Preclinical characterization of a reversible XPO1 inhibitor for cancer therapy.
Van Hauwenhuyse J, Reniers F, Persoons L, Noppen S, Wing C E, Niesman AB, Fung HYJ, Vanstreels E, Jacquemyn M, Boel E, Vankerckhoven A, Berckmans Y, Kwanten B, Coosemans A, Van den Mooter G, Chook YM, Dehaen W, Daelemans D. Nature Communications. 2026 Jul 22. 17(1):8940. doi: 10.1038/s41467-026-75741-y.
Comparative evaluation of oncolytic viruses reveals opposing preferences for glioblastoma subtypes.
Deconinck T, Dierckx T, De Smet F, Baggen J, Daelemans D. Molecular Therapy Oncology. 2026 Jun 11. 34(3):201263. doi: 10.1016/j.omton.2026.201263.
SINE compounds activate exportin 1 degradation through an allosteric mechanism.
Wing CE, Fung HYJ, Kwanten B, Cagatay T, Niesman AB, Jacquemyn M, Gharghabi M, Permentier B, Shakya B, Nandi R, Ready JM, Kashyap T, Shacham S, Landesman Y, Lapalombella R, Daelemans D, Chook YM. Nature Chemical Biology. 2025 Dec. 21(12):2002-2013. doi: 10.1038/s41589-025-02058-0.
Ibetazol, a novel inhibitor of importin b1-mediated nuclear import.
Vercruysse T, Vanstreels E, Jacquemyn M, Boland S, Kilonda A, Allasia A, Vandecaetsbeek I, Klaassen H, Versele M, Chaltin P, Marchand A, Daelemans D. Communications Biology. 2024 Nov 23. 7(1):1560. doi: 10.1038/s42003-024-07237-8.
3-nitropyridine analogues as novel microtubule-targeting agents.
Herman J, Vanstreels E, Bardiot D, Prota A, Gaillard N, Gao L, Vercruysse T, Persoons L, Daems T, Waer M, Herdewijn P, Louat T, Steinmetz M, De Jonghe S, Sprangers B, Daelemans D.
PLoS One. 2024 Nov 7. 19(11):e0307153. doi: 10.1371/journal.pone.0307153. eCollection 2024.
TMEM106B is a receptor mediating ACE2-independent SARS-CoV-2 cell entry.
Baggen J, Jacquemyn M, Persoons L, Vanstreels E, Pye VE, Wrobel AG, Calvaresi V, Martin SR, Roustan C, Cronin NB, Reading E, Thibaut HJ, Vercruysse T, Maes P, De Smet F, Yee A, Nivitchanyong T, Roell M, Franco-Hernandez N, Rhinn H, Mamchak AA, Ah Young-Chapon M, Brown E, Cherepanov P, Daelemans D. Cell. 2023 Aug 3. 186(16):3427-3442.e22. doi: 10.1016/j.cell.2023.06.005.
E3 ubiquitin ligase ASB8 promotes selinexor-induced proteasomal degradation of XPO1
Kwanten B, Deconick T, Walker C, Wang F, Landesman Y, Daelemans D. Biomedicine & Pharmacotherapy. 2023 Apr. 160. doi: 10.1016/j.biopha.2023.114305
Target Identification of Small Molecules Using Large-Scale CRISPR-Cas Mutagenesis Scanning of Essential Genes.
Kwanten B, Neggers JE, Daelemans D. Methods in Molecular Biology. 2022. 2377:43-67. doi: 10.1007/978-1-0716-1720-5_3.
Cellular Stress Induces Nucleocytoplasmic Transport Deficits Independent of Stress Granules.
Vanneste J, Vercruysse T, Boeynaems S, Van Damme P, Daelemans D, Van Den Bosch L. Biomedicines. 2022 May 3. 10(5):1057. doi: 10.3390/biomedicines10051057.
Cellular host factors for SARS-CoV-2 infection.
Baggen J, Vanstreels E, Jansen S, Daelemans D. Nature Microbiology. 2021 Oct;6(10):1219-1232. doi: 10.1038/s41564-021-00958-0. PMID: 34471255 Review.
Genome-wide CRISPR screening identifies TMEM106B as a proviral host factor for SARS-CoV-2.
