D Daelemans

Summary

Affiliation: Katholieke Universiteit Leuven
Country: Belgium

Publications

  1. ncbi S-adenosylhomocysteine hydrolase inhibitors interfere with the replication of human immunodeficiency virus type 1 through inhibition of the LTR transactivation
    D Daelemans
    Rega Institute for Medical Research, Katholieke Universtiteit Leuven, Belgium
    Mol Pharmacol 52:1157-63. 1997
  2. ncbi Stereospecificity of 6'-C-neplanocin A analogues as inhibitors of S-adenosylhomocysteine hydrolase activity and human immunodeficiency virus replication
    D Daelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Nucleosides Nucleotides 17:479-86. 1998
  3. ncbi Human immunodeficiency virus gene regulation as a target for antiviral chemotherapy
    D Daelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antivir Chem Chemother 10:1-14. 1999
  4. ncbi 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
    D Daelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 57:116-24. 2000
  5. pmc Kinetic and molecular analysis of nuclear export factor CRM1 association with its cargo in vivo
    Dirk Daelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, 3000 Leuven, Belgium
    Mol Cell Biol 25:728-39. 2005
  6. ncbi A quantitative GFP-based bioassay for the detection of HIV-1 Tat transactivation inhibitors
    D Daelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, 3000, Leuven, Belgium
    J Virol Methods 96:183-8. 2001
  7. pmc A synthetic HIV-1 Rev inhibitor interfering with the CRM1-mediated nuclear export
    Dirk Daelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Proc Natl Acad Sci U S A 99:14440-5. 2002
  8. doi Inhibition of the CRM1-mediated nucleocytoplasmic transport by N-azolylacrylates: structure-activity relationship and mechanism of action
    Tine Van Neck
    Laboratory of Organic Synthesis, Katholieke Universiteit Leuven, Celestijnenlaan 200F, B 3001 Leuven, Belgium
    Bioorg Med Chem 16:9487-97. 2008
  9. pmc An intrabody based on a llama single-domain antibody targeting the N-terminal alpha-helical multimerization domain of HIV-1 rev prevents viral production
    Thomas Vercruysse
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    J Biol Chem 285:21768-80. 2010
  10. pmc Pradimicin A, a carbohydrate-binding nonpeptidic lead compound for treatment of infections with viruses with highly glycosylated envelopes, such as human immunodeficiency virus
    Jan Balzarini
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    J Virol 81:362-73. 2007

