Our research on hydantoin based TNF-α converting enzyme (TACE) inhibitors has led to an acetylene containing series that demonstrates sub-nanomolar potency (K(i)) as well as excellent activity in human whole blood. These studies led to the discovery of highly potent TACE inhibitors with good DMPK profiles.
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| http://dx.doi.org/10.1016/j.bmcl.2010.10.081 | DOI Listing |
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Discovery of novel TACE inhibitors using graph convolutional network, molecular docking, molecular dynamics simulation, and Biological evaluation.
PLoS One
December 2024
Department of Pharmacology, Kangwon National University School of Medicine, Chuncheon, Republic of Korea.
The increasing utilization of deep learning models in drug repositioning has proven to be highly efficient and effective. In this study, we employed an integrated deep-learning model followed by traditional drug screening approach to screen a library of FDA-approved drugs, aiming to identify novel inhibitors targeting the TNF-α converting enzyme (TACE). TACE, also known as ADAM17, plays a crucial role in the inflammatory response by converting pro-TNF-α to its active soluble form and cleaving other inflammatory mediators, making it a promising target for therapeutic intervention in diseases such as rheumatoid arthritis.
View Article and Find Full Text PDFALBI Grade Analyses of TACE Combined with Anti-Angiogenesis Therapies Plus PD-1 Inhibitors versus Anti-Angiogenesis Therapies Plus PD-1 Inhibitors in Advanced HCC.
J Hepatocell Carcinoma
December 2024
Department of Interventional Radiology, Affiliated Hospital 2 of Nantong University, Nantong, People's Republic of China.
Objective: To evaluate the baseline albumin-bilirubin (ALBI) grade's role in advanced hepatocellular carcinoma (HCC) receiving transarterial chemoembolization (TACE) plus anti-angiogenesis therapies and PD-1 inhibitors (TACE+TP) versus anti-angiogenesis therapies and PD-1 inhibitors (TP).
Methods: This multicenter retrospective study enrolled advanced HCC undergoing TACE+TP or TP from January 2019 to June 2023 at three hospitals in China. The primary outcomes were time to progression of the ALBI grade and change in ALBI score between the initial baseline and the final assessment point available, the secondary outcomes consisted of overall survival (OS) as well as progression-free survival (PFS).
Current Treatment Methods in Hepatocellular Carcinoma.
Cancers (Basel)
December 2024
Department of Oncological Propaedeutics, Medical University of Warsaw, 01-445 Warsaw, Poland.
Hepatocellular carcinoma (HCC) is a prevalent malignant tumour worldwide. Depending on the stage of the tumour and liver function, a variety of treatment options are indicated. Traditional radiotherapy and chemotherapy are ineffective against HCC; however, the U.
View Article and Find Full Text PDFCombinations of lenvatinib and immune checkpoint inhibitors plus transarterial chemoembolization, is it the prime time for unresectable hepatocellular carcinoma?
World J Gastrointest Oncol
December 2024
Center for Personalized Medicine, Hospital Israelita Albert Einstein, Sao Paulo 05651-901, Brazil.
Hepatocellular carcinoma (HCC) is a lethal disease and unfortunately, most patients will be diagnosed with unresectable/advanced stages and the overall prognosis is poor. For patients with initially unresectable HCC (uHCC), transarterial chemoembolization (TACE) was the mainstream treatment. Lately, the incorporation of immune checkpoint inhibitors and antiangiogenics for the treatment of metastatic disease has paved the way for significant improvements in the treatment of initially uHCC.
View Article and Find Full Text PDFHepatocellular carcinoma (HCC) is the most common type of liver cancer and is associated with major risk factors such as hepatitis B virus (HBV), hepatitis C virus (HCV), alcoholic fatty liver disease, and metabolic dysfunction-associated steatotic liver diseases. Despite the recent progress in systemic treatment regimens involving immunotherapies and targeted therapeutics, advanced HCC remains difficult to control. Moreover, with several treatment modalities currently available for HCC such as radiation therapy, transarterial chemoembolization (TACE), checkpoint immunotherapies, and multi-tyrosine kinase inhibitors, it is unclear what combination yields the greatest treatment efficacy and durability.
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