Publications 2016-2020

Publications

2020 2019 2018 2017 2016

2020

105.
A. Hauser, S. Hwang, H. Sun, C.P.R. Hackenberger

Chem.Sci. 2020, 11, 12655-12661
Combining free energy calculations with tailored enzyme activity assays to elucidate substrate binding of a phospho-lysine phosphatase
Link to the article

Studying enzymatic activity of LHPP on phosphorylated peptides using experimental and computational methods.
Cover Combining free energy calculations with tailored enzyme activity assays to elucidate substrate binding of a phospho-lysine phosphatase

104.
C.P.R. Hackenberger, P.E. Dawson, Y.X. Chen, H. Hojo

J. Org. Chem. 2020, 85, 1328-1330
Modern Peptide and Protein Chemistry: Reaching New Heights
Link to the article

103.
T. Zhaoxu, I.S. Donskyi, H. Qiao, Z. Zhu, W.E.S. Unger,  C.P.R. Hackenberger, W. Chen, M. Adeli, R. Haag

Adv. Funct. Mater. 2020, 30, 2000933
Graphene Oxide-Cyclic R10 Peptide Nuclear Translocation Nanoplatforms for the Surmounting of Multiple-Drug Resistance
Link to the article

Nanoplatform with cR10 peptide overcomes multidrug resistance in cancer through targeted drug delivery and controlled release.

102.
A.L. Baumann, S. Schwagerus, K. Broi, K. Kemnitz-Hassanin, C.E. Stieger, N. Trieloff, P. Schmieder, C.P.R. Hackenberger

JACS 2020, 142(20), 9544-9552
Chemically Induced Vinylphosphonothiolate Electrophiles for Thiol-Thiol Bioconjugations
Link to the article

highlighted in: Synfacts 2020, 16(07), 0851, DOI: 10.1055/s-0040-1707878
Link to the article

Novel vinylphosphonothiolates used for selective protein labeling and stable protein-protein conjugates.

101.
P. Ochtrop, C.P.R. Hackenberger

Curr. Op. in Chem. Biology 2020, 58, 28-36
Recent advances of thiol-selective bioconjugation reactions (review)
Link to the article

Cys-selective protein modification for research and therapeutics. New reagents for stable conjugation.

100.
D. Lauster, S. Klenk, K. Ludwig, S. Nojoumi, S. Behren, L. Adam, M. Stadtmüller, S. Saenger, S. Franz, K. Hönzke, L. Yao, U. Hoffmann, M. Bardua, A. Hamann, M. Witzenrath, L.E. Sander, T. Wolff, A.C. Hocke, S. Hippenstiel, S. DeCarlo, J. Neudecker, K. Osterrieder, N. Budisa, R.R. Netz, C. Böttcher, S. Liese, A. Herrmann, C.P.R. Hackenberger

Nature Nanotechnology 2020, 15, 373-379
Phage capsid nanoparticles with defined ligand arrangement block influenza virus entry
Link to the article

highlighted in: ChemBioChem 2020, 22(3), 478-480
Link to the article

Multivalent binder inhibits virus adhesion, preventing infection in vitro, ex vivo, and in vivo.

99.
M.-A. Kasper, M. Gerlach, A.F.L. Schneider, C. Groneberg, P. Ochtrop, S. Boldt, D. Schumacher, J. Helma, H. Leonhardt, M. Christmann, C.P.R. Hackenberger

ChemBioChem 2020, 21, 113-119
N-Hydroxysuccinimide-Modified Ethynylphosphonamidates Enable the Synthesis of Configurationally Defined Protein Conjugates
Link to the article

Developing cysteine-selective phosphonamidate building blocks for protein modification, reducing side products and enhancing stability.
Cover N-Hydroxysuccinimide-Modified Ethynylphosphonamidates Enable the Synthesis of Configurationally Defined Protein Conjugates

2019

98.
C. Apel, M.-A. Kasper, C.E. Stieger, C.P.R. Hackenberger, M. Christmann

Org. Lett. 2019, 21(24), 10043-10047
Protein Modification of Lysine with 2-(2-Styrylcyclopropyl)ethanal
Link to the article

highlighted in: Synfacts 2020, 16(04), 0465
Protein Modification by Cope Rearrangement

New lysine-reactive aldehyde for covalent protein modification w/ excellent chemoselectivity & potential for further modifications.

