- Protection strategies for directionally-controlled synthesis of previously inaccessible metal-organic polyhedra (MOPs): The cases of carboxylate: The amino-functionalised Rh(ii)-MOPs
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Herein we report that strategic use of protecting groups in coordination reactions enables directional inhibition that leads to synthesis of highly functionalised metal-organic polyhedra (MOPs), rather than of the extended coordination networks. Using this approach, we functionalised two new porous cuboctahedral Rh(ii)-based MOPs with 24 peripheral carboxylic acid groups or 24 peripheral amino groups.
- Albalad, Jorge,Carné-Sánchez, Arnau,Grancha, Thais,Hernández-López, Laura,Maspoch, Daniel
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- The synthesis and evaluation of multivalent glycopeptoids as inhibitors of the adhesion of candida albicans
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Multivalency is a strategy commonly used by medicinal carbohydrate chemists to increase the affinity of carbohydrate-based small molecules for their protein targets. Although this approach has been very successful in enhancing binding to isolated carbohyd
- Kavanagh, Kevin,Martin, Harlei,Masterson, Hannah,Velasco-Torrijos, Trinidad
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- BIOPROBES FOR LYSYL OXIDASES AND USES THEREOF
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The present invention relates to novel bioprobes which are capable of binding to certain amine oxidase enzymes. These bioprobes are useful in methods of detecting and determining the concentration of certain amine oxidase enzymes in a sample as well as in methods for the quantitative assessment of inhibition of certain amine oxidases.
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Paragraph 00216; 00217
(2021/08/14)
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- Multivalent Presentations of Glycomimetic Inhibitor of the Adhesion of Fungal Pathogen Candida albicans to Human Buccal Epithelial Cells
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Candida albicans causes some of the most prevalent hospital-acquired fungal infections, particularly threatening for immunocompromised patients. C. albicans strongly adheres to the surface of epithelial cells so that subsequent colonization and biofilm fo
- Martin, Harlei,Goyard, David,Margalit, Anatte,Doherty, Kyle,Renaudet, Olivier,Kavanagh, Kevin,Velasco-Torrijos, Trinidad
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p. 971 - 982
(2021/05/31)
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- Facile synthesis and antitumor activity of novel N(9) methylated AHMA analogs
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A facile synthesis of novel antitumor N(9)-methyl-3-(9-acridinylamino)-5- hydroxymethylaniline (AHMA) derivatives is described. Boc protection of aminobenzoic acids followed by LiAlH4 reduction yielded novel methylaminobenzyl alcohol reactants. Their interaction with 9-chloroacridine provides N(9)-methylated AHMA derivatives for biological screening. A preliminary anti-proliferative assay against seven cancer cell lines identified compounds with low μM IC50 values. The Royal Society of Chemistry and the Centre National de la Recherche Scientifique.
- Redko, Boris,Albeck, Amnon,Gellerman, Gary
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p. 2188 - 2191
(2013/01/15)
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- Design and synthesis of bis-biotin-containing reagents for applications utilizing monoclonal antibody-based pretargeting systems with streptavidin mutants
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Previous studies have shown that pretargeting protocols, using cancer-targeting fusion proteins, composed of 4 anti-CD20 single chain Fv (scFv) fragments and streptavidin (scFv4-SAv), followed by a biotinylated dendrimeric N-acetyl-galactosamine blood clearing agent (CA), 1, then a radiolabeled DOTA-biotin derivative (a monobiotin), 3a, can provide effective therapy for lymphoma xenografts in mouse models. A shortcoming in this pretargeting system is that endogenous biotin may affect its efficacy in patients. To circumvent this potential problem, we investigated a pretargeting system that employs anti-CD20 scFv4-SAv mutant fusion proteins with radioiodinated bis-biotin derivatives. With that combination of reagents, good localization of the radiolabel to lymphoma tumor xenografts was obtained in the presence of endogenous biotin. However, the blood clearance reagents employed in the studies were ineffective, resulting in abnormally high levels of radioactivity in other tissues. Thus, in the present investigation a bis-biotin-trigalactose blood clearance reagent, 2, was designed, synthesized, and evaluated in vivo. Additionally, another DOTA-biotin derivative (a bis-biotin), 4a, was designed and synthesized, such that radiometals (e.g., 111In, 90Y, 177Lu) could be used in the pretargeting protocols employing scFv4-SAv mutant fusion proteins. Studies in mice demonstrated that the CA 2 was more effective than CA 1 at removing [125I]scFv4-SAv-S45A mutant fusion proteins from blood. Another in vivo study compared tumor targeting and normal tissue concentrations of the new reagents (2 and [111In]4b) with standard reagents (1 and [111In]3b) used in pretargeting protocols. The study showed that lymphoma xenografts could be targeted in the presence of endogenous biotin when anti-CD20 fusion proteins containing SAv mutants (scFv 4-SAv-S45A or scFv4-SAv-Y43A) were employed in combination with CA 2 and [111In]4b. Importantly, normal tissue concentrations of [111In]4b were similar to those obtained using the standard reagents (1 and [111In]3b), except that the blood and liver concentrations were slightly higher with the new reagents. While the reasons for the higher blood and liver concentrations are unknown, the differences in the galactose structures of the clearance agents 1 and 2 may play a role.
- Wilbur, D. Scott,Park, Steven I.,Chyan, Ming-Kuan,Wan, Feng,Hamlin, Donald K.,Shenoi, Jaideep,Lin, Yukang,Wilbur, Shani M.,Buchegger, Franz,Pantelias, Anastasia,Pagel, John M.,Press, Oliver W.
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scheme or table
p. 1225 - 1238
(2011/04/24)
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- Robust multidentate ligands for diagnosis and anti-viral drugs for influenza and related viruses
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Design and synthesis of a novel library of compounds comprising a spacer with an attachment element on one terminus and a recognition element on the other terminus is presented. The library of compounds can be attached to a solid support and used as an in
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Page/Page column 3; sheet 1
(2008/12/07)
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- Synthesis of soluble multivalent glycoconjugates that target the Hc region of botulinum neurotoxin A
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The design, synthesis, and initial inhibitory studies of di- and tetravalent glycoconjugates that target the heavy chain of botulinum neurotoxin A are reported.
- Kale, Ramesh R.,Clancy, Colin M.,Vermillion, Rebecca M.,Johnson, Eric A.,Iyer, Suri S.
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p. 2459 - 2464
(2008/02/13)
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- Fluorescence resonance energy transfer across a mechanical bond of a rotaxane
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Fluorescence transfer across a donor-acceptor tagged rotaxane was studied and a small conformational change of the rotaxane observed using fluorescent spectroscopy and ROESY NMR. The Royal Society of Chemistry 2005.
- Onagi, Hideki,Rebek Jr., Julius
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p. 4604 - 4606
(2007/10/03)
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- Cyclic hexapeptides with free carboxylate groups as new receptors for monosaccharides
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(Equation presented) Cyclic hexapeptides composed of alternating L-proline and 3-aminobenzoic acid subunits with substituents on the aromatic subunits that contain free carboxylate groups are able to bind monosaccharides in 4% CD3OD/CDCl3
- Bitta, Joachim,Kubik, Stefan
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p. 2637 - 2640
(2007/10/03)
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