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Identification of AHCY inhibitors using novel high-throughput mass spectrometry.

Abstract：

:S-adenosylhomocysteine hydrolase (AHCY) catalyzes the reversible hydrolysis of S-adenosylhomocysteine (SAH) to adenosine and l-homocysteine. This enzyme is frequently overexpressed in many tumor types and is considered to be a validated anti-tumor target. In order to enable the development of small molecule AHCY inhibitors as targeted cancer therapeutics we developed an assay based on a RapidFire high-throughput mass spectrometry detection system, which allows the direct measurement of AHCY enzymatic activity. This technique avoids many of the problems associate with the previously reported method of using a thiol-reactive fluorescence probes to measure AHCY activity. Screening of a ∼500,000 compound library using this technique identified multiple SAH competitive hits. Co-crystal structures of the hit compounds complexed with AHCY were obtained showing that the compounds indeed bind in the SAH site of the enzyme. In addition, some hit compounds increased the SAH levels in HCT116 cells and showed growth inhibition. These compounds could be promising starting points for the optimization of cancer treatments.

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Uchiyama N,Dougan DR,Lawson JD,Kimura H,Matsumoto SI,Tanaka Y,Kawamoto T

doi

10.1016/j.bbrc.2017.05.107

subject

Has Abstract

pub_date

2017-09-09 00:00:00

pages

1-7

issue

1

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(17)30989-0

journal_volume

491

pub_type

杂志文章

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