97.
A.L. Baumann, C.P.R. Hackenberger

Curr. Opin. Chem. Biol. 2019, 52, 39-46
Tag and release: strategies for the intracellular cleavage of protein conjugates (Review)
Link to the article

Strategies for introducing cleavable linkages into proteins for targeted intracellular delivery and activation.

96.
M.-A. Kasper, M. Glanz, A. Oder, P. Schmieder, J.P. von Kries, C.P.R. Hackenberger

Chem Sci. 2019, 10, 6322-6329
Vinylphosphonites for Staudinger-induced chemoselective peptide cyclizaton and functionalization

Dedicated to Prof. Ron Raines on the occasion of his 60th birthday
Link to the article

Vinylphosphonites enable chemoselective modification of peptides and proteins, enhancing cellular uptake and protein interactions.

95.
M.-A. Kasper, A. Stengl, P. Ochtrop, M. Gerlach, T. Stoschek, D. Schumacher, J. Helma, M. Penkert, E. Krause, H. Leonhardt, C.P.R. Hackenberger

Angew. Chem. Int. Ed. 2019, 58(34), 11631-11636
Ethynylphosphonamidates for the Rapid and Cysteine-Selective Generation of Efficacious Antibody-Drug Conjugates
Link to the article

Angew. Chem. 2019, 131(34), 11757-11762
Link to the article

Dedicated to Prof. Sam Gellman on the occasion of his 60th birthday

highlighted in: ADC review 2019 (July)
New Reagents for the Rapid Generation of Efficacious Antibody-Drug Conjugates

highlighted in: Synfacts 2019, 15(10), 1189
Ethynylphosphonamidates in the Synthesis of Antibody–Drug Conjugates

New Cys-selective ethynylphosphonamidates are efficient for generating ADCs from non-engineered antibodies, with excellent stability and antitumor activity.

94.
M.-A. Kasper, M. Glanz, A. Stengl, M. Penkert, S. Klenk, T. Sauer, D. Schumacher, J. Helma, E. Krause, C. Cardoso, H. Leonhardt, C.P.R. Hackenberger

Angew. Chem. Int. Ed. 2019, 58(34), 11625-11630
Cysteine-Selective Phosphonamidate Electrophiles for Modular Protein Bioconjugations
Link to the article

Angew. Chem. 2019, 131(34), 11751-11756
Cysteinselektive phosphonamidatbasierte Elektrophile für modulare Biokonjugationen
Link to the article

Dedicated to Prof. Hans-Ulrich Reißig on the occasion of his 70th birthday
 

highlighted in: Synfacts 2019, 15(05), 0561
Ethynylphosphonamidate-Cysteine Bioconjugation

Novel protein modification technique using ethynylphosphonamidates for stable functional conjugates.

93.
M. Penkert, A. Hauser, R. Harmel, D. Fiedler, C.P.R. Hackenberger, E. Krause

J. Am. Soc. Mass Spectrom. 2019, 30(9), 1578-1585
Electron Transfer/Higher Energy Collisional Dissociation of Doubly Charged Peptide Ions: Identificaton of Labile Protein Phosphorylations
Link to the article

92.
S. Nojoumi, Y. Ma, A. Oder, S. Schwagerus, C.P.R. Hackenberger, N. Budisa

Int. J. Mol. Sci. 2019, 20(9), 2299
In-Cell Synthesis of Bioorthogonal Alkene Tag S-Allyl-Homocycteine and Its Coupling with Reprogrammed Translation
Link to the article

91.
A. Stengl, M. Gerlach, M.-A. Kasper, C.P.R. Hackenberger, H. Leonhardt, D. Schumacher, J. Helma

OBC 2019, 17, 4964-4969
TuPPL: Tub-tag mediated C-terminal protein-protein-ligation using complementary click-chemistry handles
Link to the article

Chemoenzymatic strategy for generating fusion proteins using tubulin tyrosine ligase. Ideal for modular protein ligation.

90.
A.F.L. Schneider, A.L.D. Wallabregue, L. Franz, C.P.R. Hackenberger

Bioconjugate Chem. 2019, 30(2), 400-404
Targeted Subcellular Protein Delivery Using Cleavable Cyclic Cell-Penetrating Peptides
Link to the article

cCPPs deliver mCherry protein into cells for precise subcellular localization, demonstrating potential for targeted protein delivery.

