Lipophilic Pyridinium Bisphosphonates: Potent γδT Cell Stimulators
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چکیده
منابع مشابه
Lipophilic Pyridinium Bisphosphonates: Potent gd T Cell Stimulators**
Bisphosphonates such as risedronate and ibandronate are widely used to treat a variety of bone resorption diseases, preventing protein prenylation and disrupting osteoclast function. Bisphosphonates also activate human gd T cells (expressing the Vg2Vd2 T cell receptor), and these activated gd T cells kill tumor cells. 3] There has thus been interest in using bisphosphonates in cancer immunother...
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Nitrogen-containing bisphosphonates, drugs used to treat bone resorption diseases, also have activity against a broad range of protists, including blood-stage Plasmodium spp. Here, we show that new-generation "lipophilic" bisphosphonates designed as anticancer agents that block protein prenylation also have potent activity against Plasmodium liver stages, with a high (>100) therapeutic index. T...
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We report the design, synthesis and testing of a series of novel bisphosphonates, pyridinium-1-yl-hydroxy-bisphosphonates, based on the results of comparative molecular similarity indices analysis and pharmacophore modeling studies of farnesyl diphosphate synthase (FPPS) inhibition, human Vgamma2Vdelta2 T cell activation and bone resorption inhibition. The most potent molecules have high activi...
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We report the cloning and sequencing of a gene encoding the farnesyl pyrophosphate synthase of Trypanosoma cruzi. The protein (T. cruzi farnesyl pyrophosphate synthase, TcFPPS) is an attractive target for drug development, since the growth of T. cruzi is inhibited by carbocation transition state/reactive intermediate analogs of its substrates, the nitrogen-containing bisphosphonates currently i...
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BACKGROUND Nickel was recently identified as a potent activator of dendritic cells through ligating with human Toll-like receptor (TLR)-4. OBJECTIVES Here, we studied an extended panel of transition metals neighbouring nickel in the periodic table of elements, for their capacity to activate human monocyte-derived dendritic cells (MoDCs). METHODS The panel included chromium, cobalt, and pall...
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ژورنال
عنوان ژورنال: Angewandte Chemie International Edition
سال: 2010
ISSN: 1433-7851,1521-3773
DOI: 10.1002/anie.200905933