Publications
2025
Openy, J., Vega-Ces, S., Amrahova, G., Mestdach, E., Chi, C., Kissel, B., ‘t Hart, P.
Single atom substitutions in backbone aromatic groups alter membrane permeability and biological activity of cyclic peptides
ChemRxiv, 2025. https://doi.org/10.26434/chemrxiv-2025-pb6d3Pal, S., Gordijenko, I., Schmeing, S., Biswas, S., Akbulut, Y., Gasper, R., 't Hart, P.
Stapled Peptides as Inhibitors of mRNA Deadenylation
Angew. Chem. Int. Ed., 2025, 64(1), e202413911. https://doi.org/10.1002/anie.2024139112024
Schmeing, S., 't Hart, P.
Challenges in Therapeutically Targeting the RNA-Recognition Motif
WIREs Interdisciplinary reviews: RNA, 2024, 15(6), e1877. https://doi.org/10.1002/wrna.1877Pal, S., ‘t Hart, P.
Imbuing peptide libraries with drug-likeness
Nat. Chem. Biol., 2024, 20(2), 140–141. https://doi.org/10.1038/s41589-023-01524-xChang, J.Y., Neugebauer, C., Mues genannt Koers, A., ‘t Hart, P.
Small molecule WDR5 inhibitors down-regulate lncRNA expression
RSC Med. Chem., 2024, 15, 636. https://doi.org/10.1039/D3MD00605K2023
Chang, J.Y., Neugebauer, C., Schmeing, S., Amrahova, G., ‘t Hart, P.
Macrocyclic peptides as inhibitors of WDR5–lncRNA interactions
Chem. Commun., 2023, 59, 10656. https://doi.org/10.1039/D3CC03221CSchmeing, S., Amrahova, G., Bigler, K., Chang, J.Y., Openy, J., Pal, S., Posada, L., Gasper, R., 't Hart P.
Rationally designed stapled peptides allosterically inhibit PTBP1 RNA-binding
Chem. Sci., 2023, 14, 8269. https://doi.org/10.1039/D3SC00985HPal, S., Openy, J., Krzyzanowski, A., Noisier, A., 't Hart, P.
On-resin Photochemical Decarboxylative Arylation of Peptides
Org. Lett., 2023, 26(14), 2795. https://doi.org/10.1021/acs.orglett.3c03070Nowacki, J., Malenica, M., Schmeing, S., Schiller, D., Buchmuller, B., Amrahova, G., ‘t Hart P.
A translational repression reporter assay for the analysis of RNA-binding protein consensus sites
RNA Biology, 2023, 20(1), 85. https://doi.org/10.1080/15476286.2023.21925532022
Krzyzanowski, A., Esser, L.M., Willaume, A., Prudent, R., Peter, C., ‘t Hart. P., Waldmann, H.
Development of Macrocyclic PRMT5 Adaptor Protein Interaction Inhibitors
J. Med. Chem., 2022, 65(22), 15300. https://doi.org/10.1021/acs.jmedchem.2c01273Openy, J., Amrahova, G., Chang, J., Noisier, A., ‘t Hart, P.
Solid‐phase peptide modification via deaminative photochemical Csp3‐Csp3 bond formation using Katritzky salts
Chem. Eur. J., 2023, 28(39), e202201121. https://doi.org/10.1002/chem.202201121Pal, S., 't Hart, P.
RNA-Binding Macrocyclic Peptides
Front Mol. Biosci., 2022, 9, 83060. https://doi.org/10.3389/fmolb.2022.8830602021
Krzyzanowski, A., Gasper, R., Adihou, H., ’t Hart, P., Waldmann, H.
Biochemical Investigation of the Interaction of PICln, RioK1 and COPR5 with the PRMT5–MEP50 Complex
ChemBioChem, 2021, 22(11), 1908. https://doi.org/10.1002/cbic.202100079‘t Hart, P., Hommen, P., Noisier, A., Krzyzanowski, A., Schüler, D., Porfetye, A.T., Akbarzadeh, M., Vetter, I.R., Adihou, H., Waldmann, H.
Structure Based Design of Bicyclic Peptide Inhibitors of RbAp48
Angew. Chem. Int. Ed., 2021, 60(4), 1813. https://doi.org/10.1002/anie.2020097492019
‘t Hart, P., Openy, J., Krzyzanowski, A., Adihou, H., Waldmann, H.