Baggen J, Persoons L, Vanstreels E, Jansen S, Van Looveren D, Boeckx B, Geudens V, De Man J, Jochmans D, Wauters J, Wauters E, Vanaudenaerde BM, Lambrechts D, Neyts J, Dallmeier K, Thibaut HJ, Jacquemyn M, Maes P, Daelemans D. Nature Genetics. 2021 doi: 10.1038/s41588-021-00805-2
Intermedilysin cytolytic activity depends on heparan sulfates and membrane composition.
Drabavicius G, Daelemans D. PLoS Genetics. 2021 doi: 10.1371/journal.pgen.1009387
XPO1 inhibitors represent a novel therapeutic option in Adult T-cell Leukemia, triggering p53-mediated caspase-dependent apoptosis.
Boons E, Nogueira TC, Dierckx T, Menezes SM, Jacquemyn M, Tamir S, Landesman Y, Farré L, Bittencourt A, Kataoka K, Ogawa S, Snoeck R, Andrei G, Van Weyenbergh J, Daelemans D. Blood Cancer Journal. 2021 doi: 10.1038/s41408-021-00409-3.
enAsCas12a Enables CRISPR-Directed Evolution to Screen for Functional Drug Resistance Mutations in Sequences Inaccessible to SpCas9. Neggers JE, Jacquemyn M, Dierckx T, Kleinstiver BP, Thibaut HJ, Daelemans D. Molecular Therapy. 2021 doi: 10.1016/j.ymthe.2020.09.025
Quantitative Nucleocytoplasmic Transport Assays in Cellular Models of Neurodegeneration.
Vanneste J, Vercruysse T, Van Damme P, Van Den Bosch L, Daelemans D.
Bio-Protocol. 2020 Jun 20. 10(12):e3659. doi:10.21769/BioProtoc.3659.
Iron/Copper Co-Catalyzed Cross-Coupling Reaction for the Synthesis of 6-Substituted 7-Deazapurines and the Corresponding Nucleosides.
Li Q, Persoons L, Daelemans D, Herdewijn P.
The Journal of Organic Chemistry. 2020 Jan 17. 85(2):403-418. doi:10.1021/acs.joc.9b02414.
C9orf72-generated poly-GR and poly-PR do not directly interfere with nucleocytoplasmic transport.
Vanneste J, Vercruysse T, Boeynaems S, Sicart A, Van Damme P, Daelemans D, Van Den Bosch L.
Scientific Reports. 2019 Oct 31. 9(1):15728. doi:10.1038/s41598-019-52035-6.
STK38 kinase acts as XPO1 gatekeeper regulating the nuclear export of autophagy proteins and other cargoes.
Martin AP, Jacquemyn M, Lipecka J, Chhuon C, Aushev VN, Meunier B, Singh MK, Carpi N, Piel M, Codogno P, Hergovich A, Parrini MC, Zalcman G, Guerrera IC, Daelemans D, Camonis JH. EMBO Reports. 2019 Nov 5. 20(11):e48150. doi:10.15252/embr.201948150.
Xylo-C-nucleosides with a pyrrolo[2,1-f][1,2,4]triazin-4-amine hetrocyclic base: Synthesis and antiproliferative properties.
Nie P, Groaz E, Daelemans D, Herdewijn P. Bioorganic & Medicinal Chemistry Letters. 2019 Jun 15. 29(12):1450-1453. doi:10.1016/j.bmcl.2019.04.023.
Down-regulation of AR splice variants through XPO1 suppression contributes to the inhibition of prostate cancer progression.
Aboukameel A, Muqbil I, Baloglu E, Senapedis W, Landesman Y, Argueta C, Kauffman M, Chang H, Kashyap T, Shacham S, Neggers JE, Daelemans D, Heath EI, Azmi AS. Oncotarget. 2018 Oct 19. 9(82):35327-35342. doi: 10.18632/oncotarget.26239.
Targeting the XPO1-dependent nuclear export of E2F7 reverses anthracycline resistance in head and neck squamous cell carcinomas.
Saenz-Ponce N, Pillay R, de Long LM, Kashyap T, Argueta C, Landesman Y, Hazar-Rethinam M, Boros S, Panizza B, Jacquemyn M, Daelemans D, Gannon OM, Saunders NA.
Science Translational Medicine. 2018 Jun 27. 10(447):eaar7223. doi: 10.1126/scitranslmed.aar7223.
Near-native, site-specific and purification-free protein labeling for quantitative protein interaction analysis by MicroScale Thermophoresis.
