《Catch and Anchor Approach To Combat Both Toxicity and Longevity of Botulinum Toxin A》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Lin, Lucy; Olson, Margaret E.; Sugane, Takashi; Turner, Lewis D.; Tararina, Margarita A.; Nielsen, Alexander L.; Kurbanov, Elbek K.; Pellett, Sabine; Johnson, Eric A.; Cohen, Seth M.; Allen, Karen N.; Janda, Kim D.. Reference of 8-Bromooctanoic acid The article mentions the following:
Botulinum neurotoxins have remarkable persistence (~weeks to months in cells), outlasting the small-mol. inhibitors designed to target them. To address this disconnect, inhibitors bearing two pharmacophores-a zinc binding group and a Cys-reactive warhead-were designed to leverage both affinity and reactivity. A series of first-generation bifunctional inhibitors was achieved through structure-based inhibitor design. Through X-ray crystallog., engagement of both the catalytic Zn2+ and Cys165 was confirmed. A second-generation series improved on affinity by incorporating known reversible inhibitor pharmacophores; the mechanism was confirmed by exhaustive dialysis, mass spectrometry, and in vitro evaluation against the C165S mutant. Finally, a third-generation inhibitor was shown to have good cellular activity and low toxicity. In addition to our findings, an alternative method of modeling time-dependent inhibition that simplifies assay setup and allows comparison of inhibition models is discussed. In the part of experimental materials, we found many familiar compounds, such as 8-Bromooctanoic acid(cas: 17696-11-6Reference of 8-Bromooctanoic acid)
8-Bromooctanoic acid(cas: 17696-11-6) acid is used in the synthesis of 8-(N-Methyl-4,4′-bipyridinyl)- octanoic acid. 8-Mercaptooctanoic acid was prepared from 8-bromooctanoic acid.Reference of 8-Bromooctanoic acid
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary