Drug discovery targeting bromodomain-containing protein 4

Z Liu, P Wang, H Chen, EA Wold, B Tian… - Journal of medicinal …, 2017 - ACS Publications
BRD4, the most extensively studied member of the BET family, is an epigenetic regulator
that localizes to DNA via binding to acetylated histones and controls the expression of …

Targeting Brd4 for cancer therapy: inhibitors and degraders

Y Duan, Y Guan, W Qin, X Zhai, B Yu, H Liu - Medchemcomm, 2018 - pubs.rsc.org
Bromodomain-containing protein 4 (Brd4) plays an important role in mediating the
expression of genes involved in cancers and non-cancer diseases such as inflammatory …

Discovery of QCA570 as an exceptionally potent and efficacious proteolysis targeting chimera (PROTAC) degrader of the bromodomain and extra-terminal (BET) …

C Qin, Y Hu, B Zhou, E Fernandez-Salas… - Journal of medicinal …, 2018 - ACS Publications
Proteins of the bromodomain and extra-terminal (BET) family are epigenetics “readers” and
promising therapeutic targets for cancer and other human diseases. We describe herein a …

Cobalt-Catalyzed Direct Carbonylative Synthesis of Free (NH)-Benzo[cd]indol-2(1H)-ones from Naphthylamides

J Ying, LY Fu, G Zhong, XF Wu - Organic letters, 2019 - ACS Publications
A cobalt-catalyzed C–H carbonylation of naphthylamides for the synthesis of benzo [cd]
indol-2 (1 H)-one scaffolds has been developed. The reaction employs a traceless directing …

Cyclopiazonic acid type indole alkaloids from Nicotiana tabacum-derived fungus Aspergillus versicolor and their anti-tobacco mosaic virus activities

GY Yang, JM Dai, QL Mi, ZJ Li, XM Li, JD Zhang… - Phytochemistry, 2022 - Elsevier
Indole alkaloids have attracted widespread attention of chemists and biologists. Therefore,
the aim of this study is to screen more bioactivities indole alkaloids from the microorganisms …

The compromise of virtual screening and its impact on drug discovery

O Slater, M Kontoyianni - Expert opinion on drug discovery, 2019 - Taylor & Francis
Introduction: Docking and structure-based virtual screening (VS) have been standard
approaches in structure-based design for over two decades. However, our understanding of …

Discovery of Benzo[cd]indol-2(1H)-ones and Pyrrolo[4,3,2-de]quinolin-2(1H)-ones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for …

F Jiang, Q Hu, Z Zhang, H Li, H Li… - Journal of medicinal …, 2019 - ACS Publications
The bromodomain and extra-terminal domain (BET) family of proteins are readers which
specifically recognize histone-acetylated lysine residues. Each BET bromodomain protein …

Computer-aided drug design in epigenetics

W Lu, R Zhang, H Jiang, H Zhang, C Luo - Frontiers in chemistry, 2018 - frontiersin.org
Epigenetic dysfunction has been widely implicated in several diseases especially cancers
thus highlights the therapeutic potential for chemical interventions in this field. With rapid …

Discovery of Highly Potent and Efficient CBP/p300 Degraders with Strong In Vivo Antitumor Activity

J Hu, H Xu, T Wu, C Zhang, H Shen… - Journal of Medicinal …, 2024 - ACS Publications
The transcriptional coactivator cAMP response element binding protein (CREB)-binding
protein (CBP) and its homologue p300 have emerged as attractive therapeutic targets for …

Structure-Based Discovery and Optimization of Benzo[d]isoxazole Derivatives as Potent and Selective BET Inhibitors for Potential Treatment of Castration-Resistant …

M Zhang, Y Zhang, M Song, X Xue… - Journal of medicinal …, 2018 - ACS Publications
The bromodomain and extra-terminal (BET) family proteins have gained increasing interest
as drug targets for treatment of castration-resistant prostate cancer (CRPC). Here, we …