Synthesis of NVS-BPTF-1 and evaluation of its biological activity
2
Zenith Epigenetics Ltd, Suite 300, 4820 Richard Road SW, Calgary, AB T3E 6L1, Canada.
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Publication type: Journal Article
Publication date: 2021-09-01
scimago Q2
wos Q2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
34146702
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
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.
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13
Total citations:
13
Citations from 2024:
8
(61.54%)
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GOST
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Mélin L. et al. Synthesis of NVS-BPTF-1 and evaluation of its biological activity // Bioorganic and Medicinal Chemistry Letters. 2021. Vol. 47. p. 128208.
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Mélin L., Calosing C., Kharenko O. A., Hansen H. S., Gagnon A. Synthesis of NVS-BPTF-1 and evaluation of its biological activity // Bioorganic and Medicinal Chemistry Letters. 2021. Vol. 47. p. 128208.
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TY - JOUR
DO - 10.1016/j.bmcl.2021.128208
UR - https://doi.org/10.1016/j.bmcl.2021.128208
TI - Synthesis of NVS-BPTF-1 and evaluation of its biological activity
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Mélin, Léa
AU - Calosing, Cyrus
AU - Kharenko, Olesya A.
AU - Hansen, Henrik Steen
AU - Gagnon, Alexandre
PY - 2021
DA - 2021/09/01
PB - Elsevier
SP - 128208
VL - 47
PMID - 34146702
SN - 0960-894X
SN - 1464-3405
ER -
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BibTex (up to 50 authors)
Copy
@article{2021_Mélin,
author = {Léa Mélin and Cyrus Calosing and Olesya A. Kharenko and Henrik Steen Hansen and Alexandre Gagnon},
title = {Synthesis of NVS-BPTF-1 and evaluation of its biological activity},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2021},
volume = {47},
publisher = {Elsevier},
month = {sep},
url = {https://doi.org/10.1016/j.bmcl.2021.128208},
pages = {128208},
doi = {10.1016/j.bmcl.2021.128208}
}