2025 |
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MA Albers, TN Grossmann*
Chem Lett, DOI: 10.1093/chemle/upaf110
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C Durukan, J Faierson, I van der Wal, J Lizandra Pérez, S Hennig, TN Grossmann*
J Pept Sci, 31, e70024 (2025) – open access (PDF)
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G Schouten, F Paulussen, TN Grossmann, W Bitter, P van Ulsen*
J Mol Biol, 437, 169135 (2025) – open access (PDF)
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2024 |
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M Reissland, O Hartmann, S Tauch, JM Bugter, C Prieto-Garcia, C Schulte, S Loebbert, D Solvie, E Bitman-Lotan, A Narain, AC Jacomin, C Schuelein-Voelk, CT Fuss, N Pahor, C Ade, V Buck, M Potente, V Li, G Beliu, A Wiegering, TN Grossmann, M Eilers, E Wolf, H Maric, M Rosenfeldt, MM Maurice, I Dikic, P Gallant, A Orian, ME Diefenbacher*
Oncogene, 43, 3645–3659 (2024) – open access (PDF)
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| Structure-based design of bicyclic helical peptides that target the oncogene β-catenin A Yeste-Vázquez, FM Paulussen, M Wendt, R Klintrot, C Schulte, K Wallraven, L van Gijzel, B Simeonov, M van der Gaag, A Gerber, HM Maric, S Hennig*, TN Grossmann* Angew Chem Int Ed, 63, e202411749 (2024) – open access (PDF) |
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| Identification of an H-Ras nanocluster disrupting peptide CL Steffen, G Manoharan, K Pavic, A Yeste-Vázquez, M Knuuttila, N Arora, Y Zhou, H Härmä, A Gaigneaux, TN Grossmann, DK Abankwa* Commun Biol, 7, 837 (2024) – open access (PDF) |
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Multivalent CXCR4-targeting nanobody formats differently affect affinity, re‐ ceptor clustering, and antagonism
SM Anbuhl, X Dervillez, S Neubacher, AI Schriek, V Bobkov, SW de Taeye, M Szpakowska, M Siderius, TN Grossmann, A Chevigné, MJ Smit, R Heukers* Biochem Pharmacol, 227, 116457 (2024) – open access (PDF) |
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| From protein structures to functional biomimetics (account) C Durukan, TN Grossmann* Synlett, 36, 119–128 (2025) – open access (PDF) |
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| Binding dynamics of a stapled peptide targeting the transcription factor NF-Y C Durukan, F Arbore, R Klintrot, C Bigiotti, IM Ilie, J Vreede, TN Grossmann*, S Hennig* ChemBioChem, 25, e202400020 (2024) – open access (PDF) |
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2023 |
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| Covalent bicyclization of protein complexes yields durable quaternary structures GH Hutchins, S Kiehstaller, P Poc, AH Lewis, J Oh, R Sadighi, NM Pearce, M Ibrahim, I Drienovska, AM Rijs, S Neubacher*, S Hennig*, TN Grossmann* Chem (Cell press), 10, 615–627 (2024) – open access (PDF) |
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| A modular flow platform for sulfur(VI) fluoride exchange ligation of small molecules, peptides and proteins M Bernús, D Mazzarella, J Stanić, Z Zhai, A Yeste-Vázquez, O Boutureira, AFG Gargano, TN Grossmann, T Noël* Nature Synth, 3, 185–191 (2024) – accessible via ChemRxiv |
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| Environment-responsive peptide dimers bind and stabilize double-stranded RNA NM McLoughlin, MA Albers, E Collado Camps, J Paulus, YA Ran, S Neubacher, S Hennig, R Brock, TN Grossmann* Angew Chem Int Ed, 62, e202308028 (2023) – open access (PDF) |
