Publications 2021-2024



L. Franz T. Rubil, A. Balazs, M. Overtus, K. Kemnitz-Hassanin, C. Govaerts, M.A. Mall, C.P.R. Hackenberger

A Cell-Permeable Nanobody to Restore F508del Cystic Fibrosis Transmembrane Conductance Regulator Activity
Link to the article

A. Kocak, A.K. Homer, A. Feida, F. Telschow, J.L. Gorenflos Lopez, C. Baydaroglu, M. Gradzielski, C.P.R. Hackenberger, U. Alexiev, O. Seitz

Chem.Commun. 2024, accepted, DOI: 10:1039/D4CC00884G
Fluorogenic cell surface glycan labelling with fluorescence molecular rotor dyes and nucleic acid stains
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A. Galasov, E. Kazakova, C.E. Stieger, C.P.R. Hackenberger, O. Seitz

Chem.Sci. 2024, 15, 1297
Rapid building block-economic synthesis of long, multi-O-GalNAcylated MUC5AC tandem repeat peptides
Link to the article


S. Schmitt, P. Machui, I. Mai, S. Herterich, S. Wunder, P. Cyrpys, M. Gerlach, P. Ochtrop, C.P.R. Hackenberger, D. Schumacher, J. Helma, A.M. Vogl, M.-A. Kasper

Mol Cancer Ther 2023, 23(2), 199-211
Design and evaluation of phosphonamidate-linked exatecan constructs for highly loaded, stable, and efficacious Antibody-Drug-Conjugates
Link to the article

J.V.V. Arafiles, J. Franke, L. Franz, J. Gómez-González, K. Kemnitz-Hassanin, C.P.R. Hackenberger

JACS 2023, 145(45), 24535-24548
Cell-Surface-Retained Peptide Additives for the Cytosolic Delivery of Functional Proteins
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J.L. Gorenflos López, G.L. Dornan, N. Boback, M. Neuenschwander, A. Oder, K. Kemnitz-Hassanin, P. Schmieder, E. Specker, H.C. Asikoglu, C. Oberdanner, C. Seyffarth, J.P. von Kries,  D. Lauster, S. Hinderlich, C.P.R. Hackenberger

ChemBioChem 2023, 24(24), e202300555
Small Molecules Targeting Human UDP-GlcNAc 2-Epimerase (selected as VIP paper)
Link to the article

Highlighted in
Editors' Choice: Spotlights EFMC Collection: Advances in Chemical Probing Concepts for Chemical Biology Applications
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Hot Topic: Automated Synthesis
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D.S. Munasinghe, M.-A. Kasper, R. Jasinski, K. Kula, M. Palusiak, M. Celeda, G. Mloston, C.P.R. Hackenberger

Chem. Eur. J. 202329(33), e202300806
(3+2)-Cyclization Reactions of Unsaturated Phosphonites with Aldehydes and Thioketones 
Link to the article

Highlighted in Synfacts 2023, 19(8): 0753
Highlights in Chemical Synthesis
Synthesis of P-Heterocycles from Unsaturated Phosphonites with C(sp2)-Electrophiles
Link to the article

M. Roas, B. Vick, M.-A. Kasper, M. Able, H. Polzer, M. Gerlach, E. Kremmer, J. Hecker, S. Schmitt, A. Stengl, V. Waller, N. Hohmann, M. Festini, A. Ludwig, L. Rohrbacher, T. Herold, M. Subklewe, K.S. Götze, C.P.R. Hackenberger, D. Schumacher, J. Helma-Smets, I. Jeremias, H. Leonhardt, K. Spiekermann

Blood 2023, 141(9), 1023-1035
Targeting FLT3 with a new-generation antibody-drug conjugate in combination with kinase inhibitors for treatment of AML
Link to the article

J.L. Gorenflos López, P. Schmieder, K. Kemnitz-Hassanin, H.C. Asikoglu, A. Celik, C. Stieger, D. Fiedler, S. Hinderlich, C.P.R. Hackenberger

