14790-63-7Relevant academic research and scientific papers
LIVER PRODRUGS OF MITOCHONDRIAL PROTON IONOPHORES
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Page/Page column 50; 51, (2018/06/06)
The present invention provides novel liver-targeted prodrugs of mitochondrial proton ionophores. These compounds have utility in medicine including their use in treatment of diseases such as NASH and NAFLD.
A Mechanism-Based Approach to Screening Metagenomic Libraries for Discovery of Unconventional Glycosidases
Nasseri, Seyed Amirhossein,Betschart, Leo,Opaleva, Daria,Rahfeld, Peter,Withers, Stephen G.
supporting information, p. 11359 - 11364 (2018/08/28)
Functional metagenomics has opened new opportunities for enzyme discovery. To exploit the full potential of this new tool, the design of selective screens is essential, especially when searching for rare enzymes. To identify novel glycosidases that employ cleavage strategies other than the conventional Koshland mechanisms, a suitable screen was needed. Focusing on the unsaturated glucuronidases (UGLs), it was found that use of simple aryl glycoside substrates did not allow sufficient discrimination against β-glucuronidases, which are widespread in bacteria. While conventional glycosidases cannot generally hydrolyze thioglycosides efficiently, UGLs follow a distinct mechanism that allows them to do so. Thus, fluorogenic thioglycoside substrates featuring thiol-based self-immolative linkers were synthesized and assessed as selective substrates. The generality of the approach was validated with another family of unconventional glycosidases, the GH4 enzymes. Finally, the utility of these substrates was tested by screening a small metagenomic library.
Chromogenic carbamate and acetal substrates for glycosaminidases
Chibba, Anthony,Dasgupta, Somnath,Yakandawala, Nandadeva,Madhyastha, Srinivasa,Nitz, Mark
scheme or table, p. 549 - 558 (2012/06/01)
The enzyme Dispersin B is a medicinally relevant β-hexosaminidase with potential for use in the treatment of biofilm-related infections. Here we describe the synthesis and evaluation of a p-nitrophenyl glycosyl carbamate and a p-nitrophenyl glycosyl aceta
