Inhibitors of protein–protein interactions (PPIs): an analysis of scaffold choices and buried surface area

X Ran, JE Gestwicki - Current opinion in chemical biology, 2018 - Elsevier
Protein–protein interactions (PPI) were once considered 'undruggable', but clinical
successes, driven by advanced methods in drug discovery, have challenged that notion …

Small-molecule PROTAC degraders of the Bromodomain and Extra Terminal (BET) proteins—A review

CY Yang, C Qin, L Bai, S Wang - Drug Discovery Today: Technologies, 2019 - Elsevier
The PROteolysis TArgeting C himeric (PROTAC) concept has provided an opportunity for
the discovery and development of a completely new type of therapy involving induction of …

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 …

BET–HDAC dual inhibitors for combinational treatment of breast cancer and concurrent candidiasis

Y Huang, N Liu, Z Pan, Z Li… - Journal of Medicinal …, 2023 - ACS Publications
Breast cancer is susceptible to Candida infections, and candidiasis has an enhancing effect
on the progression and metastasis of tumor. Breast cancer and concurrent candidiasis …

Discovery of 1H-Imidazo[4,5-b]pyridine Derivatives as Potent and Selective BET Inhibitors for the Management of Neuropathic Pain

X Chen, D Cao, C Liu, F Meng, Z Zhang… - Journal of medicinal …, 2023 - ACS Publications
Neuropathic pain (NP) is an intolerable pain syndrome that arises from continuous
inflammation and excitability after nerve injury. Only a few NP therapeutics are currently …

Cell-based relay delivery strategy in biomedical applications

Y Chen, S Pal, Q Hu - Advanced Drug Delivery Reviews, 2023 - Elsevier
The relay delivery strategy is a two-step targeting approach based on two distinct modules in
which the first step with an initiator is to artificially create a target/environment which can be …

Discovery of (R)-4-(8-methoxy-2-methyl-1-(1-phenylethy)-1H-imidazo [4, 5-c] quinnolin-7-yl)-3, 5-dimethylisoxazole as a potent and selective BET inhibitor for …

S Yu, Y Zhang, J Yang, H Xu, S Lan, B Zhao… - European Journal of …, 2024 - Elsevier
The functions of the bromodomain and extra terminal (BET) family of proteins have been
proved to be involved in various diseases, particularly the acute myeloid leukemia (AML). In …

Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins

D Chen, T Lu, Z Yan, W Lu, F Zhou, X Lyu, B Xu… - European Journal of …, 2019 - Elsevier
Recently, selective inhibition of BET BD2 is emerging as a promising strategy for drug
discovery. Despite significant progress in this area, systematic studies of selective BET BD2 …

Design, synthesis and biological evaluation of novel indole derivatives as potential HDAC/BRD4 dual inhibitors and anti-leukemia agents

G Cheng, Z Wang, J Yang, Y Bao, Q Xu, L Zhao… - Bioorganic …, 2019 - Elsevier
HDAC inhibitors and BRD4 inhibitors were considered to be potent anti-cancer agents.
Recent studies have demonstrated that HDAC and BRD4 participate in the regulation of …

Selective degradation of cellular BRD3 and BRD4-L promoted by PROTAC molecules in six cancer cell lines

Z Yan, X Lyu, D Lin, G Wu, Y Gong, X Ren… - European Journal of …, 2023 - Elsevier
Targeted degradation of BET family proteins BRD2/3/4 or only BRD4 with PROTAC
molecules has been a promising strategy for the treatment of human cancer. Meanwhile …