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 …

Inhibitors of the PLK1 polo-box domain: drug design strategies and therapeutic opportunities in cancer

JM Stafford, MD Wyatt, C McInnes - Expert Opinion on Drug …, 2023 - Taylor & Francis
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 …

Insights into the Pharmacological Activity of the Imidazo− Pyrazole Scaffold

A Spallarossa, F Rapetti, MG Signorello… - …, 2023 - Wiley Online Library
In previous studies, we synthesized different imidazo− pyrazoles 1 and 2 with interesting
anticancer, anti‐angiogenic and anti‐inflammatory activities. To further extend the structure …

Non-covalent cyclic peptides simultaneously targeting Mpro and NRP1 are highly effective against Omicron BA. 2.75

S Yin, S Mei, Z Li, Z Xu, Y Wu, X Chen, D Liu… - Frontiers in …, 2022 - frontiersin.org
Available vaccine-based immunity may at high risk of being evaded due to substantial
mutations in the variant Omicron. The main protease (Mpro) of SARS-CoV-2 and human …

Disordered linkers in multidomain allosteric proteins: Entropic effect to favor the open state or enhanced local concentration to favor the closed state?

M Li, H Cao, L Lai, Z Liu - Protein Science, 2018 - Wiley Online Library
There are many multidomain allosteric proteins where an allosteric signal at the allosteric
domain modifies the activity of the functional domain. Intrinsically disordered regions …

Discovery of targeted covalent natural products against PLK1 by herb-based screening

H Liang, H Liu, Y Kuang, L Chen, M Ye… - Journal of chemical …, 2020 - ACS Publications
Natural products (NPs) are a rich source of drug discovery, and some of them act by
covalently binding to the targets. Recently, targeted covalent natural product (TCNP) design …

Structure-based pharmacophore design and virtual screening for novel tubulin inhibitors with potential anticancer activity

Y Zhou, B Di, MM Niu - Molecules, 2019 - mdpi.com
Tubulin inhibitors have been considered as potential drugs for cancer therapy. However,
their drug resistance and serious side-effects are the main reasons for clinical treatment …

Identification of acylthiourea derivatives as potent Plk1 PBD inhibitors

T Yun, T Qin, Y Liu, L Lai - European Journal of Medicinal Chemistry, 2016 - Elsevier
Thiourea derivatives have drawn much attention for their latent capacities of biological
activities. In this study, we designed acylthiourea compounds as polo-like kinase 1 (Plk1) …

Modulation of the allosteric communication between the polo-box domain and the catalytic domain in Plk1 by small compounds

M Raab, M Sanhaji, L Pietsch, I Béquignon… - ACS chemical …, 2018 - ACS Publications
The Polo-like kinases (Plks) are an evolutionary conserved family of Ser/Thr protein kinases
that possess, in addition to the classical kinase domain at the N-terminus, a C-terminal polo …

Discovery of inhibitors of Aurora/PLK targets as anticancer agents

B Qi, L Zhong, J He, H Zhang, F Li… - Journal of Medicinal …, 2019 - ACS Publications
Aurora and polo-like kinases control the G2/M phase in cell mitosis, which are both
considered as crucial targets for cancer cell proliferations. Here, naphthalene-based …