2018

89.
A. Baumann, C.P.R. Hackenberger

CHIMIA 2018, 72(11), 802-808
Modern Ligations Methods to Access Natural and Modified Proteins
Link to the article

88.
D. Schumacher, J. Helma, A.F.L. Schneider, H. Leonhardt, C.P.R. Hackenberger

Angew. Chem. Int. Ed. 2018, 57, 2314-2333
Chemical Functionalization Strategies and Intracellular Applications
Link to the article

Angew. Chem. 2018, 130, 2336-2357
Nanobodys: Strategien zur chemischen Funktionalisierung und intrazelluläre Anwendungen
Link to the article

Nanobodys, highly stable and compact antibodies, are used in molecular biology for antigen detection and modulation. Techniques for functionalization include chemoenzymatic approaches and protein ligation. Applications range from advanced imaging to intracellular antigen manipulation.

87.
K.D. Siebertz, C.P.R. Hackenberger

Chem. Comm. 2018, 54, 763-766
Chemoselective triazole-phosphonamidate conjugates suitable for photo-release
Link to the article

Novel method: Azide compounds conjugated for release as amines by UV light.

2017

86.
H.D. Herce, D. Schumacher, A.F.L. Schneider, A.K. Ludwig, F.A. Mann, M. Fillies, M.-A. Kasper, S. Reinke, E. Krause, H. Leonhardt, M.C. Cardoso, C.P.R. Hackenberger

Nature Chemistry 2017, 9, 762-771
Cell-permeable nanobodies for targeted immunolabelling and antigen manipulation in living cells
Link to the article
Link to supplementary movie

highlighted in: Nature Chemistry 2017, 9, 727-728
Cytosolic delivery - Just passing through

highlighted in: c&en 2017, 95(30), 8-9
Drug Delivery -Two new ways to get proteins into cells

highlighted in: ChemBioChem 2017, 18(22), 2196-2198
Dodging Endosomes: Effective Cytosolic Antibody Delivery

Cell-permeable nanobodies enable targeting and manipulation of intracellular antigens, advancing cell biology and medicine.

85.
A. Hauser, M. Penkert, C.P.R. Hackenberger

Acc. Chem. Res. 2017, 50(8), 1883-1893
Chemical Approaches to Investigate Labile Peptide and Protein Phosphorylation
Link to the article

Investigating novel labile phosphorylations using chemical approaches and proteomic analysis. Exciting advancements in understanding PTMs.

84.
D. Schumacher, O. Lemke, J. Helma, L. Gerszonowicz, V. Waller, T. Stoschek, P.M. Durkin, N. Budisa, H. Leonhardt, B.G. Keller, C.P.R. Hackenberger

Chemical Science 2017, 8, 3471-3478
Broad substrate tolerance of tubulin tyrosine ligase enables one-step site-specific enzymatic protein labeling
Link to the article

Tubulin tyrosine ligase has wide substrate flexibility for protein functionalization with unnatural amino acids.

83.
D. Lauster, M. Glanz, M. Bardua, K. Ludwig, M. Hellmund, U. Hoffmann, A. Hamann, C. Böttcher, R. Haag, C.P.R. Hackenberger, A. Herrmann

Angew. Chem. Int. Ed. 2017, 56(21), 5931-5936
Multivalent Peptide-Nanoparticle Conjugates for Influenza-Virus Inhibition
Link to the article

Angew. Chem. 2017, 129(21), 6025-6030
Multivalente Peptid-Nanopartikel-Konjugate zur Hemmung des Influenzavirus
Link to the article

Nanoparticles inhibit influenza virus binding to cells in vitro and in vivo using multivalent peptide-polymer conjugates.

82.
S. Hinderlich, R. Tauber, C.R. Bertozzi , C.P.R. Hackenberger

ChemBioChem 2017, 18(13), 1141-1145
Werner Reutter: A Visionary Pioneer in Molecular Glycobiology
Link to the article

81.
S. Hinderlich, M. Neuenschwander, P.R. Wratil, A. Oder, M. Lisurek, L.D. Nguyen, J.P. von Kries, C.P.R. Hackenberger

ChemBioChem 2017, 18(13), 1279-1285
Small Molecules Targeting Human N-Acetylmannosamine Kinase
Link to the article

Identification of potential MNK inhibitors for downregulation of sialic acid content in glycoconjugates and studying disease development.