Chemical Science 2023, 14, 3482-3492
Real-Time Monitoring of the Sialic acid Biosynthesis Pathway by NMR
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Highlighted in Chemistry World
NMR reveals sialic acid biosynthesis in real time
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P. Ochtrop, J. Jahzerah, P. Machui, I. Mai, D. Schumacher, J. Helma, M.-A. Kasper, C.P.R. Hackenberger

Chemical Science 2023, 14, 2259-2266
Compact hydrophilic electrophiles enable highly efficacious high DAR ADCs with excellent in vivo PK profile
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V. Hagenhaus, J.L. Gorenflos López, R. Rosenstengel, C. Neu, C.P.R. Hackenberger, A. Celik, K. Weinert, M.-B. Nguyen, K. Bork, R. Horstkorte, A. Gesper

Biomolecules 2023, 13(3), 422
Glycation Interferes with the Activity of the Bi-Functional UDP-N-Acetylglucosamine 2-Epimerase/N-Acetyl-mannosamine Kinase (GNE)
Link to the article


E. Poulou, C.P.R. Hackenberger

IJC 2022, e202200057
Staudinger Ligation and Reactions -From Bioorthogonal Labeling to Next-Generation Biopharmaceuticals
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A. Saha, S. Mandal, J.V.V. Arafiles, J. Gómez-González, C.P.R. Hackenberger, A. Brik

Angew. Chem. Int. Ed. 2022, 61(47), e202207551
Angew. Chem. 2022, 134(47), e202207551
Structure-Uptake Relationship Study of DABCYL Derivatives Linked to Cyclic Cell-Penetrating Peptides for Live-Cell Delivery of Synthetic Proteins
Link to the article

C.E. Stieger, Y. Park, M.A.R. de Geus, D. Kim, C. Huhn, J.S. Slenczka, P. Ochtrop, J.M. Müchler, R. Süssmuth, J. Broichhagen, M.-H. Baik, C.P.R. Hackenberger

Angew. Chem. Int. Ed. 2022, 61(41), e202205348
Angew. Chem. 2022, 134(41), e202205348
DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling
Link to the article

S. Hansen, J.V. Arafiles, P. Ochtrop, C.P.R. Hackenberger

Chem. Commun. 2022, 58, 8388-8391
Modular Solid-Phase Synthesis of Electrophilic Cysteine-Selective Ethynyl-Phosphonamidate Peptides
Link to the article

L. Adam, E. Muller, K. Ludwig, S. Klenk, D. Lauster, S. Liese, A. Herrmann, C.P.R. Hackenberger

Bioconjugate Chem. 2022, 33(7), 1269-1278
Design and Functional Analysis of Heterobifunctional Multivalent Phage Capsid Inhibitors Blocking the Entry of Influenza Virus
Link to the article

C. Sarto, S. Florez-Rueda, M. Arrar, C.P.R. Hackenberger, D. Lauster, S. Di Lella

Biological Chemistry 2022, 403(5-6), 615-624
Atomistic insight into the essential binding event of ACE2-derived peptides to the SARS-CoV-2 spike protein
Link to the article

M.-A. Kasper, L. Lassak, A.M. Vogl, I. Mai, J. Helma, D. Schumacher, C.P.R. Hackenberger

EurJOC  2022, 10, e202101389
Bis-ethynylphosphonamidates as an Modular Conjugation Platform to Generate Multi-Functional Protein- and Antibody-Drug-Conjugates
Link to the article


A.F.L. Schneider, J. Kallen, J. Ottl, P.C. Reid, S. Ripoche, S. Ruetz, T.-M. Stachyra, S. Hintermann, C.E. Dumelin, C.P.R. Hackenberger, A.L. Marzinzik

RSC Chem. Biol. 2021, 2, 1661-1668
Discovery, X-ray structure and CPP-conjugation enabled uptake of p53/MDM2 macrocyclic peptide inhibitors
Link to the article