Bartoschik T, Galinec S, Kleusch C, Walkiewicz K, Breitsprecher D, Weigert S, Muller YA, You C, Piehler J, Vercruysse T, Daelemans D, Tschammer N.
Scientific Reports. 2018 Mar 21. 8(1):4977. doi: 10.1038/s41598-018-23154-3.
Target identification of small molecules using large-scale CRISPR-Cas mutagenesis scanning of essential genes.
Neggers JE, Kwanten B, Dierckx T, Noguchi H, Voet A, Bral L, Minner K, Massant B, Kint N, Delforge M, Vercruysse T, Baloglu E, Senapedis W, Jacquemyn M, Daelemans D. Nature Communications. 2018
The second-generation exportin-1 inhibitor KPT-8602 demonstrates potent activity against acute lymphoblastic leukemia.
Vercruysse T, De Bie J, Neggers J, Jacquemyn M, Vanstreels E, Schmid-Burgk JL, Hornung V, Baloglu E, Landesman Y, Senapedis W, Shacham S, Dagklis A, Cools J, Daelemans D. Clinical Cancer Research. 2016 Oct 25.
XPO1-dependent nuclear export is a druggable vulnerability in KRAS-mutant lung cancer.
Kim J, McMillan E, Kim HS, Venkateswaran N, Makkar G, Rodriguez-Canales J, Villalobos P, Neggers JE, Mendiratta S, Wei S, Landesman Y, Senapedis W, Baloglu E, Chow CB, Frink RE, Gao B, Roth M, Minna JD, Daelemans D, Wistuba II, Posner BA, Scaglioni PP, White MA. Nature. 2016 Oct 6;538(7623):114-117
Heterozygous mutation of cysteine528 in XPO1 is sufficient for resistance to selective inhibitors of nuclear export.
Neggers JE, Vanstreels E, Baloglu E, Shacham S, Landesman Y, Daelemans D. Oncotarget. 2016 Oct 18;7(42):68842-68850.
Human exportin-1 is a target for combined therapy of HIV and AIDS related lymphoma.
Boons E, Vanstreels E, Jacquemyn M, Nogueira TC, Neggers JE, Vercruysse T, van den Oord J, Tamir S, Shacahm S, Landesman Y, Snoeck R, Pannecouque C, Andrei G, Daelemans D. EBioMedicine. 2015 2:1102-1113
A stably expressed llama single-domain intrabody targeting Rev displays broad-spectrum anti-HIV activity.
Boons E, Li G, Vanstreels E, Vercruysse T, Pannecouque C, Vandamme AM, Daelemans D. Antiviral Research. 2014 Dec;112:91-102.
Dynamics of the ternary complex formed by c-Myc interactor JPO2, transcriptional co-activator LEDGF/p75, and chromatin.
Hendrix J, van Heertum B, Vanstreels E, Daelemans D, De Rijck J. Journal of Biological Chemistry. 2014 May 2. 289(18):12494-506. doi: 10.1074/jbc.M113.525964.
HIV-1 Rev multimerization: mechanism and insights.
Vercruysse T, Daelemans D. Current HIV Research. 2013 Dec;11(8):623-34.
Mapping the binding interface between an HIV-1 inhibiting intrabody and the viral protein Rev.
Vercruysse T, Boons E, Venken T, Vanstreels E, Voet A, Steyaert J, De Maeyer M, Daelemans D. PLoS One. 2013;8(4)
A time-of-drug addition approach to target identification of antiviral compounds.
Daelemans D, Pauwels R, De Clercq E, Pannecouque C. Nature Protocols. 2011 Jun;6(6):925-33.
Measuring cooperative Rev protein-protein interactions on Rev responsive RNA by fluorescence resonance energy transfer.
Vercruysse T, Pawar S, De Borggraeve W, Pardon E, Pavlakis GN, Pannecouque C, Steyaert J, Balzarini J, Daelemans D. RNA Biology. 2011 Mar-Apr;8(2):316-24.
An intrabody based on a llama single-domain antibody targeting the N-terminal alpha-helical multimerization domain of HIV-1 rev prevents viral production.
Vercruysse T, Pardon E, Vanstreels E, Steyaert J, Daelemans D. Journal of Biological Chemistry. 2010 Jul 9;285(28):21768-80.
