650604-97-0Relevant academic research and scientific papers
γ-Difluorolysine as a19F NMR probe for histone lysine methyltransferases and acetyltransferases
Hintzen, Jordi C. J.,Jian, Jie,Luo, Yan,Mecinovi?, Jasmin,Porzberg, Miriam R. B.,Proietti, Giordano,White, Paul B.
, p. 6788 - 6791 (2021/07/13)
Histone lysine methylation and acetylation are important posttranslational modifications that regulate gene expression in humans. Due to the interplay of these two modifications, new chemical methods to study lysine posttranslational modifications are highly desired. Here, we report the use of γ-difluorolysine as a lysine mimic and19F NMR probe for examinations of histone methylation and acetylation.
4-Fluorinated L-lysine analogs as selective i-NOS inhibitors: Methodology for introducing fluorine into the lysine side chain
Hallinan, E. Ann,Kramer, Steven W.,Houdek, Stephen C.,Moore, William M.,Jerome, Gina M.,Spangler, Dale P.,Stevens, Anna M.,Shieh, Huey S.,Manning, Pamela T.,Pitzele, Barnett S.
, p. 3527 - 3534 (2007/10/03)
In the literature, the introduction of fluorine into bioactive molecules has been known to enhance the biological activity relative to the parent molecule. Described in this article is the synthesis of 4R-fluoro-L-NIL (12) and 4,4-difluoro-L-NIL (23) as part of our iNOS program. Both 12 and 23 were found to be selective iNOS inhibitors as shown in Table 2 below. Secondarily, methodology to synthesize orthogonally protected 4-fluoro-L-lysine and 4,4-difluoro-L-lysine has been developed.
