GLI1-Inducible Glucuronidation Targets a Broad Spectrum of Drugs

ACS Chem Biol. 2019 Mar 15;14(3):348-355. doi: 10.1021/acschembio.8b01118. Epub 2019 Feb 19.

Abstract

Cancer therapies are plagued by resistance. Previously, we discovered a novel form of cancer drug resistance where the Glioma-associated protein 1 (GLI1) elevates UGT1A glucuronidation enzymes, thereby glucuronidating cytarabine and ribavirin, leading to resistance in leukemia patients. Here, we demonstrate that GLI1 imparts resistance to ∼40 compounds, including FDA-approved drugs with disparate chemotypes ( e.g., methotrexate and venetoclax). GLI1 indirectly elevates UGT1As via the chaperone calreticulin, which is required for resistance. Further, we demonstrate that resistant cells are more sensitive to ATP inhibitors, suggesting an Achilles' heel, which could be exploited in the future. In all, we identify GLI1-inducible glucuronidation as a broad-spectrum multidrug resistance pathway.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate / antagonists & inhibitors
  • Antimetabolites, Antineoplastic / chemistry*
  • Antimetabolites, Antineoplastic / metabolism
  • Calreticulin / metabolism
  • Cytarabine / chemistry*
  • Cytarabine / metabolism
  • Drug Resistance, Multiple
  • Drug Resistance, Neoplasm
  • Drug Screening Assays, Antitumor
  • Glucuronosyltransferase / metabolism*
  • Humans
  • Small Molecule Libraries / chemistry*
  • Small Molecule Libraries / metabolism
  • Zinc Finger Protein GLI1 / antagonists & inhibitors*

Substances

  • Antimetabolites, Antineoplastic
  • Calreticulin
  • Small Molecule Libraries
  • Zinc Finger Protein GLI1
  • Cytarabine
  • Adenosine Triphosphate
  • UGT1A1 enzyme
  • Glucuronosyltransferase

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