Details

Autor(en) / Beteiligte

• Zhao, Le
• Dunne, Christine E.
• Clausen, Dane J.
• Roberts, Justin M.
• Paulk, Joshiawa
• Liu, Haining
• Wiest, Olaf G.
• Bradner, James E.
• Williams, Robert M.

Titel

Synthesis and Biochemical Evaluation of Biotinylated Conjugates of Largazole Analogues: Selective Class I Histone Deacetylase Inhibitors

Ist Teil von

• Israel journal of chemistry, 2017-04, Vol.57 (3-4), p.319-330

Ort / Verlag

Germany: Wiley Subscription Services, Inc

Erscheinungsjahr

2017

Link zum Volltext

Quelle

Wiley Online Library - AutoHoldings Journals

Beschreibungen/Notizen

• The synthesis of biotinylated conjugates of synthetic analogues of the potent and selective histone deacetylase (HDAC) inhibitor largazole is reported. The thiazole moiety of the parent compound's cap group was derivatized to allow the chemical conjugation to biotin. The derivatized largazole analogues were assayed across a panel of HDACs 1–9 and retained potent and selective inhibitory activity towards the class I HDAC isoforms. The biotinylated conjugate was further shown to pull down HDACs 1, 2, and 3.