Prof. Dr. Tom N. Grossmann

Chair of Biomimetic Chemistry
ResearcherID: A-4175-2015
ORCID: 0000-0003-0179-4116

Curriculum Vitae

Department of Chemistry and
Pharmaceutical Sciences

Amsterdam Institute for
Molecules, Medicines and Systems

VU University Amsterdam
De Boelelaan 1108
1081 HZ Amsterdam, The Netherlands



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, Anita 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




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)




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

peptide beacon


Protein-RNA interactions: Structural characteristics and hotspot amino acids
DM Krüger, S Neubacher, TN Grossmann*
RNA, 24, – 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, e0134618 (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)

nucleic acids


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, , , , , , *, *, 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)


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)


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


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)


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)


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 – PDF)

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)