A versatile strategy for the design and synthesis of novel ADP conjugates and their evaluation as potential poly(ADP-ribose) polymerase 1 inhibitors

Yuliya V. Sherstyuk, Alexandra L. Zakharenko, Mikhail M. Kutuzov, Polina V. Chalova, Maria V. Sukhanova, Olga I. Lavrik, Vladimir N. Silnikov, Tatyana V. Abramova

Результат исследования: Научные публикации в периодических изданияхстатьярецензирование

4 Цитирования (Scopus)

Аннотация

Abstract: A versatile strategy for the synthesis of NAD + mimetics was developed, involving an efficient pyrophosphate linkage formation in key conjugates containing a functional amino group which acts as useful reactive anchor for further derivatization. These NAD + mimetics consist of ADP conjugated through a diphosphate chain to an extended aliphatic linker bearing an aromatic acid residue. A number of conjugates containing aromatic carboxylic acids were found to inhibit poly(ADP-ribose) synthesis catalyzed by poly(ADP-ribose) polymerase-1 (PARP-1). A new class of potential PARP-1 inhibitors mimicking NAD +, a substrate in the PARP-1 catalyzed reaction, was proposed.

Язык оригиналаанглийский
Страницы (с-по)101-113
Число страниц13
ЖурналMolecular Diversity
Том21
Номер выпуска1
DOI
СостояниеОпубликовано - 1 февр. 2017

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