Targeted Covalent Inhibition of Telomerase.

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.

SUBMITTER: Betori RC 

PROVIDER: S-EPMC7233141 | biostudies-literature | 2020 Mar

REPOSITORIES: biostudies-literature