Search filters

List of works by Dirk Daelemans

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

scientific article published on September 2002

5-Hydroxypyrido[2,3- b ]pyrazin-6(5 H )-one derivatives as novel dual inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H and integrase

article

A 1,8-naphthyridone derivative targets the HIV-1 Tat-mediated transcription and potently inhibits the HIV-1 replication

scientific article

A novel and efficient approach to discriminate between pre- and post-transcription HIV inhibitors

scientific article published on 23 February 2005

A phenyl-thiadiazolylidene-amine derivative ejects zinc from retroviral nucleocapsid zinc fingers and inactivates HIV virions ⬇️

scientific article published on November 12, 2012

A stably expressed llama single-domain intrabody targeting Rev displays broad-spectrum anti-HIV activity

scientific article

A synthetic HIV-1 Rev inhibitor interfering with the CRM1-mediated nuclear export

scientific article

A time-of-drug addition approach to target identification of antiviral compounds

scientific article published on 2 June 2011

Abstract 2442: XPO1 is selinexor prime target: validation by mutating cysteine 528 on both XPO1 alleles using CRISPR/Cas9 genome editing

Abstract LB-210: KPT-8602 is a second-generation XPO1 inhibitor with improvedin vivotolerability that demonstrates potent acute lymphoblastic leukemia activity

An Intrabody based on a Llama Single-domain Antibody Targeting the N-terminal α-Helical Multimerization Domain of HIV-1 Rev Inhibits Viral Replication

article

An intrabody based on a llama single-domain antibody targeting the N-terminal alpha-helical multimerization domain of HIV-1 rev prevents viral production.

scientific article

Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action

scientific article published on 6 April 2015

Anti-HIV-1 activity of the G-quadruplex ligand BRACO-19.

scientific article published on 6 August 2014

Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach

scientific article published on 21 July 2016

Arylazolyl(azinyl)thioacetanilides: Part 19: Discovery of Novel Substituted Imidazo[4,5-b]pyridin-2-ylthioacetanilides as Potent HIV NNRTIs Via a Structure-based Bioisosterism Approach

article

Automatic and quantitative measurement of protein-protein colocalization in live cells.

scientific article

Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer's Disease

scientific article published on 19 March 2020

C9orf72-generated poly-GR and poly-PR do not directly interfere with nucleocytoplasmic transport

scientific article published on 31 October 2019

CXCR4 Antagonists: A New Generation of Configurationally Restricted Bis-azamacrocyclic Compounds

scientific article published in 2009

CXCR4 Chemokine Receptor Antagonists from Ultra-rigid Metal Complexes Profoundly Inhibit HIV-1 Replication, and also AMD3100-resistant Strains

article

CXCR4 chemokine receptor antagonists: nickel(II) complexes of configurationally restricted macrocycles

scientific article published on 14 August 2012

Capture and transmission of HIV-1 by the C-type lectin L-SIGN (DC-SIGNR) is inhibited by carbohydrate-binding agents and polyanions

scientific article

Cell type-dependent effect of sodium valproate on human immunodeficiency virus type 1 replication in vitro.

scientific article published on January 1997

Cellular Stress Induces Nucleocytoplasmic Transport Deficits Independent of Stress Granules

scientific article published on 03 May 2022

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

scientific article published on 7 February 2007

Comparative study of the organisation and phenotypes of bladder interstitial cells in human, mouse and rat.

scientific article

Computational investigation of the HIV-1 Rev multimerization using molecular dynamics simulations and binding free energy calculations

scientific article published on 23 March 2012

Debio-025 inhibits HIV-1 by interfering with an early event in the replication cycle

scientific article published on 24 October 2009

Deletion of the transient receptor potential cation channel TRPV4 impairs murine bladder voiding

scientific article

Design and Synthesis of New 6-Nitro and 6-Amino-3,3a,4,5-Tetrahydro-2H-Benzo[g]indazole Derivatives: Antiproliferative and Antibacterial Activity

scientific article published on 21 November 2019

Design, Synthesis, and Biological Evaluation of Novel 2-(Pyridin-3-yloxy)acetamide Derivatives as Potential Anti-HIV-1 Agents

scientific article published on 8 September 2015

Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles

scientific article published on 19 August 2016

Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs

scientific article

Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket

scientific article published on 22 December 2015

Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs

scientific article published on 30 December 2018

Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket

scientific article

Design, synthesis, and antiviral evaluation of novel hydrazone-substituted thiophene[3,2-d]pyrimidine derivatives as potent human immunodeficiency virus-1 inhibitors

scientific article published on 26 August 2018

Design, synthesis, and biological evaluation of novel 5-Alkyl-6-Adamantylmethylpyrimidin-4(3H)-ones as HIV-1 non-nucleoside reverse-transcriptase inhibitors

scientific article published on 09 April 2016

Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site

scientific article published on 27 February 2018

Discovery of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the Tolerant Region I of NNIBP.

