremely challenging assay. S-Adenosyl-methionine (AdoMet or SAM) analogs play an important role in this regard. Prior-art discloses the use of few of these analogs such as electrophilic aziridinium. However, these are associated with certain potential limitations such as an intrinsically high reactivity and instability with limited in-vivo applications. This approach comprises the development and use of novel AdoMet analogs (such as Adovin) for study of AdoMet-Dependent Methyl-transferase based methylations.
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