The SAR of a series of potent sulfonamide hydroxamate TACE inhibitors, all bearing a butynyloxy P1' group, was explored. In particular, compound 5j has excellent in vitro potency against isolated TACE enzyme and in cells, good selectivity over MMP-1 and MMP-9, and oral activity in an in vivo model of TNF-alpha production and a collagen-induced arthritis model.
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http://dx.doi.org/10.1016/s0960-894x(03)00514-6 | DOI Listing |
Front Oncol
December 2024
Sichuan Key Laboratory of Medical Imaging, Department of Radiology, The Affiliated Hospital of North Sichuan Medical College, Nanchong, China.
Objectives: This study aimed to evaluate the effectiveness of combining hepatic arterial infusion chemotherapy (HAIC) with lenvatinib and programmed cell death protein 1 (PD-1) inhibitors in the treatment of advanced, unresectable hepatocellular carcinoma (HCC).
Methods: A comprehensive search across multiple databases was conducted to identify relevant studies published up to May 2024. This search focused on clinical trials investigating the combination of HAIC with lenvatinib and PD-1 inhibitors for the treatment of advanced HCC.
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 PDFJ 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).
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 PDFWorld 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.
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