Inhibition of HIV-1 replication by a bis-thiadiazolbenzene-1,2-diamine that chelates zinc ions from retroviral nucleocapsid zinc fingers.
Pannecouque C, Szafarowicz B, Volkova N, Bakulev V, Dehaen W, Mély Y, Daelemans D. Antimicrobial Agents and Chemotherapy. 2010 Apr;54(4):1461-8.
Debio-025 inhibits HIV-1 by interfering with an early event in the replication cycle.
Daelemans D, Dumont JM, Rosenwirth B, De Clercq E, Pannecouque C. Antiviral Research. 2010 Feb;85(2):418-21.
Inhibition of the CRM1-mediated nucleocytoplasmic transport by N-azolylacrylates: structure-activity relationship and mechanism of action.
Van Neck T, Pannecouque C, Vanstreels E, Stevens M, Dehaen W, Daelemans D. Bioorganic & Medicinal Chemistry. 2008 Nov 1;16(21):9487-97.
Tetrazolium-based colorimetric assay for the detection of HIV replication inhibitors: revisited 20 years later.
Pannecouque C, Daelemans D, De Clercq E. Nature Protocols. 2008;3(3):427-34.
Characterization of a replication-competent, integrase-defective human immunodeficiency virus (HIV)/simian virus 40 chimera as a powerful tool for the discovery and validation of HIV integrase inhibitors.
Daelemans D, Lu R, De Clercq E, Engelman A. Journal of Virology. 2007 Apr;81(8):4381-5.
HIV-1 Rev function as target for antiretroviral drug development.
Daelemans D, Pannecouque C. HIV-1 Rev function as target for antiretroviral drug development. Current Opinion in HIV and AIDS. 2006 Sep;1(5):388-97.
A novel and efficient approach to discriminate between pre- and post-transcription HIV inhibitors.
Daelemans D, Pannecouque C, Pavlakis GN, Tabarrini O, De Clercq E. Molecular Pharmacology. 2005 May;67(5):1574-80.
Kinetic and molecular analysis of nuclear export factor CRM1 association with its cargo in vivo.
Daelemans D, Costes SV, Lockett S, Pavlakis GN. Molecular Cell Biology. 2005 Jan;25(2):728-39.
In vivo HIV-1 Rev multimerization in the nucleolus and cytoplasm identified by fluorescence resonance energy transfer.
Daelemans D, Costes SV, Cho EH, Erwin-Cohen RA, Lockett S, Pavlakis GN. Journal of Biological Chemistry. 2004 Nov 26;279(48):50167-75.
A synthetic HIV-1 Rev inhibitor interfering with the CRM1-mediated nuclear export.
Daelemans D, Afonina E, Nilsson J, Werner G, Kjems J, De Clercq E, Pavlakis GN, Vandamme AM. Proceedings of the National Academy of Sciences. 2002 Oct 29;99(22):14440-5.
A quantitative GFP-based bioassay for the detection of HIV-1 Tat transactivation inhibitors.
Daelemans D, De Clercq E, Vandamme AM. Journal of Virological Methods. 2001 Aug;96(2):183-8.
A second target for the peptoid Tat/transactivation response element inhibitor CGP64222: inhibition of human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry.
Daelemans D, Schols D, Witvrouw M, Pannecouque C, Hatse S, van Dooren S, Hamy F, Klimkait T, de Clercq E, VanDamme AM. Molecular Pharmacology. 2000 Jan;57(1):116-24.
Human immunodeficiency virus gene regulation as a target for antiviral chemotherapy.
Daelemans D, Vandamme AM, De Clercq E. Antiviral Chemistry and Chemotherapy. 1999 Jan;10(1):1-14. Review.
Stereospecificity of 6′-C-neplanocin A analogues as inhibitors of S-adenosylhomocysteine hydrolase activity and human immunodeficiency virus replication.
Daelemans D, Vandamme AM, Shuto S, Matsuda A, De Clercq E. Nucleosides Nucleotides. 1998 Jan-Mar;17(1-3):479-86.
S-adenosylhomocysteine hydrolase inhibitors interfere with the replication of human immunodeficiency virus type 1 through inhibition of the LTR transactivation.
Daelemans D, Esté JA, Witvrouw M, Pannecouque C, Jonckheere H, Aquaro S, Perno CF, De Clercq E, Vandamme AM. Molecular Pharmacology. 1997 Dec;52(6):1157-63.