117499-16-8Relevant articles and documents
Optimizing saccharide-directed molecular delivery to biological receptors: Design, synthesis, and biological evaluation of glycodendrimer-cyclodextrin conjugates
Benito, Juan M.,Gomez-Garcia, Marta,Ortiz Mellet, Carmen,Baussanne, Isabelle,Defaye, Jacques,Garcia Fernandez, Jose M.
, p. 10355 - 10363 (2004)
Dendritic β-cyclodextrin (βCD) derivatives bearing multivalent mannosyl ligands have been prepared and assessed for their binding efficiency toward the tetrameric plant lectin concanavalin A (Con A) and a mammalian mannose/fucose specific cell surface receptor from macrophages. The synthetic strategy exploits the reactivity between isothiocyanate and amine functionalities for the high-yielding assembly via thioureido links of the various building blocks, including host, spacer, branching, and carbohydrate ligand elements. The methodology has been applied to the preparation of a series of βCD-polymannoside scaffolds differing in the ligand valency and geometry. This series allowed us to explore: (i) The effects of the glycodendritic architecture on the binding efficiency; (ii) the mutual influence between the cyclodextrin core and the glycodendritic moieties on the molecular inclusion and lectin-binding properties; and (iii) the consequence of inclusion complex formation, using the anticancer drug docetaxel (Taxotere) as a target guest, on biological recognition. Our results confirm the high drug solubilization capability of this new type of βCD-dendrimer construct and indicate that subtle changes in the architecture of the conjugate may have important consequences on receptor affinity. Interestingly, the host-guest interaction can be monitored to build up supramolecular dynamic glycoclusters with increased lectin affinity. Alternatively, the information obtained from the structure-lectin-binding avidity-inclusion capability studies has been put forward in the design of very efficient molecular transporters for docetaxel based on glycodendritic CD dimers.
Organocatalysts of oxidative protein folding inspired by protein disulfide isomerase
Lukesh, John C.,Andersen, Kristen A.,Wallin, Kelly K.,Raines, Ronald T.
, p. 8598 - 8602 (2014)
Organocatalysts derived from diethylenetriamine effect the rapid isomerization of non-native protein disulfide bonds to native ones. These catalysts contain a pendant hydrophobic moiety to encourage interaction with the non-native state, and two thiol gro
Selective convergent synthesis of aliphatic polyurethane dendrimers
Feast, W. James,Rannard, Steve P.,Stoddart, Alison
, p. 9704 - 9706 (2003)
An overview is given of the first convergent synthesis of aliphatic polyurethane homodendrimers. The synthesis only uses urethane links and has a repeating structure that is consistent from the surface groups through to the core nitrogen atom. Dendrimer molecules up to the third generation and dendrons up to the fourth generation have been synthesized with masses over 7000 Da.
A ternary sensor system based on pyrene derivative-SDS assemblies-Cu2+ displaying dual responsive signals for fast detection of arginine and lysine in aqueous solution
Cao, Jianhua,Ding, Liping,Zhang, Yuanyuan,Wang, Shihuai,Fang, Yu
, p. 66 - 74 (2016)
A new cationic pyrene derivative-based fluorescent probe (IPy) was designed and synthesized. This cationic fluorophore with two imidazolium groups can be well-dissolved in aqueous solution and exhibits only monomer emission. The anionic surfactant SDS ass
Polyamine-substituted gadolinium chelates: A new class of intracellular contrast agents for magnetic resonance imaging of tumors
Wolf, Markus,Hull, William E.,Mier, Walter,Heiland, Sabine,Bauder-Wüst, Ulrike,Kinscherf, Ralf,Haberkorn, Uwe,Eisenhut, Michael
, p. 139 - 148 (2007)
A new class of intracellular contrast agents (CA) for magnetic resonance imaging has been developed, based on Gd(DTPA) with two positively charged amide-linked substituents. Uptake of Gd(DTPA) into cultured tumor cell lines (B16 mouse melanoma, MH3924A Morris hepatoma) was below the detection limit while CA with the melanin-binding pharmacophore 2-(diethylamino)ethylamine reached intracellular concentrations of ca. 0.03 fmol/cell (ca. 20 μM) for melanoma and 0.02 fmol/cell for hepatoma (24 h at 10 μM CA). With the polyamine substituents bis(2-aminoethyl)amine or spermidine, CA uptake increased up to 3-fold for melanoma (0.083 fmol/cell) and 9-fold for hepatoma (0.18 fmol/cell). Uptake of polyamine-substituted CA was reduced by the polyamine transport inhibitor benzyl viologen. Molar relaxivities for three Gd-DTPA-polyamine complexes were in the range 5.6-6.9 for the free complex in solution and 7.7-23.5 s-1 mM-1 for Morris hepatoma cell pellets. T1-weighted magnetic resonance imaging at 2.35 T of rats with MH3924A tumors showed contrast enhancement in tumor at 1 and 24 h postinjection of polyamine-substituted CA.
Ternary system based on fluorophore-surfactant assemblies-Cu2+ for highly sensitive and selective detection of arginine in aqueous solution
Cao, Jianhua,Ding, Liping,Hu, Wenting,Chen, Xiangli,Chen, Xiao,Fang, Yu
, p. 15364 - 15372 (2015)
A new cationic dansyl derivative-based (DIlSD) fluorescence probe was designed and synthesized. Its combination with anionic surfactant SDS assemblies shows enhanced fluorescence intensity and blue-shifted maximum wavelength. Its fluorescence can be slightly quenched by Cu2+; however, the fluorescence quenching efficiency by Cu2+ is highly increased upon titration of arginine (Arg). As a result, the ternary system containing the cationic fluorophore, anionic surfactant, and Cu2+ functions as a highly sensitive and selective sensor to Arg. The optimized sensor system displays a detection limit of 170 nM, representing the highest sensitivity to Arg in total aqueous solution by a fluorescent sensor. Control experiments reveal that the imidazolium groups in the fluorophore, the anionic surfactant, and Cu2+ all play important roles in the process of sensing Arg. The electrostatic interaction between the cationic fluorophore and anionic surfactants facilitates the binding of imidazolium rings with Cu2+, the surfactant surface-anchored Cu2+ is responsible for further binding of Arg, and the electrostatic interaction between anionic surfactants and positively charged amino acids accounts for the selective responses to Arg.
CONJUGATES OF ANTIBODIES AN IMMUNE CELL ENGAGERS
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Paragraph 0195, (2021/07/24)
The present invention concerns a process for preparing a multispecific antibody construct, comprising conjugating a functionalized antibody Ab(F)x containing x reactive moieties F, wherein x is an integer in the range 1 – 10, and an immune cell
VIA CYCLOADDITION BILATERALLY FUNCTIONALIZED ANTIBODIES
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Page/Page column 59, (2021/07/24)
The present invention provides antibody-payload conjugates having a payload-to-antibody ratio of 1. The antibody-payload conjugate is according to structure (1): formula (1), wherein: - a, b, c and d are each independently 0 or 1; - e is an integer in the