scientific article published on 19 October 2017

Discovery of novel DAPY-IAS hybrid derivatives as potential HIV-1 inhibitors using molecular hybridization based on crystallographic overlays

scientific article

Discovery of novel diarylpyrimidines as potent HIV-1 NNRTIs by investigating the chemical space of a less explored "hydrophobic channel".

scientific article

Discovery of novel piperidine-substituted indolylarylsulfones as potent HIV NNRTIs via structure-guided scaffold morphing and fragment rearrangement

scientific article published on 05 October 2016

Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors

scientific article published on 27 April 2015

Discovery of potent HIV-1 non-nucleoside reverse transcriptase inhibitors by exploring the structure-activity relationship of solvent-exposed regions I

article

Discovery of potential dual-target prodrugs of HIV-1 reverse transcriptase and nucleocapsid protein 7

scientific article published on 26 May 2020

Down-regulation of AR splice variants through XPO1 suppression contributes to the inhibition of prostate cancer progression

scientific article published on 19 October 2018

Dynamics of the ternary complex formed by c-Myc interactor JPO2, transcriptional co-activator LEDGF/p75, and chromatin

scientific article

Entry of hepatitis C virus and human immunodeficiency virus is selectively inhibited by carbohydrate-binding agents but not by polyanions

scientific article

Exploiting the Tolerant Region I of the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) Binding Pocket: Discovery of Potent Diarylpyrimidine-Typed HIV-1 NNRTIs against Wild-Type and E138K Mutant Virus with Significantly Improved Water Solubili

scientific article published on 5 February 2019

Exploiting the anti-HIV 6-desfluoroquinolones to design multiple ligands.

scientific article published on 22 July 2014

First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain

scientific article published on 5 March 2018

Fluorescence-based antiviral assay for the evaluation of compounds against vaccinia virus, varicella zoster virus and human cytomegalovirus

scientific article

Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery

scientific article published in March 2018

HIV-1 Rev multimerization: mechanism and insights.

scientific article published on December 2013

Hemozoin induces lung inflammation and correlates with malaria-associated acute respiratory distress syndrome.

scientific article

Heterozygous mutation of cysteine528 in XPO1 is sufficient for resistance to selective inhibitors of nuclear export

scientific article published on 13 September 2016

Human Exportin-1 is a Target for Combined Therapy of HIV and AIDS Related Lymphoma

scientific article

Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors

scientific article published on 27 June 2015

Identification of different phenotypes of interstitial cells in the upper and deep lamina propria of the human bladder dome

scientific article published on 2 June 2014

Identification of the Type of Cells Responsible for Transfer of Herpes Simplex Virus (HSV) and Vaccinia Virus (VACV) Infection to Epithelial Cells Grown in 3D

scientific article published in 2009

Identifying drug-target selectivity of small-molecule CRM1/XPO1 inhibitors by CRISPR/Cas9 genome editing

scientific article published on 8 January 2015

In vivo HIV-1 Rev multimerization in the nucleolus and cytoplasm identified by fluorescence resonance energy transfer

scientific article published on 3 August 2004

Inhibition of HIV-1 replication by a bis-thiadiazolbenzene-1,2-diamine that chelates zinc ions from retroviral nucleocapsid zinc fingers

scientific article

Inhibition of the CRM1-mediated nucleocytoplasmic transport by N-azolylacrylates: structure-activity relationship and mechanism of action

scientific article published on 20 September 2008

Intracytoplasmic trapping of influenza virus by a lipophilic derivative of aglycoristocetin.

scientific article

Iron/Copper Co-Catalyzed Cross-Coupling Reaction for the Synthesis of 6-Substituted 7-Deazapurines and the Corresponding Nucleosides

scientific article published on 20 December 2019

Kinetic and molecular analysis of nuclear export factor CRM1 association with its cargo in vivo

scientific article

L-Aspartic and l-glutamic acid ester-based ProTides of anticancer nucleosides: Synthesis and antitumoral evaluation

scientific article published on 22 March 2016

Mapping the binding interface between an HIV-1 inhibiting intrabody and the viral protein Rev

scientific article

Measuring cooperative Rev protein-protein interactions on Rev responsive RNA by fluorescence resonance energy transfer

scientific article

Mechanistic Studies on a Novel Hydrophobic Derivative of Aglycoristocetin with Potent and Broad Activity Against Influenza Viruses

article published in 2011

Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors

scientific article published on 3 May 2013

Mouse adenovirus type 1 attachment is not mediated by the coxsackie-adenovirus receptor.

