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

Iacopo Galleano; John Nielsen; Andreas Stahl Madsen; Christian Adam Olsen

doi:10.1055/s-0036-1588875

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

Iacopo Galleano, John Nielsen, Andreas Stahl Madsen, Christian Adam Olsen

1 Citation (Scopus)

Abstract

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 synthesis
is scalable and does not involve chromatographic purification, making this substrate readily available in few steps.

Original language	English
Journal	SYNLETT: Accounts and Rapid Communications in Chemical Synthesis
Volume	28
Issue number	16
Pages (from-to)	2169-2173
ISSN	0936-5214
DOIs	https://doi.org/10.1055/s-0036-1588875
Publication status	Published - 2017

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title = "Scalable and Purification-Free Synthesis of a Myristoylated Fluorogenic Sirtuin Substrate",

abstract = "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.",

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

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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 -

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

Abstract

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