B. Yan, W. Li, C.P.R. Hackenberger

Org. Biomol. Chem. 2021, 19, 8014-8017
A silyl ether-protected building block for O-GlcNAcylated peptide synthesis to enable one-pot acidic deprotection
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M.N. Stadtmueller, S. Bhatia, P. Kiran, M. Hilsch, L. Adam, B. Parshad, S. Klenk, K. Sellrie, D. Lauster, P. Seeberger, C.P.R. Hackenberger, A. Herrmann, R. Haag, T. Wolff

J. Med. Chem. 2021, 64(17), 12774-12789
Evaluation of Multivalent Sialylated Polyglycerols for Resistance and Broad Antiviral Activity against Influenza Viruses
Link to the article

A.F.L. Schneider, L. Benz, M. Lehmann, C.P.R. Hackenberger

Angew. Chem. Int. Ed. 2021, 60(40), 22075-22080
Cell-Permeable Nanobodies Allow Dual-Color Super-Resolution
Link to the article

Angew. Chem. 2021, 133(40), 22246-22252
Zellpermeable Nanobodys ermöglichen Zwei-Farben-Superauflösungsmikroskopie in lebenden, nicht transfizierten Zellen
Link to the article

C.E. Stieger, L. Franz, F. Körlin, C.P.R. Hackenberger

Angew. Chem. Int. Ed. 2021, 60(28), 15359-15364
Diethynyl Phosphinates for Cysteine-Selective Protein Labeling and Disulfide Rebridging
Link to the article

Angew. Chem. 2021, 133(28), 15487-15492
Diethinylphosphinate für die Cystein-selektive Proteinmarkierung und Disulfid-Verbrückung
Link to the article

Y. Park*, A.L. Baumann*, H. Moon, S. Byrne, M.-A. Kasper, S. Hwang, H. Sun, M.-H. Baik, C.P.R. Hackenberger

Chem. Sci. 2021, 12, 8141-8148
The mechanism behind enhanced reactivity of unsaturated phosphorus(v) electrophiles towards thiols
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A.F.L. Schneider, M. Kithil, M.C. Cardoso, M. Lehmann, C.P.R. Hackenberger

Nature Chemistry 2021, 13, 530-539
Cellular uptake of large biomolecules enabled by cell-surface-reactive cell-penetrating peptide additives
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F.-X. Cantrelle, A. Loyens, X. Trivelli, O. Reimann, C. Despres, N.S. Gandhi, C.P.R. Hackenberger, I. Landrieu, C. Smet-Nocca

Front. Mol. Neurosci. 2021, 14:661368, DOI: 10.3389/fnmol.2021.661368
Phosphorylation and O-GlcNAcylation of the PHF-1 Epitope of Tau Protein Induce Local Conformational Changes of the C-Terminus and Modulate Tau Self-Assembly Into Fibrillar Aggregates
Link to the article

R. Brandt, S. Timm, J.L. Gorenflos López, J.K. Abledu, W.M. Kuebler, C.P.R. Hackenberger, M. Ochs, E. Lopez-Rodriguez

Front. Bioeng. Biotechnol. 2021, 8, Art. 614357, DOI: 10.3389/fbioe.2020.614357
Metabolic Glycoengineering Enables the Ultrastructural Visualization of Sialic Acids in the Glycocalyx of the Alveolar Epithelial Cell Line hAELVi
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J. Schwach, K. Kolobynina, K. Brandstetter, M. Gerlach, P. Ochtrop, J. Helma, C.P.R. Hackenberger. H. Harz, M.C. Cardoso, H. Leonhardt, A. Stengl

ChemBioChem 2021, 22(7), 1205-1209
Site‐Specific Antibody Fragment Conjugates for Reversible Staining in Fluorescence Microscopy
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A. Hauser, E. Poulou, F. Müller, P. Schmieder, C.P.R. Hackenberger

Chem. Eur. J. 2021, 27, 2326-2331
Synthesis and Evaluation of Non-Hydrolyzable Phospho-Lysine Peptide Mimics
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