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Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer

43 views | Dec 24 2023

The development of SBP-7455, a dual ULK1/2 inhibitor showing potent activity against TNBC cells and synergistic effects with olaparib, suggests a promising strategy for treating triple-negative breast cancer by targeting autophagy and PARP pathways simultaneously. [Read the Full Post]

Pharmacological inhibition of TBK1/IKKε blunts immunopathology in a murine model of SARS-CoV-2 infection

94 views | Nov 28 2023

In this study, researchers discovered that the small molecule idronoxil inhibits TBK1/IKKε signaling, attenuating hyper-inflammation in SARS-CoV-2-challenged mice and establishing a critical role for TBK1/IKKε signaling in severe COVID-19 pathology. [Read the Full Post]

Mussel-inspired multifunctional surface through promoting osteogenesis and inhibiting osteoclastogenesis to facilitate bone regeneration

50 views | Oct 15 2023

This study developed a multifunctional bone repair scaffold coated with LYN and HA, which exhibited dual effects of promoting osteogenesis and inhibiting osteoclastogenesis, resulting in accelerated bone regeneration in both in vitro and in vivo experiments. [Read the Full Post]

Autophagy regulates transforming growth factor β signaling and receptor trafficking

60 views | Aug 27 2023

Inhibition of autophagy in non-small cell lung cancer cells attenuates pro-tumorigenic TGFβ signaling by impairing receptor trafficking, leading to decreased Smad2/Smad3 phosphorylation and nuclear accumulation. [Read the Full Post]

Evaluation of the Effectiveness of Various Autophagy Inhibitors in A549 Cancer Stem Cells

59 views | Jul 07 2023

Autophinib, among the panel of autophagy inhibitors tested, demonstrated a significant toxic effect on cancer stem cells by downregulating Sox2 expression, inducing apoptosis, and reducing stemness in A549 cells. [Read the Full Post]

Interactive webtool for analyzing drug sensitivity and resistance associated with genetic signatures of cancer cell lines

293 views | Jan 19 2023

Myriam Boeschen et al. found support for the described sensitivity of H1047 mutants to GSK690693 targeting the AKT pathway. [Read the Full Post]

ATM deficiency aggravates the progression of liver fibrosis induced by carbon tetrachloride in mice

84 views | Jan 13 2023

Ming Li et al. found that ATM might be a critical regulator of liver fibrosis progression. [Read the Full Post]

BL-918, a small-molecule activator of ULK1, induces cytoprotective autophagy for amyotrophic lateral sclerosis therapy

36 views | Dec 17 2022

Wei Liu et al. found that ULK1 activator BL-918 displayed a therapeutic potential on ALS through inducing cytoprotective autophagy. [Read the Full Post]

ATM kinase inhibitor AZD0156 in combination with irinotecan and 5-fluorouracil in preclinical models of colorectal cancer

105 views | Oct 31 2022

S Lindsey Davis et al. found that AZD0156 and irinotecan provided a rational and active combination in preclinical colorectal cancer models. [Read the Full Post]

Combined ataxia telangiectasia mutated and DNA-dependent protein kinase inhibition radiosensitizes Madin-Darby canine kidney cells

81 views | Oct 30 2022

Manabu Koike et al. suggested that MDCK cells might be useful in clarifying the cytotoxicity in canine epithelial cells due to radiation and/or radiosensitizers, such as molecule-targeted drugs. [Read the Full Post]