Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe
Carolyn N Paulson
1
,
XIANGHONG GUAN
1
,
Alex M Ayoub
2
,
Alice Chan
3, 4
,
Rezaul Md Karim
3, 4
,
Ernst Schönbrunn
3, 4
,
Gunda I Georg
1
,
Publication type: Journal Article
Publication date: 2018-10-31
scimago Q1
wos Q2
SJR: 0.805
CiteScore: 5.8
Impact factor: 4.0
ISSN: 19485875
PubMed ID:
30613330
Organic Chemistry
Drug Discovery
Biochemistry
Abstract
Several chemical probes have been developed for use in fluorescence polarization screening assays to aid in drug discovery for the bromodomain and extra-terminal domain (BET) proteins. However, few of those have been characterized in the literature. We have designed, synthesized, and thoroughly characterized a novel fluorescence polarization pan-BET chemical probe suitable for high-throughput screening, structure-activity relationships, and hit-to-lead potency and selectivity assays to identify and characterize BET bromodomain inhibitors.
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Total citations:
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Citations from 2024:
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GOST
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Paulson C. N. et al. Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe // ACS Medicinal Chemistry Letters. 2018. Vol. 9. No. 12. pp. 1223-1229.
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Paulson C. N., GUAN X., Ayoub A. M., Chan A., Karim R. M., Pomerantz W. J., Schönbrunn E., Georg G. I., Hawkinson J. E. Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe // ACS Medicinal Chemistry Letters. 2018. Vol. 9. No. 12. pp. 1223-1229.
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RIS
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TY - JOUR
DO - 10.1021/acsmedchemlett.8b00380
UR - https://doi.org/10.1021/acsmedchemlett.8b00380
TI - Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe
T2 - ACS Medicinal Chemistry Letters
AU - Paulson, Carolyn N
AU - GUAN, XIANGHONG
AU - Ayoub, Alex M
AU - Chan, Alice
AU - Karim, Rezaul Md
AU - Pomerantz, William J.
AU - Schönbrunn, Ernst
AU - Georg, Gunda I
AU - Hawkinson, Jon E
PY - 2018
DA - 2018/10/31
PB - American Chemical Society (ACS)
SP - 1223-1229
IS - 12
VL - 9
PMID - 30613330
SN - 1948-5875
ER -
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BibTex (up to 50 authors)
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@article{2018_Paulson,
author = {Carolyn N Paulson and XIANGHONG GUAN and Alex M Ayoub and Alice Chan and Rezaul Md Karim and William J. Pomerantz and Ernst Schönbrunn and Gunda I Georg and Jon E Hawkinson},
title = {Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe},
journal = {ACS Medicinal Chemistry Letters},
year = {2018},
volume = {9},
publisher = {American Chemical Society (ACS)},
month = {oct},
url = {https://doi.org/10.1021/acsmedchemlett.8b00380},
number = {12},
pages = {1223--1229},
doi = {10.1021/acsmedchemlett.8b00380}
}
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MLA
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Paulson, Carolyn N., et al. “Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe.” ACS Medicinal Chemistry Letters, vol. 9, no. 12, Oct. 2018, pp. 1223-1229. https://doi.org/10.1021/acsmedchemlett.8b00380.