Targeted Covalent Inhibition of Telomerase

Rick C. Betori, Yue Liu, Rama K. Mishra, Scott B. Cohen, Stephen J. Kron, Karl A. Scheidt*

*Corresponding author for this work

Research output: Contribution to journalArticle

2 Scopus citations

Abstract

Telomerase is a ribonuceloprotein complex responsible for maintaining telomeres and protecting chromosomal integrity. The human telomerase reverse transcriptase (hTERT) is expressed in 90% of cancer cells where it confers the capacity for limitless proliferation. Along with its established role in telomere lengthening, telomerase also serves noncanonical extra-telomeric roles in oncogenic signaling, resistance to apoptosis, and enhanced DNA damage response. We report a new class of natural-product-inspired covalent inhibitors of telomerase that target the catalytic active site.

Original languageEnglish (US)
Pages (from-to)706-717
Number of pages12
JournalACS chemical biology
Volume15
Issue number3
DOIs
StatePublished - Mar 20 2020

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine

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