Wu Lab

PUBLICATIONS

Selected publications from 2019 to 2024 (*corresponding author; ^#equally contributed authors):

Mao Jiang, Nicole Giannino, Georg L. Goebel, Sonja Sievers, Peng Wu*
LIN28-Targeting Chromenopyrazoles and Tetrahydroquinolines Induced Cellular Morphological Changes and Showed High Biosimilarity with BRD PROTACs, ChemMedChem, 01 October 2024
https://doi.org/10.1002/cmdc.202400547

Georg Goebel, Nicole Giannino, Philipp Lampe, Xiaqiu Qiu, Jeffrey Schloßhauer, Jochen Imig, Sonja Sievers, Peng Wu*.
Profiling Cellular Morphological Changes Induced by Dual-targeting PROTACs of Aurora Kinase and RNA-binding Protein YTHDF2. ChemBioChem. 2024
https://doi.org/10.1002/cbic.202400183

(Invited submission for the special issue “Advances in Chemical Probing Concepts for Chemical Biology Applications”)

Ruth Brenk, Peng Wu and Maria Duca*.
Introduction to the themed collection on ‘Targeting RNA with small molecules’. RSC Med. Chem. 2024
https://doi.org/10.1039/D4MD90017K

Yang Liu^#, Georg L. Goebel^#, Laurin Kanis, Oguz Hastürk, Claus Kemker, and Peng Wu*.
Aminothiazolone Inhibitors Disrupt the Protein–RNA Interaction of METTL16 and Modulate the m6A RNA Modification. JACS Au 2024
https://doi.org/10.1021/jacsau.3c00832

Lydia Borgelt, Lisa Hohnen, Jakob S. Pallesen, Pascal Hommen, Georg L. Goebel, Francesco Bosica, Yang Liu, Gavin O’Mahony*, and Peng Wu*.
N-Biphenyl Pyrrolinones and Dibenzofurans as RNA-Binding Protein LIN28 Inhibitors Disrupting the LIN28–Let-7 Interaction. ACS Med. Chem. Lett. 2023
https://doi.org/10.1021/acsmedchemlett.3c00341

L. Borgelt and P. Wu*. Targeting Ribonucleases with Small Molecules and Bifunctional Molecules. ACS Chem. Biol. 2023
doi: 10.1002/cbic.202300376
(Invited submission, “Nucleic Acid Regulation” special issue)

P. Hommen, J. Hwang, F. Huang, L. Borgelt, L. Hohnen, P. Wu*.
Chromenopyrazole–peptide conjugates as small-molecule based inhibitors disrupting the protein–RNA interaction of LIN28–let-7. ChemBioChem 2023, accepted.
doi:10.1002/cbic.202300376.

(for the special issue of “ChemBioTalents 2022/2023”)

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L. Borgelt^#, F. Huang^#, L. Hohnen, X. Qiu, G. Goebel, P. Hommen, P. Wu*.
Spirocyclic chromenopyrazole inhibitors disrupting the interaction between the RNA-binding protein LIN28 and let-7. ChemBioChem 2023,accepted.
doi: 10.1002/cbic.202300168.

(Invited submission for the special issue of “ChemBioTalents 2022/2023”)

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J. Hwang^#, H. Haacke^#, L. Borgelt, X. Qiu, R. Gasper, P. Wu*.
Rational design and evaluation of 2-((pyrrol-2-yl)methylene)thiophen-4-ones as RNase L inhibitors. Eur. J. Med. Chem. 2023, accepted,
see more >

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A. Avathan Veettil, J. Kirchhoff, L. Brieger, C. Strohmann, P. Wu*.
Petasis sequence reactions for the scaffold-diverse synthesis of bioactive polycyclic small molecules. ACS Omega. 2023, 8 (1), 1168–1181.
doi: 10.1021/acsomega.2c06585

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L. Borgelt^#, N. Haacke^#, P. Lampe^#, X. Qiu, R. Gasper, D. Schiller, D. Summerer, S. Sievers, P. Wu*.
Small molecule screening of ribonuclease L binders for RNA degradation. Biomed. Pharmacother. 2022, 154, 113589.
DOI: 10.1016/j.biopha.2022.113589.

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G. Goebel^#, X, Qiu^#, P. Wu*.
Kinase-targeting small-molecule inhibitors and emerging bifunctional molecules. Trends Pharmacol. Sci. 2022, 43 (10), 866–881.
DOI: 10.1016/j.tips.2022.04.006.

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C. Hui, Y. Liu, M. Jiang, P. Wu*.
Cyclobutane-containing scaffolds in bioactive small molecules. Trends Chem. 2022, 4 (8), 677–681.
DOI: 10.1016/j.trechm.2022.04.006.