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| Stabilized native protein complexes conjugated with branched molecules TN Grossmann, S Neubacher, S Hennig, S Kiehstaller, P Poc, J Saya, A Amore, I Drienovska, G Hutchnins, D Hamilton patent appl. WO/2024/177503 (priority: 21.02.2023) |
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| Bicyclic engineered Sortase A performs transpeptidation under denaturing conditions S Kiehstaller, GH Hutchins, A Amore, A Gerber, M Ibrahim, S Hennig, S Neubacher*, TN Grossmann* Bioconj Chem, 34, 1114–1121 (2023) – open access (PDF) |
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| Non-enzymatic protein templates amide bond formation and provides catalytic turnover N Brauckhoff, L Fang, A Haim, TN Grossmann* ChemComm, 59, 5241–5244 (2023) – open access (PDF) |
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2022 |
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| Peptide-based covalent inhibitors of protein-protein interactions (review) FM Paulussen, TN Grossmann* J Pept Sci, 29, e3457 (2023) – open access (PDF) |
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| Covalent proteomimetic inhibitor of the bacterial FtsQB divisome complex FM Paulussen, GK Schouten, C Moertl, J Verheul, I Hoekstra, GM Koningstein, GH Hutchins, A Alkir, RA Luirink, DP Geerke, P van Ulsen, T den Blaauwen, J Luirink*, TN Grossmann* J Am Chem Soc, 144, 15303–15313 (2022) – open access (PDF) |
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| Compounds for RNA stabilisation and delivery TN Grossmann, NM McLoughlin, S Neubacher patent appl. WO/2024/072224 (priority: 29.09.2022) |
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| Targeting the interaction of ß-catenin and TCF/LEF transcription factors to inhibit oncogenic Wnt signaling (review) EMR Koelman, A Yeste-Vázquez, TN Grossmann* Bioorg Med Chem, 70, 116920 (2022) – open access (PDF) |
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| Stapling of peptides potentiates the antibiotic treatment of Acinetobacter baumannii in vivo GK Schouten, FM Paulussen, OP Kuipers, W Bitter, TN Grossmann*, P van Ulsen* Antibiotics, 11, 273 (2022) – open access (PDF) |
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2021 |
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Constrained peptides mimic a viral suppressor of RNA silencing
A Kuepper, NM McLoughlin, S Neubacher, A Yeste-Vázquez, E Collado Camps, C Nithin, S Mukherjee, L Bethge, JM Bujnicki, R Brock, S Heinrichs, TN Grossmann* Nucleic Acids Res, 49, 12622–12633 (2021) – open access |
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| Protein macrocyclization for tertiary structure stabilization (review) A Haim, S Neubacher, TN Grossmann* ChemBioChem, 22, 2672–2679 (2021) – open access (PDF) |
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| Bicyclic β-sheet mimetics that target the transcriptional coactivator β-catenin and inhibit Wnt signaling M Wendt, R Bellavita, A Gerber, NL Efrém, T van Ramshorst, NM Pearce, PRJ Davey, I Everard, M Vazquez‑Chantada, E Chiarparin, P Grieco, S Hennig, TN Grossmann* Angew Chem Int Ed, 60, 13937–13944 (2021) – open access (PDF) – featured on back cover |
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| Synergistic DNA- and protein-based recognition promote an RNA-templated bio-orthogonal reaction NM McLoughlin, A Kuepper, S Neubacher, TN Grossmann* Chem Eur J, 27, 10477–10483 (2021) – open access (PDF) |
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| Inhibitors of the Wnt signaling pathway and uses thereof TN Grossmann, M Wendt, NL Efrem, R Bellavita, T van Ramshorst, A Gerber patent appl. EP 4063380 A1 (priority: 24.03.2021) |