Collaborators

Detail Information

Publications24

  1. ncbi S-adenosylhomocysteine hydrolase inhibitors interfere with the replication of human immunodeficiency virus type 1 through inhibition of the LTR transactivation
    D Daelemans
    Rega Institute for Medical Research, Katholieke Universtiteit Leuven, Belgium
    Mol Pharmacol 52:1157-63. 1997
    ..Our results suggest that AdoHcy hydrolase and the associated S-adenosylmethionine-dependent methylation mechanism play a role in the process of long terminal repeat transactivation and, hence, HIV replication...
  2. ncbi Stereospecificity of 6'-C-neplanocin A analogues as inhibitors of S-adenosylhomocysteine hydrolase activity and human immunodeficiency virus replication
    D Daelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Nucleosides Nucleotides 17:479-86. 1998
    ..The R-isomers showed much greater activity against AdoHcy hydrolase than the S-isomers. The same differential activity was observed against the HIV-1 replication and the Tat transactivation...
  3. ncbi Human immunodeficiency virus gene regulation as a target for antiviral chemotherapy
    D Daelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antivir Chem Chemother 10:1-14. 1999
    ..Although a promising lead, considerable research is still required before gene regulation inhibitors may come of age as clinically useful agents...
  4. ncbi 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
    D Daelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 57:116-24. 2000
    ..Mechanism of action studies revealed that CGP64222 can inhibit the HIV replicative cycle, also through a selective interaction with the CXC-chemokine receptor 4 coreceptor...
  5. pmc Kinetic and molecular analysis of nuclear export factor CRM1 association with its cargo in vivo
    Dirk Daelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, 3000 Leuven, Belgium
    Mol Cell Biol 25:728-39. 2005
    ..CRM1 is able to bind Rev cargo in the nucleolus, and upon RanGTP binding a functional export complex is produced that is exported to the cytoplasm...
  6. ncbi A quantitative GFP-based bioassay for the detection of HIV-1 Tat transactivation inhibitors
    D Daelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, 3000, Leuven, Belgium
    J Virol Methods 96:183-8. 2001
    ..The assay can be used for the detection and quantification of HIV transactivation, and for the high throughput evaluation of anti-transactivation drugs in different cellular backgrounds...
  7. pmc A synthetic HIV-1 Rev inhibitor interfering with the CRM1-mediated nuclear export
    Dirk Daelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Proc Natl Acad Sci U S A 99:14440-5. 2002
    ..The reversibility of its binding to CRM1 and its availability through chemical synthesis could make it useful for studying CRM1-mediated export pathways...
  8. doi Inhibition of the CRM1-mediated nucleocytoplasmic transport by N-azolylacrylates: structure-activity relationship and mechanism of action
    Tine Van Neck
    Laboratory of Organic Synthesis, Katholieke Universiteit Leuven, Celestijnenlaan 200F, B 3001 Leuven, Belgium
    Bioorg Med Chem 16:9487-97. 2008
    ..These specific CRM1 inhibitors are of interest as tool for analyzing the mechanisms of post-transcriptional control of gene expression and provide insight in the design of new agents...
  9. pmc An intrabody based on a llama single-domain antibody targeting the N-terminal alpha-helical multimerization domain of HIV-1 rev prevents viral production
    Thomas Vercruysse
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    J Biol Chem 285:21768-80. 2010
    ..The results indicate that the oligomeric assembly of Rev follows an ordered stepwise process and identify a new epitope within Rev that could guide strategies for the development of novel HIV inhibitors...
  10. pmc Pradimicin A, a carbohydrate-binding nonpeptidic lead compound for treatment of infections with viruses with highly glycosylated envelopes, such as human immunodeficiency virus
    Jan Balzarini
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    J Virol 81:362-73. 2007
    ....
  11. ncbi A novel and efficient approach to discriminate between pre- and post-transcription HIV inhibitors
    Dirk Daelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Mol Pharmacol 67:1574-80. 2005
    ..This GFP-based reporter system is adaptable for high-throughput screening...
  12. ncbi 2-Chloro-3-pyridin-3-yl-5,6,7,8-tetrahydroindolizine-1-carboxamide (CMV423), a new lead compound for the treatment of human cytomegalovirus infections
    Robert Snoeck
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, Belgium
    Antiviral Res 55:413-24. 2002
    ..Finally, CMV423 combined with either ganciclovir, foscarnet or cidofovir in checkerboard experiments demonstrated a highly synergistic activity...
  13. ncbi Mouse adenovirus type 1 attachment is not mediated by the coxsackie-adenovirus receptor
    L Lenaerts
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    FEBS Lett 580:3937-42. 2006
