PLK

Polo-like kinase 4 inhibitor CFI-400945 inhibits carotid arterial neointima formation but increases atherosclerosis

31 views | Jan 31 2024

CFI-400945 demonstrates dual effects by inhibiting neointima formation while accelerating atherosclerosis, attributed to its induction of mitotic arrest, polyploidization, and apoptosis in smooth muscle cells. [Read the Full Post]

Synergistic apoptotic effect of miR-183-5p and Polo-Like kinase 1 inhibitor NMS-P937 in breast cancer cells

19 views | May 31 2023

This research study explores the role of miRNAs in breast cancer and their impact on breast cancer cells' response to PLK1 inhibition, with miR-183-5p targeting the PLK1 gene and enhancing the effectiveness of NMS-P937 in inducing apoptosis. [Read the Full Post]

Differential roles of phosphatidylinositol 3-kinase/akt pathway in retinal ganglion cell survival in rats with or without acute ocular hypertension

52 views | Apr 03 2023

The study demonstrated that the PI3K/akt pathway is involved in mediating RGC survival following IOP elevation but not under normal conditions, suggesting its potential as a therapeutic target for ocular ischemic injuries and glaucoma. [Read the Full Post]

Unusually High Affinity of the PLK Inhibitors RO3280 and GSK461364 to HSA and Its Possible Pharmacokinetic Implications

77 views | Mar 17 2023

The study investigated the binding processes of two Polo-like kinase inhibitors, RO3280 and GSK461364, to the human serum albumin (HSA) protein, finding that RO3280 binds to HSA in the charge state +1 prior to a deprotonation pre-equilibrium and has a higher binding affinity for HSA than GSK461364. [Read the Full Post]

PLK1-ELAVL1/HuR-miR-122 signaling facilitates hepatitis C virus proliferation

83 views | Feb 18 2023

Rigosertib, an anticancer agent under clinical trials, targets PLK1 and modulates ELAVL1/HuR-miR-122 signaling to effectively inhibit the proliferation of wild-type and sofosbuvir resistance-associated HCVs, suggesting it could be useful for treating HCV and HCV-associated diseases. [Read the Full Post]

Another Brick to Confirm the Efficacy of Rigosertib as Anticancer Agent

101 views | Feb 18 2023

Rigosertib, a dual PLK1 and PI3K inhibitor, showed dose- and time-dependent efficacy against 5 human tumor cell lines in vitro, with A549 cells being the most sensitive and U87-MG cells the most resistant, with p53 levels affecting the efficacy, making Rigosertib a potential antineoplastic agent against lung cancer in humans. [Read the Full Post]

Dibutyl phthalate promotes angiogenesis in EA.hy926 cells through estrogen receptor-dependent activation of ERK1/2, PI3K-Akt, and NO signaling pathways

54 views | Sep 15 2022

Dunja Kokai et al. found that DBP exerted a pro-angiogenic effect on human vascular ECs and described the molecular mechanism involving ER- and GPER-dependent activation of ERK1/2, PI3K-Akt, and NO signaling pathways. [Read the Full Post]

Construction of m6A-Related lncRNA Prognostic Signature Model and Immunomodulatory Effect in Glioblastoma Multiforme

106 views | Jul 22 2022

Pan Xie et al. constructed an m6A-associated lncRNA risk model to predict the prognosis of GBM patients and provided new ideas for the treatment of GBM. [Read the Full Post]

Shedding light on the binding mechanism of kinase inhibitors BI-2536, Volasetib and Ro-3280 with their pharmacological target PLK1

71 views | Jul 08 2022

Jesús Fernández-Sainz et al. thought that the higher affinity of the inhibitors to PLK1 compared to ATP was mainly attributed to stronger van der Waals interactions. [Read the Full Post]

PLK inhibitors identified by high content phenotypic screening promote maturation of human PSC-derived cardiomyocytes

75 views | Jul 07 2022

Mengying Feng et al. found that PLK inhibitors could promote maturation of hPSC-CMs through suppressing AKT signaling pathway. [Read the Full Post]