Rational design of organic and organometallic thermoresponsive or tumor-selective anticancer drugs and their in vitro and in vivo biological evaluation
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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 ...
CCR7 is implicated in lymph node metastasis of cancer, but its role is obscure. We report a mechanism explaining how interstitial flow caused by lymphatic drainage directs tumor cell migration by autocrine CCR7 signaling. Under static conditions, lymphatic ...
Photodynamic therapy (PDT) can be used to cause vascular collapse and blood flow stasis of the irradiated pathological neovascularisation appearing in several diseases such as age-related macular degeneration (AMD) and cancer. We hypothesized that this PDT ...
Cisplatin is one of the most important and widely used anticancer drug in clinical use. However, its effectiveness is limited by its high toxicity and incidence of drug resistance. This has provided motivation for the search for transition metal-based drug ...
To detect bronchial carcinoma by autofluorescence, we measured in-vivo, in an in-vivo model, and in-vitro the spectra of tumor and normal tissue by a fiber-optic-spectrometer. The main difference between tumor and bronchial tissue is the intensity of the 5 ...
The discovery of the anticancer properties of cisplatin in 1965 heralded the development of metallopharmaceuticals and founded a revolution in cancer therapy. Platinum drugs are believed to induce cytotoxicity by cross-linking DNA, causing changes to the D ...
The 2,2'-methylenebis[furan] (1) was converted to 1-{(4R,6S))-6-[(2R)-2,4-dihydroxybutyl]-2,2-dimethyl-1,3-dioxan-4-yl}-3- [(2R,4R)-tetrahydro-4,6-dihydroxy-2H-pyran-2-yl)propan-2-one ((+)-18) and its (4S)-epimer (-)-19 with high stereo- and enantioselecti ...
The DNA repair protein O6-methylguanine-DNA methyltransferase (MGMT, alkyltransferase) is an important suicide enzyme involved in defense against O6-alkylating endogenous metabolites and environmental carcinogens. It also plays a pivotal role in primary an ...
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 ...