نتایج جستجو برای: dual inhibitors

تعداد نتایج: 340444  

Journal: :Molecular cancer research : MCR 2013
Monica Ceccon Luca Mologni William Bisson Leonardo Scapozza Carlo Gambacorti-Passerini

The dual ALK/MET inhibitor crizotinib was recently approved for the treatment of metastatic and late-stage ALK+ NSCLC, and is currently in clinical trial for other ALK-related diseases. As predicted after other tyrosine kinase inhibitors' clinical experience, the first mutations that confer resistance to crizotinib have been described in patients with non-small cell lung cancer (NSCLC) and in o...

2013
Monica Ceccon Luca Mologni William Bisson Leonardo Scapozza Carlo Gambacorti-Passerini

The dual ALK/MET inhibitor crizotinib was recently approved for the treatment of metastatic and late-stage ALKþ NSCLC, and is currently in clinical trial for other ALK-related diseases. As predicted after other tyrosine kinase inhibitors' clinical experience, the first mutations that confer resistance to crizotinib have been described in patients with non–small cell lung cancer (NSCLC) and in o...

Journal: :Journal of Enzyme Inhibition and Medicinal Chemistry 2021

Nonsteroidal aromatase inhibitors (NSAIs) are well-established drugs for the therapy of breast cancer. However, they display some serious side effects, and their efficacy can be compromised by development chemoresistance. Previously, we have reported different indazole-based carbamates piperidine-sulphonamides as potent inhibitors. Starting from most promising compounds, here synthesised new in...

Journal: :Advanced therapeutics 2023

Abstract The selective inhibition of enzymes that catalyze the conversion arachidonic acid to inflammatory eicosanoids represents a promising approach for cancer therapy. This study, therefore, focuses on incorporation metabolically stable, sterically demanding, and hydrophobic carboranes into existing dual cycloxygenase‐2 (COX‐2)/5‐lipoxygenase (5‐LO) inhibitors are key in biosynthesis eicosan...

Journal: :Drug discoveries & therapeutics 2014
Xiaoyang Li Wenfang Xu

Histone deacetylases (HDACs) have attracted a great deal of interest as anticancer drug targets, and many HDAC inhibitors (HDACIs) have displayed clinical efficacy in treating specific tumors. However, all of these agents have significant toxicity, including fatigue, nausea, vomiting, thrombocytopenia, and neutropenia. Thus, increased effort is being directed toward developing selective HDACIs ...

Journal: :Molecules 2013
Katarina Spilovska Jan Korabecny Jan Kral Anna Horova Kamil Musilek Ondrej Soukup Lucie Drtinova Zuzana Gazova Katarina Siposova Kamil Kuca

A structural series of 7-MEOTA-adamantylamine thioureas was designed, synthesized and evaluated as inhibitors of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE). The compounds were prepared based on the multi-target-directed ligand strategy with different linker lengths (n = 2-8) joining the well-known NMDA antagonist adamantine and the hAChE inhibitor 7-methoxytacrin...

Journal: :Molecular cancer therapeutics 2008
Andreas Vogt Peter R McDonald Aletheia Tamewitz Rachel P Sikorski Peter Wipf John J Skoko John S Lazo

Mitogen-activated protein kinase phosphatase (MKP)-1 is a dual-specificity phosphatase that negatively regulates the activity of mitogen-activated kinases and that is overexpressed in human tumors. Contemporary studies suggest that induction of MKP-1 during chemotherapy may limit the efficacy of clinically used antineoplastic agents. Thus, MKP-1 is a rational target to enhance anticancer drug a...

Journal: :Blood 2015
Matthew D Blunt Matthew J Carter Marta Larrayoz Lindsay D Smith Maria Aguilar-Hernandez Kerry L Cox Thomas Tipton Mark Reynolds Sarah Murphy Elizabeth Lemm Samantha Dias Andrew Duncombe Jonathan C Strefford Peter W M Johnson Francesco Forconi Freda K Stevenson Graham Packham Mark S Cragg Andrew J Steele

Current treatment strategies for chronic lymphocytic leukemia (CLL) involve a combination of conventional chemotherapeutics, monoclonal antibodies, and targeted signaling inhibitors. However, CLL remains largely incurable, with drug resistance and treatment relapse a common occurrence, leading to the search for novel treatments. Mechanistic target of rapamycin (mTOR)-specific inhibitors have be...

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