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J. Hwang^#, X, Qiu^#, L. Borgelt, N. Haacke, L. Kanis, S. Petroulia, R. Gasper, D. Schiller, P. Lampe, S. Sievers, J. Imig, P. Wu*.

Synthesis and evaluation of RNase L-binding 2-aminothiophenes as anticancer agents. Bioorg. Med. Chem. 2022, 58, 116653.
DOI: 10.1016/j.bmc.2022.116653.

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G. L. Goebel#, L. Hohnen#, L. Borgelt, P. Hommen, X. Qiu, H. Lightfoot, P. Wu*.
Small molecules with tetrahydroquinoline-containing Povarov scaffolds as inhibitors disrupting the Protein–RNA Interaction of LIN28–Let-7. Eur. J. Med. Chem. 2022, 228, 114014.,
DOI: 10.1016/j.ejmech.2021.114014

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L. Borgelt#, F. Li#, P. Hommen#, P. Lampe#, J. Hwang, G. L. Goebel, S. Sievers, P. Wu*. Trisubstituted Pyrrolinones as Small-Molecule Inhibitors Disrupting the Protein–RNA Interaction of LIN28 and Let-7. ACS Med. Chem. Lett. 2021,
DOI: 10.1021/acsmedchemlett.0c00546.
(Invited submission for the special issue of “RNA: Opening New Doors in Medicinal Chemistry”)

41
P. Wu*.
Inhibition of RNA-Binding Proteins with Small Molecules. Nat. Rev. Chem. 2020, 4, 441-458.
DOI: 10.1038/s41570-020-0201-4.

40
J. Hwang, L. Borgelt, P. Wu*.
Multicomponent Petasis Reaction for the Synthesis of Functionalized 2-Aminothiophenes and Thienodiazepines. ACS Comb. Sci. 2020, 22, 495-499.
DOI: 10.1021/acscombsci.0c00173.

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S. Siriwardena#, D. Godage#, V. Shoba#, S. Lai#, M. Shi, P. Wu, S. Chaudhary, S. L. Schreiber, A. Choudhary*.
Phosphorylation-Inducing Chimeric Small Molecules. J. Am. Chem. Soc. 2020, 142, 33, 14052-14057.
DOI:10.1021/jacs.0c05537.

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P. Wu*, M. Givskov, T. E. Nielsen*.
Reactivity and Synthetic Applications of Multicomponent Petasis Reactions. Chem. Rev. 2019, 119, 11245-11290.
DOI: 10.1021/acs.chemrev.9b00214.

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P. Wu#, W. E. Bjorn-Yoshimoto#, M. Staudt, A. A. Jensen*, L. Bunch*.
Identification and structure-activity relationship study of imidazo[1,2-α]pyridine-3-amines – as first selective inhibitors of excitatory amino acid transporter subtype 3 (EAAT3). ACS Chem NeuroSci. 2019, 10, 4414-4429.
DOI: 10.1021/acschemneuro.9b00447.

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B. Maji, S. Gangopadhyay#, M. Lee#, M. Shi#, P. Wu#, R. heler, B. Mok, D. Lim, S. Siriwardena, B. Paul, V. Dančík, A. Vetere, M. Mesleh, L. A. Marraffini, D. R. Liu, R. A. Clemons, B. K. Wagner, A. Choudhary*.
A high-throughput platform to identify inhibitors of CRISPR-Cas9. Cell 2019, 177, 1067-1079.E19.
DOI: 10.1016/j.cell.2019.04.009

Before 2019 and Full List of Publications >>>

BOOK CHAPTERS:

3.    P. Wu*, P. Diner, L. Bunch, Chapter 3. The Screening and Design of Allosteric Kinase Inhibitors
       Kinase Drug Discovery: Modern Approaches
     Edited by R. A. Ward and F. Goldberg
       Royal Society of Chemistry, London, 2019, Pp. 34-60
     DOI: 10.1039/9781788013093-00034

2.    P. Wu*, A. Choudhary*, Chapter II.2.
       Successful Drug Discovery, Volume 3
       Edited by J. Fischer, C. Klein and W. E. Childers
       Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, 2018, Pp. 65-93
       DOI: 10.1002/9783527808694.ch3

1.    P. Wu*, M. Givskov, T. E. Nielsen*, Chapter 2.4.2
       Drug Selectivity – An Evolving Concept in Drug Discovery
       Edited by N. Handler and H. Buschmann
       Book in Series Methods and Principles in Medicinal Chemistry, ISSN: 1865-0562
       Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim 2017, Pp. 33-53
       DOI: 10.1002/9783527674381.ch2