Acidic tumor microenvironment abrogates the efficacy of mTORC1 inhibitors
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Organometallic rutheniumarene compounds bearing a maltol ligand have been shown to be nearly inactive in in vitro anticancer assays, presumably due to the formation of dimeric Ru-II species in aqueous solutions. In an attempt to stabilize such complexes, [ ...
The paper proposes a learning approach to support medical researchers in the context of in-vivo cancer imaging, and specifically in the analysis of Dynamic Contrast-Enhanced MRI (DCE-MRI) data. Tumour heterogeneity is characterized by identifying regions w ...
A targeted drug delivery system that is triggered by changes in pH based on single wall carbon nanotubes (SWCNTs), derivatized with carboxylate groups and coated with a polysaccharide material, can be loaded with the anticancer drug doxorubicin (DOX). The ...
Organometallic half-sandwich complexes based on ruthenium with aminomethyl-substituted 3-hydroxy-2-pyridone ligands exist in aqueous solution as monomeric O,O′-chelate complexes or trimeric metallamacrocycles depending upon the pH. We hypothesized that adm ...
An investigation of the mol. mechanism of the anticancer activity demonstrated by the ruthenium(II)-arene compd. [Ru(η6-p-cymene)Cl2(pta)] (pta is 1,3,5-triaza-7-phosphaadamantane), termed "RAPTA-C", in Ehrlich ascites carcinoma (EAC) bearing mice is descr ...
The protein farnesyltransferase (FTase) is a Zn2+-metalloenzyme that catalyzes the farnesylation reaction, i.e., the transfer of the 15-carbon atom farnesyl group from farnesyl diphosphate (FPP) to a specific cysteine of protein substrates. Oncogenic Ras p ...
Many cancer therapeutic agents elicit resistance that renders them ineffective and often produces cross-resistance to other drugs. One of the most common mechanisms of resistance involves P-glycoprotein (Pgp)-mediated drug efflux. To address this problem, ...
The proto-oncogene KRAS is mutated in a wide array of human cancers, most of which are aggressive and respond poorly to standard therapies. Although the identification of specific oncogenes has led to the development of clinically effective, molecularly ta ...
Enzymes that are involved in the synthesis and processing of oligosaccharides, such as glycosidases, are important catalysts for the specific assembly of oligosaccharide structures on proteins. Design and preparation of selective inhibitors of these enzyme ...
Melanoma is one of the most aggressive cancers, and its incidence is increasing. These tumors derive from the melanocyte lineage and remain incurable after metastasis. Here we report that SONIC HEDGEHOG (SHH)-GLI signaling is active in the matrix of human ...