2. Academic Validation
  3. Synthesis of NVS-BPTF-1 and evaluation of its biological activity

Synthesis of NVS-BPTF-1 and evaluation of its biological activity

  • Bioorg Med Chem Lett. 2021 Sep 1:47:128208. doi: 10.1016/j.bmcl.2021.128208.
Léa Mélin 1,  Cyrus Calosing 2,  Olesya A Kharenko 2,  Henrik C Hansen 2,  Alexandre Gagnon 3
Affiliations

Affiliations

  • 1 Département de chimie, Université du Québec à Montréal, C.P. 8888, Succ. Centre-Ville, Montréal, Québec H3C 3P8, Canada.
  • 2 Zenith Epigenetics Ltd, Suite 300, 4820 Richard Road SW, Calgary, AB T3E 6L1, Canada.
  • 3 Département de chimie, Université du Québec à Montréal, C.P. 8888, Succ. Centre-Ville, Montréal, Québec H3C 3P8, Canada. Electronic address: [email protected].
PMID: 34146702 DOI: 10.1016/j.bmcl.2021.128208
Abstract

BPTF (bromodomain and PHD finger containing transcription factor) is a multidomain protein that plays essential roles in transcriptional regulation, T-cell homeostasis and stem cell pluripotency. As part of the chromatin remodeling complex hNURF (nucleosome remodeling factor), BPTF epigenetic reader subunits are particularly important for BPTF cellular function. Here we report the synthesis of NVS-BPTF-1, a previously reported highly potent and selective BPTF-bromodomain inhibitor. Evaluation of the impact of the inhibition of BPTF-bromodomain using NVS-BPTF-1 on selected proteins involved in the antigen processing pathway revealed that exclusively targeting BPTF-bromodomain is insufficient to observe an increase of PSMB8, PSMB9, TAP1 and TAP2 proteins.

Keywords

BPTF; NURF; NVS-BPTF-1; Synthesis.

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