7218-43-1Relevant articles and documents
2-Fluoropyridine prosthetic compounds for the 18F labeling of bombesin analogues
Inkster, James,Lin, Kuo-Shyan,Ait-Mohand, Samia,Gosselin, Simon,Bénard, Fran?ois,Guérin, Brigitte,Pourghiasian, Maral,Ruth, Thomas,Schaffer, Paul,Storr, Tim
, p. 3920 - 3926 (2013)
Acetylene-bearing 2-[18F]fluoropyridines [18F]FPy5yne and PEG-[18F]FPyKYNE were prepared via efficient nucleophilic heteroaromatic [18F]fluorination of their corresponding 2-trimethylammoniumpyrdinyl precursors. The prosthetic groups were conjugated to azide- and PEG3-modified bombesin(6-14) analogues via copper-catalyzed azide-alkyne cycloaddition couplings to yield mono- and di-mini-PEGylated ligands for PET imaging of the gastrin- releasing peptide receptor. The PEG3- and PEG2/PEG3-bearing 18F peptides showed decreased lipophilicity relative to an analogous non-mini-PEGylated 18F peptide. Assessment of water-soluble peptide pharmacokinetics and tumour-targeting capabilities in a mouse model of prostate cancer is currently underway.
Synthesis of a library of fucosylated glycoclusters and determination of their binding toward pseudomonas aeruginosa lectin B (PA-IIL) using a DNA-based carbohydrate microarray
Gerland, Béatrice,Goudot, Alice,Pourceau, Gwladys,Meyer, Albert,Dugas, Vincent,Cecioni, Samy,Vidal, Sébastien,Souteyrand, Eliane,Vasseur, Jean-Jacques,Chevolot, Yann,Morvan, Fran?ois
, p. 1534 - 1547 (2012)
Pseudomonas aeruginosa (PA) is a Gram negative opportunistic pathogen and is the major pathogen encounter in the cystic fibrosis (CF) lung airways. It often leads to chronic respiratory infection despite aggressive antibiotic therapy due to the emergence of resistant strains and to the formation of biofilm. The lectin PA-IIL (LecB) is a fucose-specific lectin from PA suspected to be involved in host recognition/adhesion and in biofilm formation. Thus, it can be foreseen as a potential therapeutic target. Herein, 16 fucosylated glycoclusters with antenna-like, linear, or crown-like spatial arrangements were synthesized using a combination of DNA solid-phase synthesis and alkyne azide 1,3-dipolar cycloaddition (CuAAC). Their binding properties toward PA-IIL were then evaluated based on DNA directed immobilization (DDI) carbohydrate microarray. Our results suggested that the antenna-like scaffold was preferred to linear or crown-like glycoclusters. Among the crown-like carbohydrate centered fucosylated glycoclusters, mannose-based core was better than glucose- and galactose-based ones. The influence of the linker arm was also evaluated, and long linkers between fucoses and the core led to a slight better binding than the short ones.
TARGETED BIFUNCTIONAL DEGRADERS
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Page/Page column 189, (2021/04/17)
The present invention provides, in one aspect, bifunctional compounds that can be used to promote or enhance degradation of certain circulating proteins. In another aspect, the present invention provides bifunctional compounds that can be used to promote or enhance degradation of certain autoantibodies. In certain embodiments, treatment or management of a disease and/or disorder requires degradation, removal, or reduction in concentration of the circulating protein or the autoantibody in the subject. Thus, in certain embodiments, administration of a compound of the invention to the subject removes or reduces the circulation concentration of the circulating protein or the autoantibody, thus treating, ameliorating, or preventing the disease and/or disorder. In certain embodiments, the circulating protein is TNF.
DIMERIC IMMUNO-MODULATORY COMPOUNDS AGAINST CEREBLON-BASED MECHANISMS
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Page/Page column 95, (2020/02/06)
Disclosed are small molecules against cereblon to enhance effector T cell function. Methods of making these molecules and methods of using them to treat various disease states are also disclosed.
