Fluorescent PARP Inhibitors Applied To Intracranial Glioblastoma: Accumulation and Persistence In Vivo

  • ACS Med Chem Lett. 2022 May 6;13(6):911-915. doi: 10.1021/acsmedchemlett.1c00712.
Zhe Gao  1 ,  Zhen Yang  2 ,  Zheng Li  2 ,  Kevin Burgess  1
Affiliations
  • 1. Department of Chemistry, Texas A & M University, Box 30012, College Station, Texas 77842, United States.
  • 2. Department of Radiology, Houston Methodist Academic Institute, 6670 Bertner Avenue, Houston, Texas 77030, United States.
PMID: 35707158 DOI: 10.1021/acsmedchemlett.1c00712
Abstract

Rucaparib-containing fluorescent probes (1-3) inhibit PARP1 in cell models. One of these (1) was tested in a murine model and shown to permeate into implanted intracranial glioblastoma tumors and persist there for at least 24 h.