    ..These results support further exploration of an MAV-1-derived vector as a potential vehicle for gene delivery to cell types which are not efficiently transduced by human adenovirus vectors...
  14. pmc Inhibition of HIV-1 replication by a bis-thiadiazolbenzene-1,2-diamine that chelates zinc ions from retroviral nucleocapsid zinc fingers
    Christophe Pannecouque
    Rega Institute, Katholieke Universiteit Leuven, Minderbroedersstraat 10, 3000 Leuven, Belgium
    Antimicrob Agents Chemother 54:1461-8. 2010
    ..This new lead and the mechanistic study presented provide insight into the design of a future generation of anti-NCp7 compounds...
  15. doi Debio-025 inhibits HIV-1 by interfering with an early event in the replication cycle
    Dirk Daelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Antiviral Res 85:418-21. 2010
    ..The compound proved inactive against mutant viruses that are independent of cyclophilin A binding suggesting Debio-025 targets the cyclophilin A-capsid interaction...
  16. doi Tetrazolium-based colorimetric assay for the detection of HIV replication inhibitors: revisited 20 years later
    Christophe Pannecouque
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B 3000 Leuven, Belgium
    Nat Protoc 3:427-34. 2008
    ..The use of this method can be extended to antiviral testing of compounds against other cyto-destructive viruses...
  17. ncbi Specific targeting of the F13L protein by ST-246 affects orthopoxvirus production differently
    Sophie Duraffour
    Rega Institute for Medical Research, KU Leuven, Leuven, Belgium
    Antivir Ther 13:977-90. 2008
    ..The discrepancy in sensitivities of several orthopoxviruses to ST-246 has raised questions about potential differences in their replicative cycles and/or the presence of another drug target...
  18. ncbi Capture and transmission of HIV-1 by the C-type lectin L-SIGN (DC-SIGNR) is inhibited by carbohydrate-binding agents and polyanions
    Joeri Auwerx
    Virology and Chemotherapy, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Antiviral Res 83:61-70. 2009
    ..The excess value of CBAs and polyanions to prevent HIV-1 capture and transmission by DC-SIGN and L-SIGN-expressing cells to susceptible T-lymphocytes could be of interest for the development of new drug leads targeting HIV entry/fusion...
  19. doi Fluorescence-based antiviral assay for the evaluation of compounds against vaccinia virus, varicella zoster virus and human cytomegalovirus
    Fabiana Dal Pozzo
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, 3000 Leuven, Belgium
    J Virol Methods 151:66-73. 2008
    ..Furthermore the fluorimetric data could be confirmed by a flow cytometry assay. GFP- and EYFP-recombinant viruses proved to be a convenient tool for the evaluation of antiviral agents...
  20. ncbi The nucleotide analog cidofovir suppresses basic fibroblast growth factor (FGF2) expression and signaling and induces apoptosis in FGF2-overexpressing endothelial cells
    Sandra Liekens
    Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, Leuven, Belgium
    Mol Pharmacol 71:695-703. 2007
    ..These findings suggest that the clinical use of cidofovir might be expanded to tumors that are not induced by oncogenic viruses...
  21. ncbi Entry of hepatitis C virus and human immunodeficiency virus is selectively inhibited by carbohydrate-binding agents but not by polyanions
    Claire Bertaux
    Department of Microbiology and Immunology, Albert Einstein College of Medicine, Bronx, New York, USA
    Virology 366:40-50. 2007
    ..They may represent an attractive new option for therapy of HCV/HIV coinfections. CBAs may also have the potential to prevent HCV/HIV transmission...
  22. pmc Automatic and quantitative measurement of protein-protein colocalization in live cells
    Sylvain V Costes
    Image Analysis Laboratory, National Cancer Institute, Frederick, Maryland, USA
    Biophys J 86:3993-4003. 2004
    ..25 x 10(-3) s(-1). More generally, this algorithm can be used to answer a variety of biological questions involving protein-protein interactions or co-compartmentalization and can be generalized to colocalization of more than two colors...
  23. ncbi In vivo HIV-1 Rev multimerization in the nucleolus and cytoplasm identified by fluorescence resonance energy transfer
    Dirk Daelemans
    Human Retrovirus Section, Basic Research Laboratory and Image Analysis Laboratory, Science Application International Corporation, NCI Frederick, Frederick, Maryland 21702 1201, USA
    J Biol Chem 279:50167-75. 2004
    ..Our results show that Rev multimerizes in the nucleolus of living cells, suggesting an important role of the nucleolus in nucleocytoplasmic transport...
  24. doi Structure-activity relationship study on anti-HIV 6-desfluoroquinolones
    Oriana Tabarrini
    Dipartimento di Chimica e Tecnologia del Farmaco, Universita di Perugia, Via del Liceo 1, 06123 Perugia, Italy
    J Med Chem 51:5454-8. 2008
    ..We demonstrate here that highly potent molecules can be obtained by optimizing the substituent in the various positions of the quinolone nucleus...