Yang, Peng-Yu published the artcileChemical Modification and Organelle-Specific Localization of Orlistat-Like Natural-Product-Based Probes, COA of Formula: C18H34N4O5S, the publication is Chemistry – An Asian Journal (2011), 6(10), 2762-2775, database is CAplus and MEDLINE.
Orlistat, also known as tetrahydrolipstatin (THL), is an FDA-approved anti-obesity drug with potential anti-cancer activity. Previously, we developed a chem. proteomic approach, based on the Orlistat-like probe (I) for large-scale identification of unknown cellular targets of Orlistat in human hepatocytes. In this article, we report the chem. synthesis and biol. evaluation of an expanded set of Orlistat-like compounds, with the intention to further dissect and manipulate potential cellular targets of Orlistat. In doing so, we carried out proteome-wide activity-based profiling and large-scale pull-down/LCMS anal. of these compounds in live HepG2 cells, and successfully identified many putative cellular targets for Orlistat and its structural analogs. By qual. assessing the spectra counts of potential protein hits against each of the seventeen Orlistat analogs, we obtained both common and unique targets of these probes. Our results revealed that subtle structural modifications of Orlistat led to noticeable changes in both the cellular potency and target profiles of the drug. In order to further improve the cellular activity of Orlistat, we successfully applied the well-established AGT/SNAP-tag technol. to our cell-permeable, benzylguanine (BG)-containing Orlistat variant (II). We showed that the drug could be delivered and effectively retained in different sub-cellular organelles of living cells. This strategy may provide a general and highly effective chem. tool for the potential sub-cellular targeting of small mol. drugs.
Chemistry – An Asian Journal published new progress about 359860-27-8. 359860-27-8 belongs to imidazoles-derivatives, auxiliary class Other Aliphatic Heterocyclic,Chiral,Amine,Amide,Ether,Inhibitor, name is N-(2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)ethyl)-5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamide, and the molecular formula is C11H9NO3, COA of Formula: C18H34N4O5S.
Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem