Publications 2021-2024

Publications

2024 2023 2022 2021

2024

136.
A. Celik, F. Schöpf, C.E. Stieger, J. A.M. Morgan, S. Lampe, M. Ruwolt, F. Liu, C.P.R. Hackenberger, D. Roderer, D. Fiedler

Preprint
Nucleoside diphosphate kinase A (NME1) catalyzes its own oligophosphorylation
Link to the article

135.
C. Stieger, S. Schwagerus, G. Dornan, L. Armstrong, K. Kemnitz-Hassanin, M. Nadler-Holly, H. Stephanowitz, F. Liu, V. Haucke, Y. Kulathu, C.P.R. Hackenberger

Preprint
Chemoselective placement of unsaturated phosphorus electrophiles into ubiquitin for proximity-induced protein targeting
Link to the article

Introduction of unsaturated N-alkyl-phosphonamidates as cysteine-selective electrophiles for targeted protein labeling and interaction studies.

134.
L. Franz T. Rubil, A. Balazs, M. Overtus, K. Kemnitz-Hassanin, C. Govaerts, M.A. Mall, C.P.R. Hackenberger

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

Cell-permeable nanobodies target intracellular protein, restoring function in cystic fibrosis cells. Therapeutic potential for next-gen biopharmaceuticals.

133.
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
Link to the article

132.
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

2023

131.
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

Novel exatecan-based linker-payload platform for highly potent ADCs targeting TOP1 inhibitors.

130.
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
Link to the article

Novel hydrophobic CPP-additive enhances intracellular protein delivery. Ideal for drug delivery and genome editing.

129.
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
Link to the article

and

Hot Topic: Automated Synthesis
Link to the article

Identification of high-potency GNE inhibitors for modulating sialic acid biosynthesis.

128.
D.S. Munasinghe, M.-A. Kasper, R. Jasinski, K. Kula, M. Palusiak, M. Celeda, G. Mloston, C.P.R. Hackenberger

Chem. Eur. J. 2023, 29(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

Novel P(V)-containing heterocycles synthesized from ethynyl-phosphonites via (3+2)-cyclization reactions.

127.
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

Novel FLT3-targeting ADC, 20D9-ADC, shows potent antileukemic activity in AML, with potential for combination therapy with FLT3-TKI.

126.
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
Link to the article

Highlighted in Chemistry World
NMR reveals sialic acid biosynthesis in real time
Link to the article

Real-time assay to monitor sialic acid biosynthesis using NMR techniques, revealing key enzymatic steps and potential sugar kinase preferences.

125.
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
Link to the article

Efficient phosphonamidate-based conjugation for high DAR ADCs with improved stability and antitumor activity.

124.
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

2022

123.
E. Poulou, C.P.R. Hackenberger

IJC 2022, e202200057
Staudinger Ligation and Reactions -From Bioorthogonal Labeling to Next-Generation Biopharmaceuticals
Link to the article

Staudinger reactions revolutionize bioconjugation for next-gen biopharmaceuticals.

122.
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

DABCYL-modified cell-penetrating peptides enhance Ub uptake efficiency into cells, enabling studies on Ub signaling.

121.
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

Novel ETP warheads enable selective bioconjugation for labeling proteins and peptides on live cells, creating stable antibody-drug-conjugates and protein-protein connections.

120.
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

Efficient installation of electrophilic cysteine-selective ethynyl-phosphonamidates on peptides during solid phase peptide synthesis.

119.
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

Multivalent virus binders show promise as inhibitors of viral entry into host cells.

118.
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

117.
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

Novel bis-ethynylphosphonamidates enable chemoselective addition of thiol-containing modules for constructing protein-protein conjugates.

2021

116.
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

MDM2 inhibitor identified through mRNA display for potential cancer therapy.

115.
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
Link to the article

Novel building block for O-GlcNAcylated peptides SPPS with acid-labile silyl ether protecting groups. Simplifies synthesis steps and purification.

114.
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

Rationally designed sialylated polyglycerols inhibit a wide spectrum of influenza A virus strains by targeting the receptor binding site of hemagglutinin.

113.
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

Novel cell-permeable nanobodies enable super-resolution imaging of cellular targets in live cells for functional analysis.

112.
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

Diethynyl phosphinates are bisfunctional electrophiles for site-selective modification of proteins. Stable in plasma, suitable for intracellular delivery. Ideal for biological applications.

111.
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
Link to the article

Vinyl- and ethynyl P(V) electrophiles for thiol-selective peptide modifications, with Z-selectivity. Mechanistic insights from DFT calculations.

110.
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
Link to the article

Thiol-reactive arginine-rich peptides enhance cellular uptake of protein-CPP conjugates, simplifying protein and antibody delivery.

TOC Cellular uptake of large biomolecules enabled by cell-surface-reactive cell-penetrating peptide additives

109.
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

108.
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
Link to the article

107.
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
Link to the article

Antibody-oligonucleotide conjugates enable reversible immunofluorescence imaging with sequence-specific binding.

Cover Site‐Specific Antibody Fragment Conjugates for Reversible Staining in Fluorescence Microscopy

106.
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
Link to the article

New pLys mimics were synthesized and compared to natural pLys, showing potential for proteomic studies.

Cover Synthesis and Evaluation of Non-Hydrolyzable Phospho-Lysine Peptide Mimics