Novel structural-related analogs of PFI-3 (SRAPs) that target the BRG1 catalytic subunit of the SWI/SNF complex increase the activity of temozolomide in glioblastoma cells.

Yali He¹, Chuanhe Yang², Yinan Wang², Joshua R Sacher³, Michelle M Sims², Lawrence M Pfeffer², Duane D Miller⁴

¹Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, TN 38163, United States.

²Department of Pathology and Laboratory Medicine, and Center for Cancer Research, College of Medicine, University of Tennessee Health Science Center, Memphis, TN 38103, United States.

³Cyclica, Inc., 207 Queens Quay West, Suite 420, Toronto, Ontario M5J 1A7, Canada.

⁴Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, TN 38163, United States. Electronic address: dmiller@uthsc.edu.

PubMed DOI

Abstract

Glioblastoma (GBM) is the most aggressive and treatment-refractory malignant adult brain cancer. After standard of care therapy, the overall median survival for GBM is only ∼6 months with a 5-year survival <10%. Although some patients initially respond to the DNA alkylating agent temozolomide (TMZ), unfortunately most patients become resistant to therapy and brain tumors eventually recur. We previ…

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Mentioned Companies

Cyclica
affiliation

MeSH Terms

Animals0Antineoplastic Agents, Alkylating0Azabicyclo Compounds0Cell Death0Cell Proliferation0DNA Helicases0Dose-Response Relationship, Drug0Drug Screening Assays, Antitumor0Female0Glioblastoma0Humans0Mice0Mice, Congenic0Mice, Inbred NOD0Molecular Structure0Neoplasms, Experimental0Nuclear Proteins0Pyridines0Structure-Activity Relationship0Temozolomide0Transcription Factors0

Keywords

BRG1BRG1 bromodomain inhibitorsBromodomainGlioblastoma (GBM)SWI/SNFTemozolomide (TMZ)

Article Info

PMID: 34863065
DOI: 10.1016/j.bmc.2021.116533
Received: October 27, 2021
Accepted: November 23, 2021

How to Cite

He Y et al. Novel structural-related analogs of PFI-3 (SRAPs) that target the BRG1 catalytic subunit of the SWI/SNF complex increase the activity of temozolomide in glioblastoma cells. Bioorg Med Chem2022;53116533. doi:10.1016/j.bmc.2021.116533

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