BET bromodomain inhibitors

MP Schwalm, S Knapp - Current opinion in chemical biology, 2022 - Elsevier
Lysine acetylation creates docking sites for epigenetic reader domains of BET bromodomain
proteins that have emerged as principal regulators of linage specific gene transcription. The …

Polo-like kinase 1 inhibitors in human cancer therapy: development and therapeutic potential

J Zhang, L Zhang, J Wang, L Ouyang… - Journal of medicinal …, 2022 - ACS Publications
Polo-like kinase 1 (PLK1) plays an important role in a variety of cellular functions, including
the regulation of mitosis, DNA replication, autophagy, and the epithelial–mesenchymal …

Molecular hybrids: A five-year survey on structures of multiple targeted hybrids of protein kinase inhibitors for cancer therapy

OM Soltan, ME Shoman, SA Abdel-Aziz… - European Journal of …, 2021 - Elsevier
Protein kinases have grown over the past few years as a crucial target for different cancer
types. With the multifactorial nature of cancer, and the fast development of drug resistance …

Targeting bromodomain and extraterminal proteins for drug discovery: from current progress to technological development

P Tang, J Zhang, J Liu, CM Chiang… - Journal of medicinal …, 2021 - ACS Publications
Bromodomain and extraterminal (BET) proteins bind acetylated lysine residues in histones
and nonhistone proteins via tandem bromodomains and regulate chromatin dynamics …

Bromodomain inhibitors and therapeutic applications

BK Gajjela, MM Zhou - Current opinion in chemical biology, 2023 - Elsevier
The bromodomain acts to recognize acetylated lysine in histones and transcription proteins
and plays a fundamental role in chromatin-based cellular processes including gene …

Non-mitotic functions of polo-like kinases in cancer cells

CA Raab, M Raab, S Becker, K Strebhardt - Biochimica et Biophysica Acta …, 2021 - Elsevier
Inhibitors of mitotic protein kinases are currently being developed as non-neurotoxic
alternatives of microtubule-targeting agents (taxanes, vinca alkaloids) which provide a …

The era of high-quality chemical probes

MP Licciardello, P Workman - RSC Medicinal Chemistry, 2022 - pubs.rsc.org
Small-molecule chemical probes are among the most important tools to study the function of
proteins in cells and organisms. Regrettably, the use of weak and non-selective small …

Dual‐target inhibitors of bromodomain and extra‐terminal proteins in cancer: A review from medicinal chemistry perspectives

L Feng, G Wang, Y Chen, G He, B Liu… - Medicinal research …, 2022 - Wiley Online Library
Abstract Bromodomain‐containing protein 4 (BRD4), as the most studied member of the
bromodomain and extra‐terminal (BET) family, is a chromatin reader protein interpreting …

[HTML][HTML] Design, synthesis, and biological evaluation of quinazolin-4 (3H)-one derivatives co-targeting poly (ADP-ribose) polymerase-1 and bromodomain containing …

X Chang, D Sun, D Shi, G Wang, Y Chen… - … Pharmaceutica Sinica B, 2021 - Elsevier
This study was aimed to design the first dual-target small-molecule inhibitor co-targeting
poly (ADP-ribose) polymerase-1 (PARP1) and bromodomain containing protein 4 (BRD4) …

Dual-target inhibitors of bromodomain-containing protein 4 (BRD4) in cancer therapy: Current situation and future directions

W Jin, H Tan, J Wu, G He, B Liu - Drug discovery today, 2022 - Elsevier
Abstract Bromodomain-containing protein 4 (BRD4) is emerging as a therapeutic target that
acts synergistically with other targets of small-molecule drugs in cancer. Therefore, the …