ACS Medicinal Chemistry Letters

, том 8 , издание 8 , страницы 869-874

Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models

Тип публикации: Journal Article

Дата публикации: 2017-08-02

American Chemical Society (ACS)

ACS Medicinal Chemistry Letters

SCImago Q1

WOS Q2

БС1

SJR: 0.697

CiteScore: 5.8

Impact factor: 4

ISSN: 19485875

DOI: 10.1021/acsmedchemlett.7b00220

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PubMed ID: 28835804

Organic Chemistry

Drug Discovery

Biochemistry

Краткое описание

Histone lysine demethylases (KDMs) play a vital role in the regulation of chromatin-related processes. Herein, we describe our discovery of a series of potent KDM4 inhibitors that are both cell permeable and antiproliferative in cancer models. The modulation of histone H3K9me3 and H3K36me3 upon compound treatment was verified by homogeneous time-resolved fluorescence assay and by mass spectroscopy detection. Optimization of the series using structure-based drug design led to compound 6 (QC6352), a potent KDM4 family inhibitor that is efficacious in breast and colon cancer PDX models.

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ГОСТ |

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Chen Y. K. et al. Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models // ACS Medicinal Chemistry Letters. 2017. Vol. 8. No. 8. pp. 869-874.

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Chen Y. K., Bonaldi T., Cuomo A., Del Rosario J. R., Hosfield D. J., Kanouni T., Kao S., Lai C., Lobo N. A., Matuszkiewicz J., McGeehan A., O'Connell S. M., Shi L., Stafford J. A., Stansfield R. K., Veal J. M., Weiss M. S., Yuen N. Y., Wallace M. B. Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models // ACS Medicinal Chemistry Letters. 2017. Vol. 8. No. 8. pp. 869-874.

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TY - JOUR

DO - 10.1021/acsmedchemlett.7b00220

UR - https://doi.org/10.1021/acsmedchemlett.7b00220

TI - Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models

T2 - ACS Medicinal Chemistry Letters

AU - Chen, Young K

AU - Bonaldi, Tiziana

AU - Cuomo, Alessandro

AU - Del Rosario, Joselyn R

AU - Hosfield, David J.

AU - Kanouni, Toufike

AU - Kao, Shih-Chu

AU - Lai, Chon

AU - Lobo, Neethan A

AU - Matuszkiewicz, Jennifer

AU - McGeehan, Andrew

AU - O'Connell, Shawn M.

AU - Shi, Lihong

AU - Stafford, Jeffrey A.

AU - Stansfield, Ryan K

AU - Veal, James M.

AU - Weiss, Michael S.

AU - Yuen, Natalie Y

AU - Wallace, Michael B

PY - 2017

DA - 2017/08/02

PB - American Chemical Society (ACS)

SP - 869-874

IS - 8

VL - 8

PMID - 28835804

SN - 1948-5875

ER -

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@article{2017_Chen,

author = {Young K Chen and Tiziana Bonaldi and Alessandro Cuomo and Joselyn R Del Rosario and David J. Hosfield and Toufike Kanouni and Shih-Chu Kao and Chon Lai and Neethan A Lobo and Jennifer Matuszkiewicz and Andrew McGeehan and Shawn M. O'Connell and Lihong Shi and Jeffrey A. Stafford and Ryan K Stansfield and James M. Veal and Michael S. Weiss and Natalie Y Yuen and Michael B Wallace},

title = {Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models},

journal = {ACS Medicinal Chemistry Letters},

year = {2017},

volume = {8},

publisher = {American Chemical Society (ACS)},

month = {aug},

url = {https://doi.org/10.1021/acsmedchemlett.7b00220},

number = {8},

pages = {869--874},

doi = {10.1021/acsmedchemlett.7b00220}

}

MLA

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Chen, Young K., et al. “Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models.” ACS Medicinal Chemistry Letters, vol. 8, no. 8, Aug. 2017, pp. 869-874. https://doi.org/10.1021/acsmedchemlett.7b00220.

Издатель

American Chemical Society (ACS)

Журнал

ACS Medicinal Chemistry Letters

SCImago Q1

WOS Q2

БС1

SJR

0.697

CiteScore

5.8

Impact factor

ISSN

19485875 (Print, Electronic)

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