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Your search keyword '"Dijkgraaf, Ingrid"' showing total 17 results
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17 results on '"Dijkgraaf, Ingrid"'

4. Novel Amphibian Bowman–Birk-Like Inhibitor with Antioxidant and Anticoagulant Effects Ameliorates Pancreatitis Symptoms in Mice

Author

Chai, Jinwei, primary, Wu, Jiena, additional, Li, Jinqiao, additional, Liao, Hang, additional, Lu, Wancheng, additional, Guo, Ruiyin, additional, Shao, Zuoyan, additional, Jmel, Mohamed Amine, additional, Martins, Larissa Almeida, additional, Hackeng, Tilman, additional, Ippel, Hans, additional, Dijkgraaf, Ingrid, additional, Kotsyfakis, Michail, additional, and Xu, Xueqing, additional

Published
2023
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5. Exploring the Chemical Properties and Medicinal Applications of Tetramethylthiocycloheptyne Sulfoximine Used in Strain-Promoted Azide–Alkyne Cycloaddition Reactions

Author

Timmers, Matt, primary, Kipper, Andi, additional, Frey, Raphael, additional, Notermans, Stef, additional, Voievudskyi, Maksym, additional, Wilson, Claire, additional, Hentzen, Nina, additional, Ringle, Michael, additional, Bovino, Clara, additional, Stump, Bernhard, additional, Rijcken, Cristianne J. F., additional, Vermonden, Tina, additional, Dijkgraaf, Ingrid, additional, and Liskamp, Rob, additional

Published
2023
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7. Exploring the Chemical Properties and Medicinal Applications of Tetramethylthiocycloheptyne Sulfoximine Used in Strain-Promoted Azide–Alkyne Cycloaddition Reactions

Author

Timmers, Matt, Kipper, Andi, Frey, Raphael, Notermans, Stef, Voievudskyi, Maksym, Wilson, Claire, Hentzen, Nina, Ringle, Michael, Bovino, Clara, Stump, Bernhard, Rijcken, Cristianne J.F., Vermonden, Tina, Dijkgraaf, Ingrid, Liskamp, Rob, Timmers, Matt, Kipper, Andi, Frey, Raphael, Notermans, Stef, Voievudskyi, Maksym, Wilson, Claire, Hentzen, Nina, Ringle, Michael, Bovino, Clara, Stump, Bernhard, Rijcken, Cristianne J.F., Vermonden, Tina, Dijkgraaf, Ingrid, and Liskamp, Rob

Abstract

The recently developed compound, tetramethylthiocycloheptyne sulfoximine (TMTHSI), has shown to be a promising strained alkyne for strain-promoted azide–alkyne cycloaddition (SPAAC), metal-free click chemistry. This research explores the properties of TMTHSI-based compounds via three aspects: (1) large-scale production, (2) unique stability in acidic conditions and its subsequent use in peptide synthesis, and (3) the functionalization of antibodies. Here, it is shown that (1) scale-up is achieved on a scale of up to 100 g. (2) TMTHSI is remarkably stable against TFA allowing for the site-specific functionalization of peptides on resin. Finally, (3) the functionalization of an antibody with a model payload is very efficient, with antibody conjugation demonstrating more beneficial features such as a high yield and limited hydrophobicity as compared to other alkyne reagent conjugates. These results illustrate the high potential of TMTHSI for diverse bioconjugation applications, with production already being GMP-compatible and a highly efficient conversion resulting in attractive costs of goods.

Published
2023

8. Specific N-terminal attachment of TMTHSI linkers to native peptides and proteins for strain-promoted azide alkyne cycloaddition

Author

Timmers, Matt, Peeters, Wouter, Hauwert, Niels J, Rijcken, Cristianne J F, Vermonden, Tina, Dijkgraaf, Ingrid, Liskamp, Rob M J, Timmers, Matt, Peeters, Wouter, Hauwert, Niels J, Rijcken, Cristianne J F, Vermonden, Tina, Dijkgraaf, Ingrid, and Liskamp, Rob M J

Abstract

The site specific attachment of the reactive TMTHSI-click handle to the N-terminus of peptides and proteins is described. The resulting molecular constructs can be used in strain-promoted azide alkyne cycloaddition (SPAAC) for reaction with azide containing proteins e.g., antibodies, peptides, nanoparticles, fluorescent dyes, chelators for radioactive isotopes and SPR-chips etc.

