Scalable and Purification-Free Synthesis of a Myristoylated Fluorogenic Sirtuin Substrate

TY - JOUR

T1 - Scalable and Purification-Free Synthesis of a Myristoylated Fluorogenic Sirtuin Substrate

AU - Galleano, Iacopo

AU - Nielsen, John

AU - Stahl Madsen, Andreas

AU - Olsen, Christian Adam

PY - 2017

Y1 - 2017

N2 - Sirtuins are NAD+-dependent deacylases involved in the regulation of fundamental cellular processes in both normal and diseased cells. Therefore, the development of selective inhibitors for this class of enzymes is of great interest. Herein, we report an optimized synthesis of Ac-ETDK(myristoyl)-AMC, a sirtuin 2 substrate that can be used to profile inhibitors in fluorescence-based assays. The presented synthesisis scalable and does not involve chromatographic purification, making this substrate readily available in few steps.

AB - Sirtuins are NAD+-dependent deacylases involved in the regulation of fundamental cellular processes in both normal and diseased cells. Therefore, the development of selective inhibitors for this class of enzymes is of great interest. Herein, we report an optimized synthesis of Ac-ETDK(myristoyl)-AMC, a sirtuin 2 substrate that can be used to profile inhibitors in fluorescence-based assays. The presented synthesisis scalable and does not involve chromatographic purification, making this substrate readily available in few steps.

U2 - 10.1055/s-0036-1588875

DO - 10.1055/s-0036-1588875

M3 - Letter

SN - 0936-5214

VL - 28

SP - 2169

EP - 2173

JO - SYNLETT: Accounts and Rapid Communications in Chemical Synthesis

JF - SYNLETT: Accounts and Rapid Communications in Chemical Synthesis

IS - 16

ER -