Multivalent γ‐PGA‐Exendin‐4 Conjugates to Target Pancreatic β‐Cells
Abstract: Targeting of glucagon‐like peptide 1 receptor (GLP‐1R), expressed on the surface of pancreatic β‐cells, is of great interest for the development of advanced therapies for diabetes and diagnostics for insulinoma. We report the conjugation of exendin‐4 (Ex‐4), an approved drug to treat type 2 diabetes, to poly‐γ‐glutamic acid (γ‐PGA) to obtain more stable and effective GLP‐1R ligands. Exendin‐4 modified at Lysine‐27 with PEG4‐maleimide was conjugated to γ‐PGA functionalized with furan, in different molar ratios, exploiting a chemoselective Diels‐Alder cycloaddition. The γ‐PGA presenting the highest number of conjugated Ex‐4 molecules (average 120 per polymeric chain) showed a double affinity towards GLP‐1R with respect to exendin per se, paving the way to improved therapeutic and diagnostic applications.
- Location
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Deutsche Nationalbibliothek Frankfurt am Main
- Extent
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Online-Ressource
- Language
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Englisch
- Bibliographic citation
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Multivalent γ‐PGA‐Exendin‐4 Conjugates to Target Pancreatic β‐Cells ; day:13 ; month:07 ; year:2022 ; extent:1
ChemBioChem ; (13.07.2022) (gesamt 1)
- Creator
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Rossi, Lorenzo
Kerekes, Krisztina
Kovács‐Kocsi, Judit
Körhegyi, Zoltán
Bodnár, Magdolna
Fazekas, Erika
Prépost, Eszter
Pignatelli, Cataldo
Caneva, Enrico
Nicotra, Francesco
Russo, Laura
- DOI
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10.1002/cbic.202200196
- URN
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urn:nbn:de:101:1-2022071315170113858742
- Rights
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Last update
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15.08.2025, 7:34 AM CEST
Data provider
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Associated
- Rossi, Lorenzo
- Kerekes, Krisztina
- Kovács‐Kocsi, Judit
- Körhegyi, Zoltán
- Bodnár, Magdolna
- Fazekas, Erika
- Prépost, Eszter
- Pignatelli, Cataldo
- Caneva, Enrico
- Nicotra, Francesco
- Russo, Laura
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Platelets promote insulin secretion of pancreatic β-cells
Development of Multivalent Conjugates with a Single Non‐Canonical Amino Acid
Conformational Dynamics of the Multivalent Targets
Stimulus-secretion coupling in pancreatic B-cells in islet transplantation
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Purification of replicating pancreatic β-cells for gene expression studies
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Multivalent Peptide–Nanoparticle Conjugates for Influenza‐Virus Inhibition
TBK1 regulates regeneration of pancreatic β-cells
Multivalent Functionalized Dextran-Antibody Conjugates for Efficient Tumor Cell Killing
Enhanced A3 adenosine receptor selectivity of multivalent nucleoside-dendrimer conjugates
Platelets promote insulin secretion of pancreatic β-cells
Development of Multivalent Conjugates with a Single Non‐Canonical Amino Acid
Conformational Dynamics of the Multivalent Targets
Stimulus-secretion coupling in pancreatic B-cells in islet transplantation
Inhibition of TBK1/IKKε Promotes Regeneration of Pancreatic β-cells
Purification of replicating pancreatic β-cells for gene expression studies
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