Examining Several Strategies for the Chemical Synthesis of Phosphorylated Histone H3 Reveals the Effectiveness of the Convergent Approach

Muhammad Jbara, Suman Kumar Maity, Ashraf Brik

Research output: Contribution to journalArticlepeer-review

5 Scopus citations

Abstract

Phosphorylation of Ser57 of the histone H3 was suggested to interact with the acetylated Lys56 of histone H3 and possibly affect DNA replication. Yet the exact role of Ser57 remains unknown due to difficulties in obtaining phosphorylated H3 at Ser57. Herein, we present the challenges and the solutions in the first total chemical synthesis of phosphorylated and unphosphorylated histone H3 analogues utilizing hydrazide-based native chemical ligation approach coupled with palladium-mediated thiazolidine decaging chemistry to provide each one of these analogues in highly efficient manner. We envision this synthesis would set the ground to elucidating the role of the phosphorylation and its cross-talk with acetylation mark in H3 in the DNA damage response.

Original languageEnglish
Pages (from-to)3128-3132
Number of pages5
JournalEuropean Journal of Organic Chemistry
Volume2020
Issue number21
DOIs
StatePublished - 8 Jun 2020
Externally publishedYes

Keywords

  • Chemical protein synthesis
  • Convergent synthesis
  • Histone 3
  • Palladium
  • Phosphorylation

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