Drug discovery targeting bromodomain-containing protein 4
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 …
that localizes to DNA via binding to acetylated histones and controls the expression of …
Targeting Brd4 for cancer therapy: inhibitors and degraders
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 …
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 …
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 …
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 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 …
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 …
specifically recognize histone-acetylated lysine residues. Each BET bromodomain protein …
Computer-aided drug design in epigenetics
Epigenetic dysfunction has been widely implicated in several diseases especially cancers
thus highlights the therapeutic potential for chemical interventions in this field. With rapid …
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 …
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 …
as drug targets for treatment of castration-resistant prostate cancer (CRPC). Here, we …