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| First-in-class cyclic Temporin L analogue: Design, synthesis, and antimicrobial assessment R Bellavita, B Casciaro, S Di Maro, D Brancaccio, A Carotenuto, A Falanga, F Cappiello, E Buommino, S Galdiero, E Novellino, TN Grossmann, ML Mangoni, F Merlino*, Paolo Grieco J Med Chem, 64, 11675–11694 (2021) – open access (PDF) |
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2020 |
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| Stapled peptide inhibitors of protein-protein interactions (book chapter) M Wendt, NM McLoughlin, TN Grossmann Inhibitors of Protein-Protein Interactions: Small Molecules, Peptides and Macrocycles (A Tavassoli), Royal Society of Chemistry, London (2020) |
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| A protein tertiary structure mimetic modulator of the Hippo signalling pathway H Adihou, R Gopalakrishnan, T Förster, SM Guéret, R Gasper, S Geschwindner, C Carrillo García, H Karatas, AV Pobbati, M Vazquez‑Chantada, P Davey, CM Wassvik, JKS Pang, BS Soh, W Hong, E Chiarparin, D Schade, AT Plowright, E Valeur, M Lemurell, TN Grossmann*, H Waldmann* Nature Commun, 11, 5425 (2020) – open access (PDF) |
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| Proteomimetics as protein-inspired scaffolds with defined tertiary folding patterns (perspective) WS Horne*, TN Grossmann* Nature Chem, 12, 331–337 (2020) (PDF) |
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| Acetylene containing cyclo(L-Tyr-L-Tyr)-analogs as mechanism-based inhibitors of CYP121A1 from Mycobacterium tuberculosis S Ortega Ugalde, K Wallraven, A Speer, W Bitter, TN Grossmann*, JNM Commandeur* Biomed Pharmacol, 177, 113938 (2020) – open access (PDF) |
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| Macrocyclic modalities combining peptide epitopes and natural product fragments SM Guéret*, S Thavam, RJ Carbajo, M Potowski, N Larsson, G Dahl, A Dellsen, TN Grossmann, AT Plowright, E Valeur, M Lemurell, H Waldmann* J Am Chem Soc, 142, 4904–4915 (2020) – open access (PDF) |
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| Adapting free energy perturbation simulations for large macrocyclic ligands: How to dissect contributions from direct binding and free ligand flexibility K Wallraven, FL Holmelin, A Glas, S Hennig, AI Frolov*, TN Grossmann* Chem Sci, 11, 2269–2276 (2020) – open access (PDF) |
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2019 |
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| In situ cyclization of proteins (INCYPRO): Cross-link derivatization modulates protein stability S Neubacher*, J Saya, A Amore, TN Grossmann* J Org Chem, 85, 1476–1483 (2020) – open access (PDF) – featured on supplementary cover |
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| Constrained peptides with fine-tuned flexibility inhibit NF-Y transcription factor assembly S Jeganathan, M Wendt, S Kiehstaller, D Brancaccio, A Kuepper, N Pospiech, A Carotenuto, E Novellino, S Hennig*, TN Grossmann* Angew Chem Int Ed, 58, 17351–17358 (2019) – open access (PDF) |
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| Lipidated stapled peptides targeting the acyl binding protein UNC119 PM Cromm, H Adihou, S Kapoor, M Vazquez‑Chantada, P Davey, D Longmire, E Hennes, W Hofer, P Küchler, E Chiarparin, H Waldmann*, TN Grossmann* ChemBioChem, 20, 2987–2990 (2019) – open access (PDF) – highlighted as cover feature |
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| Organisch-chemisch stabilisierte Enzyme für eine nachhaltige Wirtschaft S Neubacher, S Hennig, TN Grossmann* BIOspektrum, 25, 338–339 (2019) – open access (PDF) |