80.
A.F.L. Schneider, C.P.R. Hackenberger

Curr. Opin. in Biotechnology 2017, 48, 61-68
Fluorescent labeling in living cells
Link to the article

Expert in live cell protein labelling techniques: recent advances in chemical probes for enhanced visualization of proteins in living cells.

79.
M.P. Exner, T. Kuenzl, T.M.T. To, Z. Ouyang, S. Schwagerus, M.G. Hoesl, C.P.R. Hackenberger, M.C. Lensen, S. Panke, N. Budisa

ChemBioChem 2017, 18, 85-90
Design of S-Allylcysteine in Situ Production and Incorporation Based on a Novel Pyrrolysyl-tRNA Synthetase Variant
Link to the article

2016

78.
J. Bertran-Vicente, M. Penkert, O. Nieto-Garcia, J.-M. Jeckelmann, P. Schmieder, E. Krause, C.P.R. Hackenberger

Nature Comm. 2016, 7, Article number: 12703
Chemoselective synthesis and analysis of naturally occurring phosphorylated cysteine peptides
Link to the article

Chemoselective phosphorylation of Cys residues in peptides enables study of their biological functions using EThcD mass spectrometry.

77.
O. Reimann, C.P.R. Hackenberger

in "Tau Protein - Methods and Protocols", Verlag Humana Press, Caroline Smet-Nocca (ed.) 2017
Tag-Free Semi-Synthesis of the Tau Protein (Book Chapter)
Link to the article

76.
N. Nischan, M.-A. Kasper, T. Mathew, C.P.R. Hackenberger

Org. Biomol. Chem. 2016, 14, 7500-7508
Bis(arylmethyl)-substituted unsymmetrical phosphites for the synthesis of lipidated peptides via Staudinger-phosphite reactions
Link to the article

With this study we introduce new unsymmetrical phosphites to obtain lipidated peptide-conjugates starting from easily accessible azide-modified amino acid or peptide precursors. For this purpose, we investigated which substituents at alkyl phosphites lead to the highest formation of mono-alkylated phosphoramidate peptides. We found that phosphites containing one alkyl-chain and two picolyl or benzyl-substituents delivered alkyl phosphoramidate-conjugates in high yields, which also allowed a chemoselective lipidation of an unprotected azido polypeptide. Finally, monolipidated phosphoramidate peptides obtained by the unsymmetrical Staudinger phosphite reaction led to the formation of micelle-like structures and cellular uptake.

75.
D. Schumacher, C.P.R. Hackenberger, H. Leonhardt, J. Helma

J. Clin. Immunol. 2016, 36, 100-107
Current Status: Site-Specific Antibody Drug Conjugates
Link to the article

74.
S. Schwagerus, O. Reimann, C. Despres, C. Smet-Nocca, C.P.R. Hackenberger

J. Pept. Sci. 2016, 22(5), 327-333
Semi-synthesis of a tag-free O-GlcNAcylated tau protein by sequential chemoselective ligation
Link to the article

First semi-synthesis of Alzheimer-relevant O-GlcNAcylated tau protein demonstrated using chemoselective ligation.

73.
O. Nieto-Garcia, P.R. Wratil, L.D. Nguyen, V. Böhrsch, S. Hinderlich, W. Reutter, C.P.R. Hackenberger

Chem. Sci. 2016, 7, 3928-3933
Inhibition of the key enzyme of sialic acid biosynthesis by C6-Se modified N-acetylmannosamine analogs
Link to the article

C6-analogs of N-acetylmannosamine were tested, revealing a diselenide dimer as a potent GNE/MNK inhibitor, reducing sialylation in Jurkat cells.

72.
E. Hoffmann, K. Streichert, N. Nischan, C. Seitz, T. Brunner, S. Schwagerus, C.P.R. Hackenberger, M. Rubini

Molecular BioSystems 2016, 12, 1750-1755
Stabilization of bacterially expressed erythropoietin by single site-specific introduction of short branched PEG chains at naturally occurring glycosylation sites
Link to the article

Site-specific PEGylation of unglycosylated EPO enhances stability and activity, reducing aggregation and degradation compared to glycosylated EPO.