scientific article published on 21 June 2006

Near-native, site-specific and purification-free protein labeling for quantitative protein interaction analysis by MicroScale Thermophoresis.

scientific article published on 21 March 2018

Optical coherence tomography visualizes microstructure of apple peel

article by Pieter Verboven et al published April 2013 in Postharvest Biology and Technology

Phase Separation of C9orf72 Dipeptide Repeats Perturbs Stress Granule Dynamics ⬇️

scientific article published on March 2017

Pradimicin A, a carbohydrate-binding nonpeptidic lead compound for treatment of infections with viruses with highly glycosylated envelopes, such as human immunodeficiency virus

scientific article published on 18 October 2006

Preclinical Assessment with Clinical Validation of Selinexor with Gemcitabine and Nab-Paclitaxel for the Treatment of Pancreatic Ductal Adenocarcinoma

scientific article published on 12 December 2019

Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue

scientific article published on 7 August 2015

Quantitative Nucleocytoplasmic Transport Assays in Cellular Models of Neurodegeneration

publication published on 20 June 2020

Role of PFKFB3-driven glycolysis in vessel sprouting

scientific article

S-adenosylhomocysteine hydrolase inhibitors interfere with the replication of human immunodeficiency virus type 1 through inhibition of the LTR transactivation.

scientific article published in December 1997

STK38 kinase acts as XPO1 gatekeeper regulating the nuclear export of autophagy proteins and other cargoes

scientific article published on 23 September 2019

Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs

scientific article

Selective inhibition of Human Immunodeficiency Virus type 1 (HIV-1) by a novel family of tricyclic nucleosides

scientific article published on 12 May 2011

Selective inhibitors of nuclear export show that CRM1/XPO1 is a target in chronic lymphocytic leukemia ⬇️

scientific article published on October 3, 2012

Some hydrazones of 2-aroylamino-3-methylbutanohydrazide: synthesis, molecular modeling studies, and identification as stereoselective inhibitors of HIV-1.

scientific article

Stereospecificity of 6'-C-Neplanocin A Analogues as Inhibitors of S-Adenosylhomocysteine Hydrolase Activity and Human Immunodeficiency Virus Replication

Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket

scientific article published on 25 May 2016

Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants

scientific article published on 8 May 2017

Structure-activity relationship study on anti-HIV 6-desfluoroquinolones

scientific article published on 19 August 2008

Studies of anti-HIV transcription inhibitor quinolones: identification of potent N1-vinyl derivatives

scientific article published on November 2010

Studies on anti-HIV quinolones: New insights on the C-6 position

article

Synthesis and Biological Evaluation of Pyrrolo[2,1-f][1,2,4]triazine C-Nucleosides with a Ribose, 2'-Deoxyribose, and 2',3'-Dideoxyribose Sugar Moiety

scientific article published on 21 November 2017

Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase

scientific article published on 27 November 2014

Synthesis and biological evaluation of new conformationally restricted S-DABO hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase

article

Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors ⬇️

scientific article published on October 29, 2012

Target identification of small molecules using large-scale CRISPR-Cas mutagenesis scanning of essential genes

scientific article

Targeting the XPO1-dependent nuclear export of E2F7 reverses anthracycline resistance in head and neck squamous cell carcinomas

scientific article published on 01 June 2018

Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.

scientific article published on 23 March 2018

Tetrazolium-based colorimetric assay for the detection of HIV replication inhibitors: revisited 20 years later

scientific article

The Oxygen Sensor PHD2 Controls Dendritic Spines and Synapses via Modification of Filamin A

scientific article published on 8 March 2016

The Second-Generation Exportin-1 Inhibitor KPT-8602 Demonstrates Potent Activity against Acute Lymphoblastic Leukemia.

scientific article

The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2

scholarly article by Xueyi Lu published in May 2018

The nucleotide analog cidofovir suppresses basic fibroblast growth factor (FGF2) expression and signaling and induces apoptosis in FGF2-overexpressing endothelial cells

scientific article

The stem cell growth factor receptor KIT is not expressed on interstitial cells in bladder

scientific article

To disinfect or not to disinfect in postharvest research on the fungal decay of apple?

scientific article published on 6 December 2017

Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies

scientific article published on 30 August 2013

Understanding the molecular mechanism of host-based statin resistance in hepatitis C virus replicon containing cells

scientific article published on 9 June 2015

XPO1-dependent nuclear export is a druggable vulnerability in KRAS-mutant lung cancer.

scientific article published on 28 September 2016

Xylo-C-nucleosides with a pyrrolo[2,1-f][1,2,4]triazin-4-amine heterocyclic base: Synthesis and antiproliferative properties

scientific article published on 15 April 2019

Paulina is supported by:

About Paulina

Help