79640-70-3Relevant articles and documents
PRODRUGS ACTIVATED BY REACTIVE OXYGEN SPECIES FOR USE IN THE TREATMENT OF INFLAMMATORY DISEASES AND CANCER
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Page/Page column 16-17, (2018/03/25)
Prodrugs activated predominantly or exclusively in inflammatory tissue, more particularly prodrugs of methotrexate and derivatives thereof, which are selectively activated by Reactive Oxygen Species (ROS) in inflammatory tissues associated with cancer and inflammatory diseases, as well as method for preparing said prodrugs.
PROTEIN DEGRADATION INDUCING TAG AND USAGE THEREOF
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Paragraph 0163; 0165, (2018/05/03)
Provided are: a protein degradation inducing tag which is a molecule that has affinity with proteases and does not inhibit degradation of a protein by proteases; a protein degradation inducing molecule that is a conjugate of at least one protein degradation inducing tag and at least one protein binding molecule that binds to a protein; and a usage of those.
Methotrexate prodrugs sensitive to reactive oxygen species for the improved treatment of rheumatoid arthritis
Andersen, Nikolaj S.,Peiró Cadahía, Jorge,Previtali, Viola,Bondebjerg, Jon,Hansen, Christian A.,Hansen, Anders E.,Andresen, Thomas L.,Clausen, Mads H.
, p. 738 - 746 (2018/07/29)
Methotrexate (MTX) is the standard of care in the treatment of rheumatoid arthritis (RA), a common autoimmune disease that is characterized by chronic inflammation in the synovial membrane of joints. Unfortunately, MTX suffers from high discontinuation ra
Cell-Surface Receptor-Ligand Interaction Analysis with Homogeneous Time-Resolved FRET and Metabolic Glycan Engineering: Application to Transmembrane and GPI-Anchored Receptors
Stockmann, Henning,Todorovic, Viktor,Richardson, Paul L.,Marin, Violeta,Scott, Victoria,Gerstein, Clare,Lake, Marc,Wang, Leyu,Sadhukhan, Ramkrishna,Vasudevan, Anil
supporting information, p. 16822 - 16829 (2017/11/28)
Ligand-binding assays are the linchpin of drug discovery and medicinal chemistry. Cell-surface receptors and their ligands have traditionally been characterized by radioligand-binding assays, which have low temporal and spatial resolution and entail safety risks. Here, we report a powerful alternative (GlycoFRET), where terbium-labeled fluorescent reporters are irreversibly attached to receptors by metabolic glycan engineering. For the first time, we show time-resolved fluorescence resonance energy transfer between receptor glycans and fluorescently labeled ligands. We describe GlycoFRET for a GPI-anchored receptor, a G-protein-coupled receptor, and a heterodimeric cytokine receptor in living cells with excellent sensitivity and high signal-to-background ratios. In contrast to previously described methods, GlycoFRET does not require genetic engineering or antibodies to label receptors. Given that all cell-surface receptors are glycosylated, we expect that GlycoFRET can be generalized with applications in chemical biology and biotechnology, such as target engagement, receptor pharmacology, and high-throughput screening.
Multifunctional small molecules
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Page/Page column 48, (2016/08/29)
The present invention relates to dendrimer synthesis. Specifically, the present invention relates to dendrimer compositions (e.g., scaffolds) capable of copper-free click conjugation for use in the synthesis of functionalized dendrimers, and methods of us
Design considerations for PAMAM dendrimer therapeutics
Goonewardena, Sascha N.,Kratz, Jeremy D.,Zong, Hong,Desai, Ankur M.,Tang, Shengzhuang,Emery, Sarah,Baker Jr., James R.,Huang, Baohua
supporting information, p. 2872 - 2875 (2013/06/27)
We have previously shown that methotrexate (MTX) conjugated to a cancer-specific poly amido amine (PAMAM) dendrimer has a higher therapeutic index than MTX alone. Unfortunately, these therapeutics have been difficult to advance because of the complicated
The facile synthesis of multifunctional PAMAM dendrimer conjugates through copper-free click chemistry
Huang, Baohua,Kukowska-Latallo, Jolanta F.,Tang, Shengzhuang,Zong, Hong,Johnson, Kali B.,Desai, Ankur,Gordon, Chris L.,Leroueil, Pascale R.,Baker Jr., James R.
body text, p. 3152 - 3156 (2012/06/18)
The facile conjugation of three azido modified functionalities, namely a therapeutic drug (methotrexate), a targeting moiety (folic acid), and an imaging agent (fluorescein) with a G5 PAMAM dendrimer scaffold with cyclooctyne molecules at the surface thro
Copper-free click conjugation of methotrexate to a PAMAM dendrimer platform
Huang, Baohua,Desai, Ankur,Zong, Hong,Tang, Shengzhuang,Leroueil, Pascale,Baker Jr., James R.
supporting information; scheme or table, p. 1411 - 1414 (2011/06/10)
The synthesis of a generation 5 (G5) poly(amidoamine) (PAMAM) dendrimer platform having cyclooctyne ligands that were subsequently be used for a copper-free Huisgen 1,3-dipolar cycloaddition (click reaction) with azido modified methotrexate is described.
Synthesis, cleavage profile, and antitumor efficacy of an albumin-binding prodrug of methotrexate that is cleaved by plasmin and cathepsin B
Warnecke, Andre,Fichtner, Iduna,Sass, Gretel,Kratz, Felix
, p. 389 - 395 (2008/12/21)
Cathepsin B and plasmin are intra- or extracellular proteases that are overexpressed by several solid tumors. In order to exploit both proteases as molecular targets for tumor-specific cleavage of prodrugs, an albumin-binding formulation of methotrexate w
Tight binding ligand approach to oligosaccharide-grafted protein
Totani, Kiichiro,Matsuo, Ichiro,Ito, Yukishige
, p. 2285 - 2289 (2007/10/03)
A novel type of artificial glycoprotein was developed, by using dihydrofolate reductase (DHFR) and methotrexate (MTX) as a protein-ligand pair. Various oligosaccharides linked to MTX were shown to bind tightly with DHFR and afforded oligosaccharide-grafted protein, which could be isolated easily by lectin beads.