Hot-Spot Guided Design of Macrocyclic Inhibitors of the LSD1-CoREST1 Interaction
Tetrahedron, 2019, 75(48), 130685. https://doi.org/10.1016/j.tet.2019.1306852017
le Paige, U.B., Smits, B., ‘t Hart, P., Lefeber, F., Martin, N.I., van Ingen, H.
Weak Coupling between Magnetically Inequivalent Spins: The Deceptively Simple, Complicated Spectrum of a13C-Labeled Trimethylated Amine
Journal of Magnetic Resonance, 2017, 278, 96. https://doi.org/10.1016/j.jmr.2017.03.016’t Hart, P., Wood, T.M., Tehrani, K.H.M.E., van Harten, R.M., Śleszyńska, M., Rentero Rebollo, I., Hendrickx, A.P.A., Willems, R.J.L., Breukink, E., Martin, N.I.
De Novo Identification of Lipid II Binding Lipopeptides with Antibacterial Activity against Vancomycin-Resistant Bacteria
Chem. Sci., 2017, 8(12), 7991. https://doi.org/10.1039/C7SC03413J2016
Kleijn, L.H.J., Oppedijk, S.F., ‘t Hart, P., van Harten, R.M., Martin-Visscher, L.A., Kemmink, J., Breukink, E., Martin, N.I., 2016.
“Total Synthesis of Laspartomycin C and Characterization of Its Antibacterial Mechanism of Action.”
Journal of Medicinal Chemistry. 59(7):3569–74. https://pubs.acs.org/doi/10.1021/acs.jmedchem.6b00219’t Hart, P., Oppedijk, S.F., Breukink, E., Martin, N.I., 2016.
“New Insights into Nisin’s Antibacterial Mechanism Revealed by Binding Studies with Synthetic Lipid II Analogues.”
Biochemistry. 55(1):232–37. https://pubs.acs.org/doi/10.1021/acs.biochem.5b011732015
Koopmans, T., Wood, T.M., ’t Hart, P., Kleijn, L.H.J., Hendrickx, A.P.A., Willems, R.J.L., Breukink, E., Martin, N.I., 2015.
“Semisynthetic Lipopeptides Derived from Nisin Display Antibacterial Activity and Lipid II Binding on Par with That of the Parent Compound.”
Journal of the American Chemical Society. 137(29):9382–89. https://pubs.acs.org/doi/10.1021/jacs.5b045012014
Mooney, C.A., Johnson, S.A., ’t Hart, P., Quarles van Ufford, L., de Haan, C.A.M., Moret, E.E., Martin. N.I., 2014.
“Oseltamivir Analogues Bearing N-Substituted Guanidines as Potent Neuraminidase Inhibitors.”
Journal of Medicinal Chemistry. 57(7):3154–60. https://pubs.acs.org/doi/10.1021/jm401977j‘t Hart, P., Kleijn, L.H.J., de Bruin, G., Oppedijk, S.F., Kemmink, J., Martin, N.I., 2014.
“A Combined Solid- and Solution-Phase Approach Provides Convenient Access to Analogues of the Calcium-Dependent Lipopeptide Antibiotics.”
Organic & Biomolecular Chemistry. 12(6):913–18. https://pubs.rsc.org/en/content/articlehtml/2014/ob/c3ob42238k2012
‘t Hart, P.*, Thomas, D.*, Van Ommeren, R., Lakowski, T.M., Frankel, A., Martin, N.I., 2012.
“Analogues of the HIV-Tat Peptide Containing Nη-Modified Arginines as Potent Inhibitors of Protein Arginine N-Methyltransferases.”
MedChemComm. 3(10). https://pubs.rsc.org/en/content/articlelanding/2012/md/c2md20161e2011
’t Hart, P.*, Lakowski, T.M.*, Thomas, D., Frankel, A., Martin, N.I., 2011.
“Peptidic Partial Bisubstrates as Inhibitors of the Protein Arginine N-Methyltransferases.”
ChemBioChem. 12(9):1427–32. https://pubmed.ncbi.nlm.nih.gov/21560220/2010
Lakowski, T.M.*, ‘t Hart, P.*, Ahern, C.A., Martin, N.I., Frankel, A. 2010.
“Nη-Substituted Arginyl Peptide Inhibitors of Protein Arginine N-Methyltransferases.”
ACS Chemical Biology. 5(11):1053–63. https://pubmed.ncbi.nlm.nih.gov/20701328/*equal contribution