双吖丙啶
化学
SIRT2
光亲和标记
锡尔图因
肽
活动站点
组合化学
结合位点
共价键
立体化学
质谱法
酶
生物化学
有机化学
色谱法
NAD+激酶
作者
Tina Seifert,Marcus Malo,Johan Lengqvist,Carina Sihlbom,Elina M. Jarho,Kristina Luthman
标识
DOI:10.1021/acs.jmedchem.6b01117
摘要
Photoaffinity labeling (PAL) was used to identify the binding site of chroman-4-one-based SIRT2-selective inhibitors. The photoactive diazirine 4, a potent SIRT2 inhibitor, was subjected to detailed photochemical characterization. In PAL experiments with SIRT2, a tryptic peptide originating from the covalent attachment of photoactivated 4 was identified. The peptide covers both the active site of SIRT2 and the proposed binding site of chroman-4-one-based inhibitors. A high-power LED was used as source for the monochromatic UV light enabling rapid photoactivation.
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