Polo-like kinase 1 inhibitors in human cancer therapy: development and therapeutic potential
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 …
the regulation of mitosis, DNA replication, autophagy, and the epithelial–mesenchymal …
Small-molecule LRRK2 inhibitors for PD therapy: Current achievements and future perspectives
J Hu, D Zhang, K Tian, C Ren, H Li, C Lin… - European Journal of …, 2023 - Elsevier
Leucine-rich repeat kinase 2 (LRRK2) is a multifunctional protein that orchestrates a diverse
array of cellular processes, including vesicle transport, autophagy, lysosome degradation …
array of cellular processes, including vesicle transport, autophagy, lysosome degradation …
Hydrophobic tag-based protein degradation: Development, opportunity and challenge
Q He, X Zhao, D Wu, S Jia, C Liu, Z Cheng… - European Journal of …, 2023 - Elsevier
Targeted protein degradation (TPD) has emerged as a promising approach for drug
development, particularly for undruggable targets. TPD technology has also been …
development, particularly for undruggable targets. TPD technology has also been …
Inhibitors of the PLK1 polo-box domain: drug design strategies and therapeutic opportunities in cancer
ABSTRACT Introduction Polo Like Kinase 1 (PLK1) is a key regulator of mitosis and its
overexpression is frequently observed in a wide variety of human cancers, while often being …
overexpression is frequently observed in a wide variety of human cancers, while often being …
A MedChem toolbox for cereblon-directed PROTACs
A modular chemistry toolbox was developed for cereblon-directed PROTACs. A variety of
linkers was attached to a CRBN ligand via the 4-amino position of pomalidomide. We used …
linkers was attached to a CRBN ligand via the 4-amino position of pomalidomide. We used …
Hydrophobic tag tethering degrader as a promising paradigm of protein degradation: past, present and future perspectives
S Ha, J Zhu, H Xiang, G Luo - Chinese Chemical Letters, 2023 - Elsevier
Small molecule inhibitors have dominated the pharmaceutical landscape for a long time as
the primary therapeutic paradigm targeting pathogenic proteins. However, their efficacy …
the primary therapeutic paradigm targeting pathogenic proteins. However, their efficacy …
[HTML][HTML] Applications of bacterial degrons and degraders—toward targeted protein degradation in bacteria
MA Izert, MM Klimecka, MW Górna - Frontiers in molecular …, 2021 - frontiersin.org
A repertoire of proteolysis-targeting signals known as degrons is a necessary component of
protein homeostasis in every living cell. In bacteria, degrons can be used in place of …
protein homeostasis in every living cell. In bacteria, degrons can be used in place of …
Structural Basis for Variations in Polo-like Kinase 1 Conformation and Intracellular Stability Induced by ATP-Competitive and Novel Noncompetitive Abbapolin …
D Chapagai, G Merhej, C McInnes… - ACS Chemical …, 2023 - ACS Publications
Polo-like kinase 1 (PLK1) is an essential protein kinase with multiple roles in mitotic
progression. PLK1 consists of a kinase domain (KD) and a phosphopeptide-binding polobox …
progression. PLK1 consists of a kinase domain (KD) and a phosphopeptide-binding polobox …
Triazol: a privileged scaffold for proteolysis targeting chimeras
LW Xia, MY Ba, W Liu, W Cheng, CP Hu… - Future medicinal …, 2019 - Taylor & Francis
Current traditional drugs such as enzyme inhibitors and receptor agonists/antagonists
present inherent limitations due to occupancy-driven pharmacology as the mode of action …
present inherent limitations due to occupancy-driven pharmacology as the mode of action …
Targeted Degradation of DNA/RNA binding proteins via covalent hydrophobic tagging
Y Wang, J Zhang, J Deng, C Wang, L Fang… - CCS …, 2023 - chinesechemsoc.org
Targeted protein degradation (TPD) holds great promise for biological inquiry and
therapeutic development. However, it still remains elusive to destruct DNA/RNA binding …
therapeutic development. However, it still remains elusive to destruct DNA/RNA binding …