Targeted Covalent Inhibition of Telomerase

Overview

Journal ACS Chem Biol

Publisher American Chemical Society

Specialties Biochemistry
Biology

Date 2020 Feb 5

PMID 32017522

Citations 5

Authors

Rick C Betori

Yue Liu

Rama K Mishra

Scott B Cohen

Stephen J Kron

Karl A Scheidt

Affiliations

Soon will be listed here.

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.

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