Development of MPS1 inhibitors: recent advances and perspectives

Y Zeng, X Ren, P Jin, Y Zhang, M Zhuo… - Journal of Medicinal …, 2023 - ACS Publications
Monopolar spindle kinase 1 (MPS1) plays a pivotal role as a dual-specificity kinase
governing spindle assembly checkpoint activation and sister chromatid separation in …

Pyrimidine-fused dinitrogenous penta-heterocycles as a privileged scaffold for anti-cancer drug discovery

W Li, J Zhang, M Wang, R Dong, X Zhou… - Current Topics in …, 2022 - ingentaconnect.com
Pyrimidine-fused derivatives that are the inextricable part of DNA and RNA play a key role in
the normal life cycle of cells. Pyrimidine-fused dinitrogenous penta-heterocycles, including …

Development of Cdc2-like kinase 2 inhibitors: achievements and future directions

Z Qin, L Qin, X Feng, Z Li, J Bian - Journal of medicinal chemistry, 2021 - ACS Publications
Cdc2-like kinases (CLKs; CLK1–4) are associated with various neurodegenerative
disorders, metabolic regulation, and viral infection and have been recognized as potential …

Identifying Tumorigenesis and Prognosis‐Related Genes of Lung Adenocarcinoma: Based on Weighted Gene Coexpression Network Analysis

M Yi, T Li, S Qin, S Yu, Q Chu, A Li… - BioMed research …, 2020 - Wiley Online Library
Lung adenocarcinoma is the most frequently diagnosed subtype of nonsmall cell lung
cancer. The molecular mechanisms of the initiation and progression of lung …

Pyrido [2, 3-d] pyrimidin-7 (8H)-ones as new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors

M Huang, Y Huang, J Guo, L Yu, Y Chang… - European Journal of …, 2021 - Elsevier
Abstract A series of pyrido [2, 3-d] pyrimidin-7 (8H)-ones were designed and synthesized as
new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors. One of the …

Structure-based design and discovery of pyridyl-bearing fused bicyclic HIV-1 inhibitors: synthesis, biological characterization, and molecular modeling studies

B Huang, T Ginex, FJ Luque, X Jiang… - Journal of Medicinal …, 2021 - ACS Publications
Two series of new pyridyl-bearing fused bicyclic analogues designed to target the dual-
tolerant regions of the non-nucleoside reverse transcriptase inhibitor (NNRTI)-binding …

Upregulation of TTK expression is associated with poor prognosis and immune infiltration in endometrial cancer patients

H Du, L Zhang, J Chen, X Chen, R Qiang, X Ding… - Cancer Cell …, 2024 - Springer
Background Threonine and tyrosine kinase (TTK) is associated with invasion and metastasis
in various tumors. However, the prognostic importance of TTK and its correlation with …

Discovery of a potent and selective covalent threonine tyrosine kinase (TTK) inhibitor

Y Sun, Z Chen, G Liu, X Chen, Z Shi, H Feng, L Yu… - Bioorganic …, 2024 - Elsevier
Threonine tyrosine kinase (TTK) is a critical component of the spindle assembly checkpoint
and plays a pivotal role in mitosis. TTK has been identified as a potential therapeutic target …

Hijacking Monopolar Spindle 1 (MPS1) for Various Cancer Types by Small Molecular Inhibitors: Deep Insights from a Decade of Research and Patents

C Liang, Y Zhou, L Xin, K Kang, L Tian, D Zhang… - European Journal of …, 2024 - Elsevier
Abstract Monopolar spindle 1 (MPS1) has garnered significant attention due to its pivotal
role in regulating the cell cycle. Anomalous expression and hyperactivation of MPS1 have …

Pd-catalyzed Site-selective direct arene CH arylation of Pyrrolo [2, 3-d] pyrimidine derivatives with aryl iodides

M Liu, Z Mao, Y Jiang, Z Zhang, X Zhang - Tetrahedron Letters, 2022 - Elsevier
A simple and efficient methodology was developed for the direct ortho C single bond H
arylation of pyrrolo [2, 3-d] pyrimidine derivatives. Aryl iodides are chosen as an arylating …