Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction

Inhibitors of the BET family proteins are limited by their potency and oral bio-availability. Here, the authors report a new BET inhibitor, NHWD-870, with improved potency compared to previous BET inhibitors, and show that it suppresses BRD4 and targets tumour associated macrophages.

Bibliographic Details
Main Authors: Mingzhu Yin, Ying Guo, Rui Hu, Wesley L. Cai, Yao Li, Shiyao Pei, Hongyin Sun, Cong Peng, Jiali Li, Rui Ye, Qiaohong Yang, Nenghui Wang, Yongguang Tao, Xiang Chen, Qin Yan
Format: Article
Language:English
Published: Nature Publishing Group 2020-04-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-020-15290-0
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spelling doaj-59a306de0a994d95ae774f48771aeb952021-05-11T08:59:23ZengNature Publishing GroupNature Communications2041-17232020-04-0111111410.1038/s41467-020-15290-0Potent BRD4 inhibitor suppresses cancer cell-macrophage interactionMingzhu Yin0Ying Guo1Rui Hu2Wesley L. Cai3Yao Li4Shiyao Pei5Hongyin Sun6Cong Peng7Jiali Li8Rui Ye9Qiaohong Yang10Nenghui Wang11Yongguang Tao12Xiang Chen13Qin Yan14Department of Dermatology, Hunan Engineering Research Center of Skin Health and Disease, Hunan Key Laboratory of Skin Cancer and Psoriasis, Xiangya Hospital, Central South UniversityDepartment of Dermatology, Hunan Engineering Research Center of Skin Health and Disease, Hunan Key Laboratory of Skin Cancer and Psoriasis, Xiangya Hospital, Central South UniversityDepartment of Dermatology, Hunan Engineering Research Center of Skin Health and Disease, Hunan Key Laboratory of Skin Cancer and Psoriasis, Xiangya Hospital, Central South UniversityDepartment of Pathology, Yale School of MedicineDepartment of Dermatology, Hunan Engineering Research Center of Skin Health and Disease, Hunan Key Laboratory of Skin Cancer and Psoriasis, Xiangya Hospital, Central South UniversityDepartment of Dermatology, Hunan Engineering Research Center of Skin Health and Disease, Hunan Key Laboratory of Skin Cancer and Psoriasis, Xiangya Hospital, Central South UniversityDepartment of Dermatology, Hunan Engineering Research Center of Skin Health and Disease, Hunan Key Laboratory of Skin Cancer and Psoriasis, Xiangya Hospital, Central South UniversityDepartment of Dermatology, Hunan Engineering Research Center of Skin Health and Disease, Hunan Key Laboratory of Skin Cancer and Psoriasis, Xiangya Hospital, Central South UniversityDepartment of Pathology, Yale School of MedicineDepartment of Pathology, Yale School of MedicineSchool of Basic Medical Sciences, Guangzhou University of Chinese MedicineNingbo Wenda Pharma, NinghaiKey Laboratory of Carcinogenesis and Cancer Invasion, Ministry of Education, Xiangya Hospital, Central South UniversityDepartment of Dermatology, Hunan Engineering Research Center of Skin Health and Disease, Hunan Key Laboratory of Skin Cancer and Psoriasis, Xiangya Hospital, Central South UniversityDepartment of Pathology, Yale School of MedicineInhibitors of the BET family proteins are limited by their potency and oral bio-availability. Here, the authors report a new BET inhibitor, NHWD-870, with improved potency compared to previous BET inhibitors, and show that it suppresses BRD4 and targets tumour associated macrophages.https://doi.org/10.1038/s41467-020-15290-0
collection DOAJ
language English
format Article
sources DOAJ
author Mingzhu Yin
Ying Guo
Rui Hu
Wesley L. Cai
Yao Li
Shiyao Pei
Hongyin Sun
Cong Peng
Jiali Li
Rui Ye
Qiaohong Yang
Nenghui Wang
Yongguang Tao
Xiang Chen
Qin Yan
spellingShingle Mingzhu Yin
Ying Guo
Rui Hu
Wesley L. Cai
Yao Li
Shiyao Pei
Hongyin Sun
Cong Peng
Jiali Li
Rui Ye
Qiaohong Yang
Nenghui Wang
Yongguang Tao
Xiang Chen
Qin Yan
Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction
Nature Communications
author_facet Mingzhu Yin
Ying Guo
Rui Hu
Wesley L. Cai
Yao Li
Shiyao Pei
Hongyin Sun
Cong Peng
Jiali Li
Rui Ye
Qiaohong Yang
Nenghui Wang
Yongguang Tao
Xiang Chen
Qin Yan
author_sort Mingzhu Yin
title Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction
title_short Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction
title_full Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction
title_fullStr Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction
title_full_unstemmed Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction
title_sort potent brd4 inhibitor suppresses cancer cell-macrophage interaction
publisher Nature Publishing Group
series Nature Communications
issn 2041-1723
publishDate 2020-04-01
description Inhibitors of the BET family proteins are limited by their potency and oral bio-availability. Here, the authors report a new BET inhibitor, NHWD-870, with improved potency compared to previous BET inhibitors, and show that it suppresses BRD4 and targets tumour associated macrophages.
url https://doi.org/10.1038/s41467-020-15290-0
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