Published
2023

9. Exploring the Chemical Properties and Medicinal Applications of Tetramethylthiocycloheptyne Sulfoximine Used in Strain-Promoted Azide–Alkyne Cycloaddition Reactions

Author

Afd Pharmaceutics, Sub Drug delivery, Afd Chemical Biology and Drug Discovery, Pharmaceutics, Chemical Biology and Drug Discovery, Timmers, Matt, Kipper, Andi, Frey, Raphael, Notermans, Stef, Voievudskyi, Maksym, Wilson, Claire, Hentzen, Nina, Ringle, Michael, Bovino, Clara, Stump, Bernhard, Rijcken, Cristianne J.F., Vermonden, Tina, Dijkgraaf, Ingrid, Liskamp, Rob, Afd Pharmaceutics, Sub Drug delivery, Afd Chemical Biology and Drug Discovery, Pharmaceutics, Chemical Biology and Drug Discovery, Timmers, Matt, Kipper, Andi, Frey, Raphael, Notermans, Stef, Voievudskyi, Maksym, Wilson, Claire, Hentzen, Nina, Ringle, Michael, Bovino, Clara, Stump, Bernhard, Rijcken, Cristianne J.F., Vermonden, Tina, Dijkgraaf, Ingrid, and Liskamp, Rob

Published
2023

10. Specific N-terminal attachment of TMTHSI linkers to native peptides and proteins for strain-promoted azide alkyne cycloaddition

Author

Afd Pharmaceutics, Sub Drug delivery, Afd Chemical Biology and Drug Discovery, Pharmaceutics, Chemical Biology and Drug Discovery, Timmers, Matt, Peeters, Wouter, Hauwert, Niels J, Rijcken, Cristianne J F, Vermonden, Tina, Dijkgraaf, Ingrid, Liskamp, Rob M J, Afd Pharmaceutics, Sub Drug delivery, Afd Chemical Biology and Drug Discovery, Pharmaceutics, Chemical Biology and Drug Discovery, Timmers, Matt, Peeters, Wouter, Hauwert, Niels J, Rijcken, Cristianne J F, Vermonden, Tina, Dijkgraaf, Ingrid, and Liskamp, Rob M J

Published
2023

14. Molecular Detection of Venous Thrombosis in Mouse Models Using SPECT/CT

Author

Dickhout, Annemiek, primary, Van de Vijver, Pieter, additional, Bitsch, Nicole, additional, van Hoof, Stefan J., additional, Thomassen, Stella L. G. D., additional, Massberg, Steffen, additional, Timmerman, Peter, additional, Verhaegen, Frank, additional, Koenen, Rory R., additional, Dijkgraaf, Ingrid, additional, and Hackeng, Tilman M., additional

Published
2022
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15. Strategies for Site-Specific Radiolabeling of Peptides and Proteins

Author

Dijkgraaf, Ingrid, Agten, Stijn M., Bauwens, Matthias, and Hackeng, Tilman M.

Subjects
Medical
Abstract

Although anatomical imaging modalities (X-ray, computed tomography (CT), magnetic resonance imaging (MRI)) still have a higher spatial resolution (0.1–1 mm) than molecular imaging modalities (single-photon emission computed tomography (SPECT), positron emission tomography (PET), optical imaging (OI)), the advantage of molecular imaging is that it can detect molecular and cellular changes at the onset of a disease before it leads to morphological tissue changes, which can be detected by anatomical imaging. During the last decades, noninvasive diagnostic imaging has encountered a rapid growth due to the development of dedicated imaging equipment for preclinical animal studies. In addition, the introduction of multimodality imaging (PET/CT, SPECT/CT, PET/MRI) which combines high-resolution conventional anatomical imaging with high sensitivity of tracer-based molecular imaging techniques has led to successful accomplishments in this exciting field. In this book chapter, we will focus on chemical synthesis techniques for site-specific incorporation of radionuclide chelators. Subsequently, radiolabeling based on complexation of a radionuclide with a chelator will be discussed, with focus on: diethylenetriaminepentaacetic acid (DTPA), 1,4,7,10-tetraazacyclododecane-tetraacetic acid (DOTA), 1,4,7-triazacyclononane-triacetic acid (NOTA), hexa-histidine (His-tag), and 6-hydrazinonicotinic acid (HYNIC) that allow the production of peptides labeled with 18F, 68Ga, 99mTc, and 111In – the currently most widely used isotopes.

Published
2022

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