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2018 |
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| Coiled-coil peptide beacon: A tuneable conformational switch for protein detection C Mueller, TN Grossmann* Angew Chem Int Ed, 57, 17079–17083 (2018) – open access (PDF) – featured on inside cover |
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| Protein-RNA interactions: Structural characteristics and hotspot amino acids DM Krüger, S Neubacher, TN Grossmann* RNA, 24, 1157–1165 (2018) – open access (PDF) |
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| Linking Cytochrome P450 enzymes from Mycobacterium tuberculosis to their cognate ferredoxin partners S Ortega Ugalde, CP de Koning, K Wallraven, B Bruyneel, NPE Vermeulen, TN Grossmann, W Bitter, JNM Commandeur, JC Vos* Appl Microbiol Biotechnol, 102, 9231–9242 (2018) |
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| Structural analysis of the interaction between the bacterial cell division proteins FtsQ and FtsB D Kureisaite-Ciziene, A Varadajan, SH McLaughlin, M Glas, AM Sliva, R Luirink, C Mueller, T den Blaauwen, TN Grossmann, J Luirink*, J Löwe* mBio, 9, e01346–18 (2018) |
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| In situ cyclization of native proteins: Structure-based design of a bicyclic enzyme M Pelay‑Gimeno, T Bange, S Hennig, TN Grossmann* Angew Chem Int Ed, 57, 11164–11170 (2018) – open access (PDF) |
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| Protein macrocyclization TN Grossmann, M Pelay-Gimeno, S Hennig, S Neubacher patent appl. WO 2019203645 A1 (priority: 19.04.2018) |
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2017
Oligonucleotides with cationic backbone and their hybridization with DNA: Interplay of base pairing and electrostatic attraction
B Schmidtgall, A Kuepper, M Meng, TN Grossmann*, C Ducho*
Chem Eur J, 24, 1544–1553 (2018) – open access (PDF)
Targeting β-catenin dependent Wnt signaling via peptidomimetic inhibitors in murine chondrocytes and OA cartilage
A Held, A Glas, L Dietrich, M Bollmann, K Brandstädter, TN Grossmann, CH Lohmann, T Pap, J Bertrand*
Osteoarthritis and Cartilage, 26, 818–823 (2018)
The therapeutic potential of PTEN modulation: Targeting strategies from gene to protein (perspective)
NM McLoughlin, C Mueller, TN Grossmann*
Cell Chem Biol, 25, 19–29 (2018)
Structure-based design of non-natural macrocyclic peptides that inhibit protein-protein interactions
DM Krüger, A Glas, D Bier, N Pospiech, K Wallraven, L Dietrich, C Ottmann, O Koch*, S Hennig*, TN Grossmann*
J Med Chem, 60, 8982–8988 (2017) – open access (PDF)
Increased conformational flexibility of a macrocycle-receptor complex contributes to reduced dissociation rates
A Glas, EC Wamhoff, DM Krüger, C Rademacher,* TN Grossmann*
Chem Eur J, 23, 16157–16161 (2017) – open access (PDF) – featured on inside cover
Cell permeable stapled peptide inhibitor of Wnt signaling that targets β-catenin protein-protein interactions
L Dietrich, B Rathmer, K Ewan, T Bange, S Heinrichs, TC Dale, D Schade, TN Grossmann*
Cell Chem Biol, 24, 958–968 (2017)
Plant cysteine oxidases are dioxygenases that directly enable arginyl transferase-catalyzed arginylation of N-end rule targets
MD White, M Klecker, R Hopkinson, D Weits, C Mueller, C Naumann, R O’Neill, J Wickens, J Yang, JC Brooks‑Bartlett, EF Garman, TN Grossmann, N Dissmeyer*, E Flashman*
Nature Commun, 8, 14690 (2017) – open access (PDF)
New modalities for challanging targets in drug discovery (review)
E Valeur*, SM Gueret, H Adihou, R Gopalakrishnan, M Lemurell, H Waldmann, TN Grossmann, AT Plowright
