ACS Medicinal Chemistry Letters

, том 9 , издание 12 , страницы 1223-1229

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}

William J. Pomerantz ²

Ernst Schönbrunn ^{3, 4}

Gunda I Georg ¹

Jon E Hawkinson ¹

Скрыть аффилиации авторов Показать аффилиации авторов: 4 аффилиации

Department of Medicinal Chemistry and Institute for Therapeutics Discovery & Development, College of Pharmacy, University of Minnesota, 717 Delaware Street SE, Minneapolis, Minnesota 55414, United States |

Department of Chemistry, University of Minnesota, 207 Pleasant Street, SE, Minneapolis, Minnesota 55455, United States |

H. Lee Moffitt Cancer Center & Research Institute, 12902 Magnolia Drive, Tampa, Florida 33612, United States |

⁴

Department of Molecular Medicine, University of South Florida, Tampa, Florida 33612, United States |

Тип публикации: Journal Article

Дата публикации: 2018-10-31

American Chemical Society (ACS)

ACS Medicinal Chemistry Letters

scimago Q1

wos Q2

БС1

SJR: 0.805

CiteScore: 5.8

Impact factor: 4.0

ISSN: 19485875

DOI: 10.1021/acsmedchemlett.8b00380

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PubMed ID: 30613330

Organic Chemistry

Drug Discovery

Biochemistry

Краткое описание

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.

Найдено

1 цитирование

Белоглазкина Елена

д.х.н., проф.

297 публикаций, 3 270 цитирований, 11 рецензий

Индекс Хирша: 29

Московский государственный университет имени М.В. Ломоносова

1 цитирование

Красновская Ольга

53 публикации, 883 цитирования, 10 рецензий

Индекс Хирша: 17

Московский государственный университет имени М.В. Ломоносова

Топ-30

Журналы

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European Journal of Medicinal Chemistry	European Journal of Medicinal Chemistry, 2, 20% European Journal of Medicinal Chemistry 2 публикации, 20%
Journal of Medicinal Chemistry	Journal of Medicinal Chemistry, 2, 20% Journal of Medicinal Chemistry 2 публикации, 20%
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ACS Chemical Biology	ACS Chemical Biology, 1, 10% ACS Chemical Biology 1 публикация, 10%
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Dyes and Pigments	Dyes and Pigments, 1, 10% Dyes and Pigments 1 публикация, 10%
Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy	Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy, 1, 10% Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy 1 публикация, 10%
Russian Chemical Reviews	Russian Chemical Reviews, 1, 10% Russian Chemical Reviews 1 публикация, 10%
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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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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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@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 Скопировать

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.

Издатель

American Chemical Society (ACS)

Журнал

ACS Medicinal Chemistry Letters

scimago Q1

wos Q2

БС1

SJR

0.805

CiteScore

5.8

Impact factor

4.0

ISSN

19485875 (Print, Electronic)