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., DOI: 10.1002/anie.202102082 (PDF)
2020
Stapled Peptide Inhibitors of Protein-Protein Interactions
M Wendt, NM McLoughlin, TN Grossmann
Inhibitors of Protein-Protein Interactions: Small Molecules, Peptides and Macrocycles (A Tavassoli), Royal Society of Chemistry, London (2020)
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) (PDF)
Proteomimetics as protein-inspired scaffolds with defined tertiary folding patterns (perspective)
WS Horne*, TN Grossmann*
Nature Chem., 12, 331–337 (2020) (PDF)
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)
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)
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)
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
2019
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., 131, 17512–17519; Angew. Chem. Int. Ed., 58, 17351–17358 (2019) – open access (PDF)
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)
Organisch-chemisch stabilisierte Enzyme für eine nachhaltige Wirtschaft
S Neubacher, S Hennig, TN Grossmann*
BIOspektrum, 25, 338–339 (2019) – open access (PDF)
2018
Coiled-coil peptide beacon: A tuneable conformational switch for protein detection
C Mueller, TN Grossmann*
Angew. Chem., 130, 17325–17329; Angew. Chem. Int. Ed., 57, 17079–17083 (2018) – open access (PDF) – featured on inside cover
Protein-RNA interactions: Structural characteristics and hotspot amino acids
DM Krüger, S Neubacher, TN Grossmann*
RNA, 24, 1157–1165 (2018) – open access (PDF)
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)
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)
In situ cyclization of native proteins: Structure-based design of a bicyclic enzyme
M Pelay‑Gimeno, T Bange, S Hennig, TN Grossmann*
Angew. Chem., 130, 11334–11340; Angew. Chem. Int. Ed., 57, 11164–11170 (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)
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)
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)
2017
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. 129, 10428–10459; Angew. Chem. Int. Ed. 56, 10294–10323 (2017)
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)
2016
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. 128, 10904–10908; 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. 127, 14001–14005; 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. 127, 13718–13741; 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. 127, 9022–9054; 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. 126, 4425–4429; 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. 126, 2522–2526; 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. 126, 2531–2536; 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. 124, 8829–8831; 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. 123, 2880–2884; 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. 121, 10037–10041; 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. 120, 7228–7231; 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. 119, 5315–5318; 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)