Angew Chem Int Ed, 56, 10294–10323 (2017)
2016
Translocation of an intracellular protein via peptide-directed ligation
C Stiller, DM Krüger, N Brauckhoff, M Schmidt, P Janning, H Salamon, TN Grossmann*
ACS Chem Biol, 12, 504–509 (2017)
Constraining an irregular peptide secondary structure through ring-closing alkyne metathesis
PM Cromm, K Wallraven, A Glas, D Bier, A Fürstner, C Ottmann, TN Grossmann*
ChemBioChem, 17, 1915–1919 (2016) – open access (PDF)
Selective protein hyperpolarization in cell lysates using targeted dynamic nuclear polarization
T Viennet, A Viegas, A Kuepper, S Arens, V Gelev, O Petrov, TN Grossmann, H Heise, M Etzkorn*
Angew Chem Int Ed, 55, 10746–10750 (2016) – featured on inside cover
Protease-resistant and cell-permeable double-stapled peptides targeting the Rab8a GTPase
PM Cromm, J Spiegel, P Küchler, L Dietrich, J Kriegesmann, M Wendt, RS Goody, H Waldmann*, TN Grossmann*
ACS Chem Biol, 11, 2375–2382 (2016) – featured on cover
Orthogonal ring-closing alkyne and olefin metathesis for the synthesis of small GTPase-targeting bicyclic peptides
PM Cromm, S Schaubach, J Spiegel, A Fürstner*, TN Grossmann*, H Waldmann*
Nature Commun, 7, 11300 (2016) – open access (PDF)
2015
Redox modulation of PTEN phosphatase activty by hydrogen peroxide and bisperoxidovanadium complexes
CU Lee, G Hahne, J Hanske, T Bange, D Bier, C Rademacher, S Hennig, TN Grossmann*
Angew Chem Int Ed, 54, 13796–13800 (2015) – open access (PDF)
Direct modulation of small GTPase activity and function (review)
PM Cromm, J Spiegel, TN Grossmann*, H Waldmann*
Angew Chem Int Ed, 54, 13516–13537 (2015)
Structure-based design of inhibitors of protein-protein interactions: Mimicking peptide binding epitopes (review)
M Pelay‑Gimeno, A Glas, O Koch, TN Grossmann*
Angew Chem Int Ed, 54, 8896–8927 (2015) – open access (PDF)
Towards understanding cell penetration by stapled peptides
Q Chu, RE Moellering, GJ Hilinski, YW Kim, TN Grossmann, JTH Yeh, GL Verdine*
Med Chem Commun, 6, 111–119 (2015)
Hydrocarbon stapled peptides as modulators of biological function (review)
PM Cromm, J Spiegel, TN Grossmann*
ACS Chem Biol, 10, 1362–1375 (2015)
Constraining peptide conformations with the help of ring-closing metathesis (synpacts)
A Glas, TN Grossmann*
Synlett, 26, 1–5 (2015) – featured on cover
2014
Small-molecule modulation of Ras signaling (review)
J Spiegel, PM Cromm, G Zimmermann, TN Grossmann*, H Waldmann*
Nature Chem. Biol. 10, 613–622 (2014)
Protein-templated peptide ligation
N Brauckhoff, G Hahne, JTH Yeh, TN Grossmann*
Angew Chem Int Ed, 53, 4337–4340 (2014)
Modulators of protein-protein interactions (review)
LG Milroy, TN Grossmann, H Hennig, L Brunsveld, C Ottmann*
Chem Rev, 114, 4695–4748 (2014)
Constrained peptides with target-adapted cross-links as inhibitors of a pathogenic protein-protein interaction
A Glas, D Bier, G Hahne, C Rademacher, C Ottmann*, TN Grossmann*
Angew Chem Int Ed, 53, 2489–2493 (2014) – featured on back cover
Direct targeting of Rab-GTPase-effector interactions
J Spiegel, PM Cromm, A Itzen, RS Goody, TN Grossmann*, H Waldmann*
Angew Chem Int Ed, 53, 2498–2503 (2014)
Targeting the transcriptional hub β-catenin using stapled peptides
TN Grossmann, GL Verdine
Concepts and Case Studies in Chemical Biology (H Waldmann, P Janning), Wiley-VCH, Weinheim (2014)
2013
Means and methods for treating Pseudomonas infection
TN Grossmann, C Ottmann, A Glas, D Bier
patent appl. EP 2835135 A2 (priority: 19.06.2013)
Direct targeting of β-catenin: Inhibition of protein-protein interactions for the inactivation of Wnt signaling (review)
G Hahne, TN Grossmann*
Bioorg Med Chem, 21, 4020–4026 (2013)
Chemical Biology 2012: From drug targets to biological systems and back (conference report)
E Socher*, TN Grossmann*
ChemBioChem, 14, 23–27 (2013)
2012
Reversible covalent inhibition of a protein target (highlight)
CU Lee, TN Grossmann*
Angew Chem Int Ed, 51, 8699–8700 (2012)
Postdoc, Graduate and Undergraduate research
Inhibition of oncogenic Wnt signaling through direct targeting of β-catenin
TN Grossmann, JTH Yeh, BR Bowman, Q Chu, RE Moellering, GL Verdine*
PNAS, 109, 17942–17947 (2012)
Synthesis of all-hydrocarbon stapled α-helical peptides via ring-closing olefin metathesis
YW Kim, TN Grossmann, GL Verdine*
Nature Protoc, 6, 761–771 (2011)
DNA-instructed acyl transfer reactions for the synthesis of bioactive peptides
A Erben, TN Grossmann, O Seitz*
Bioorg Med Chem Lett, 21, 4993–4997 (2011)
DNA-triggered synthesis and bioactivity of proapoptotic peptides
A Erben, TN Grossmann, O Seitz*
Angew Chem Int Ed, 50, 2828–2832 (2011)
Semi-rational design of β-catenin targeting peptides for the inhibition of Wnt-dependent signalling (conference abstract)
TN Grossmann, JTH Yeh, GL Verdine*
EJC Suppl, 7, 31 (2010)
Beta-catenin targeting peptides and uses thereof
GL Verdine, TN Grossmann, JTH Yeh
patent appl. US 61/385405 (priority: 22.09.2010); WO 2012/040459 A2 (22.09.2011)
Bifunctional stapled polypeptides and uses thereof
GL Verdine, TN Grossmann, RE Moellering, JTH Yeh, Y Liang
patent appl. US 61/225191 (priority: 13.07.2009); WO 2011/008260 A2 (20.01.2011)
Nucleic acid-templated reactions: Consequences of probe reactivity and readout strategy for amplified signaling and sequence selectivity
TN Grossmann, O Seitz*
Chem Eur J, 15, 6723–6730 (2009)
New aspects in fragmentation of peptide nucleic acids: Comparison of positive and negative ions by electrospray ionization Fourier transform ion cyclotron resonance mass spectrometry
M Ziehe, TN Grossmann, O Seitz, MW Linscheid*
Rapid Commun Mass Spectrom, 23, 1132–1138 (2009)
Chemical control of biomolecular interaction modules
F Altenbrunn, TN Grossmann, C Haase, F Mende, L Röglin, O Seitz*
Pure Appl Chem, 81, 273–284 (2009)
Photo-thermal haptotropism in cyclopentadienylcobalt complexes of linear phenylenes: Intercyclobutadiene metal migration
TA Albright, PI Dosa, TN Grossmann, VN Khrustalev, OA Oloba, R Padilla, R Paubelle, A Stanger, TV Timofeeva, KPC Vollhardt*
Angew Chem Int Ed, 48, 9853–9857 (2009)
Target-catalyzed transfer reactions for the amplified detection of RNA
TN Grossmann, L Röglin, O Seitz*
Angew Chem Int Ed, 47, 7119–7122 (2008)
Single nucleotide polymorphism
TN Grossmann, O Seitz
Nucleic Acids from A to Z (S Müller), Wiley-VCH, Weinheim (2008)
Achieving turnover in DNA-templated reactions (review)
TN Grossmann, A Strohbach, O Seitz*
ChemBioChem, 9, 2185–2192 (2008)
Inducing the replacement of PNA in DNA·PNA duplexes by DNA
TN Grossmann, S Sasaki, M Ritzefeld, SW Choi, A Maruyama, O Seitz*
Bioorg Med Chem, 16, 34–39 (2008)
Triplex molecular beacons as modular probes for DNA detection
TN Grossmann, L Röglin, O Seitz*
Angew Chem Int Ed, 46, 5223–5225 (2007)
Probe for detecting a particular nucleic acid sequence
O Seitz, TN Grossmann, L Röglin
patent appl. EP 1995327 A1 (priority: 21.06.2007); WO 2008/142571 A2 (27.11.2008)
DNA-catalyzed transfer of a reporter group
TN Grossmann, O Seitz*
J Am Chem Soc, 128, 15596–15597 (2006)
Methods for detecting target nucleic acids using template catalysed transfer reactions
O Seitz, TN Grossmann
patent appl. EP 1860197 A1 (priority: 24.05.2006); WO 2007/134869 A1 (29.11.2007)