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30 results on '"De Clercq, Dries"'

5. Table S3 from Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

Author

To, Ciric, primary, Jang, Jaebong, primary, Chen, Ting, primary, Park, Eunyoung, primary, Mushajiang, Mierzhati, primary, De Clercq, Dries J.H., primary, Xu, Man, primary, Wang, Stephen, primary, Cameron, Michael D., primary, Heppner, David E., primary, Shin, Bo Hee, primary, Gero, Thomas W., primary, Yang, Annan, primary, Dahlberg, Suzanne E., primary, Wong, Kwok-Kin, primary, Eck, Michael J., primary, Gray, Nathanael S., primary, and Jänne, Pasi A., primary

Published
2023
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6. Figure S1 from Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

Author

To, Ciric, primary, Jang, Jaebong, primary, Chen, Ting, primary, Park, Eunyoung, primary, Mushajiang, Mierzhati, primary, De Clercq, Dries J.H., primary, Xu, Man, primary, Wang, Stephen, primary, Cameron, Michael D., primary, Heppner, David E., primary, Shin, Bo Hee, primary, Gero, Thomas W., primary, Yang, Annan, primary, Dahlberg, Suzanne E., primary, Wong, Kwok-Kin, primary, Eck, Michael J., primary, Gray, Nathanael S., primary, and Jänne, Pasi A., primary

Published
2023
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7. Data from Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

Author

To, Ciric, primary, Jang, Jaebong, primary, Chen, Ting, primary, Park, Eunyoung, primary, Mushajiang, Mierzhati, primary, De Clercq, Dries J.H., primary, Xu, Man, primary, Wang, Stephen, primary, Cameron, Michael D., primary, Heppner, David E., primary, Shin, Bo Hee, primary, Gero, Thomas W., primary, Yang, Annan, primary, Dahlberg, Suzanne E., primary, Wong, Kwok-Kin, primary, Eck, Michael J., primary, Gray, Nathanael S., primary, and Jänne, Pasi A., primary

Published
2023
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8. Supplemental Methods from Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

Author

To, Ciric, primary, Jang, Jaebong, primary, Chen, Ting, primary, Park, Eunyoung, primary, Mushajiang, Mierzhati, primary, De Clercq, Dries J.H., primary, Xu, Man, primary, Wang, Stephen, primary, Cameron, Michael D., primary, Heppner, David E., primary, Shin, Bo Hee, primary, Gero, Thomas W., primary, Yang, Annan, primary, Dahlberg, Suzanne E., primary, Wong, Kwok-Kin, primary, Eck, Michael J., primary, Gray, Nathanael S., primary, and Jänne, Pasi A., primary

Published
2023
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9. Abstract 53: Discovery of novel potent and orally bioavailable small-molecule inhibitors of ENPP1 to stabilize cGAMP and ATP in the tumor microenvironment and boost anti-tumor immunity

Author

Versele, Matthias, primary, del Pino Garcia, Javier, additional, Vandecaetsbeek, Ilse, additional, Castermans, Karolien, additional, Kellens, Ranie, additional, Haeck, Wanda, additional, Klaassen, Hugo, additional, Bourin, Arnaud, additional, De Clercq, Dries, additional, Allasia, Sara, additional, Boland, Sandro, additional, Marchand, Arnaud, additional, Chaltin, Patrick, additional, and Bollen, Mathieu, additional

Published
2021
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10. Thermal imaging and image processing

Author

De Clercq, Dries

Subjects
infrared thermography, image processing, Matlab, edge detection, gradient method
Abstract

The goal was to research the abilities of thermal imaging and image processing and look in the possibilities for non-destructive testing. The goal was to identify the holes in the specimen while the photos were taken from a side which the holes are not visible from. In this case the holes were supposed to be detected but it could also be cracks and/or other errors in the part. The gradient function is to look at the way the heat moves out of the part after it is heated.

Published
2020

11. Mutant‐Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug‐Resistant Mutations

Author

Jang, Jaebong, primary, To, Ciric, additional, De Clercq, Dries J. H., additional, Park, Eunyoung, additional, Ponthier, Charles M., additional, Shin, Bo Hee, additional, Mushajiang, Mierzhati, additional, Nowak, Radosław P., additional, Fischer, Eric S., additional, Eck, Michael J., additional, Jänne, Pasi A., additional, and Gray, Nathanael S., additional

Published
2020
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12. Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors

Author

De Clercq, Dries J. H., primary, Heppner, David E., additional, To, Ciric, additional, Jang, Jaebong, additional, Park, Eunyoung, additional, Yun, Cai-Hong, additional, Mushajiang, Mierzhati, additional, Shin, Bo Hee, additional, Gero, Thomas W., additional, Scott, David A., additional, Jänne, Pasi A., additional, Eck, Michael J., additional, and Gray, Nathanael S., additional

Published
2019
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13. Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

Author

To, Ciric, primary, Jang, Jaebong, additional, Chen, Ting, additional, Park, Eunyoung, additional, Mushajiang, Mierzhati, additional, De Clercq, Dries J.H., additional, Xu, Man, additional, Wang, Stephen, additional, Cameron, Michael D., additional, Heppner, David E., additional, Shin, Bo Hee, additional, Gero, Thomas W., additional, Yang, Annan, additional, Dahlberg, Suzanne E., additional, Wong, Kwok-Kin, additional, Eck, Michael J., additional, Gray, Nathanael S., additional, and Jänne, Pasi A., additional

Published
2019
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14. Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor

Author

Jang, Jaebong, primary, Son, Jieun, additional, Park, Eunyoung, additional, Kosaka, Takayuki, additional, Saxon, Jamie A., additional, De Clercq, Dries J. H., additional, Choi, Hwan Geun, additional, Tanizaki, Junko, additional, Eck, Michael J., additional, Jänne, Pasi A., additional, and Gray, Nathanael S., additional

Published
2018
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16. Proteome-scale Binary Interactomics in Human Cells

Author

Lievens, Sam, primary, Van der Heyden, José, additional, Masschaele, Delphine, additional, De Ceuninck, Leentje, additional, Petta, Ioanna, additional, Gupta, Surya, additional, De Puysseleyr, Veronic, additional, Vauthier, Virginie, additional, Lemmens, Irma, additional, De Clercq, Dries J.H., additional, Defever, Dieter, additional, Vanderroost, Nele, additional, De Smet, Anne-Sophie, additional, Eyckerman, Sven, additional, Van Calenbergh, Serge, additional, Martens, Lennart, additional, De Bosscher, Karolien, additional, Libert, Claude, additional, Hill, David E., additional, Vidal, Marc, additional, and Tavernier, Jan, additional

Published
2016
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28. Kinase Substrate Sensor (KISS), a Mammalian In SituProtein Interaction Sensor*

Author

Lievens, Sam, Gerlo, Sarah, Lemmens, Irma, De Clercq, Dries J.H., Risseeuw, Martijn D.P., Vanderroost, Nele, De Smet, Anne-Sophie, Ruyssinck, Elien, Chevet, Eric, Van Calenbergh, Serge, and Tavernier, Jan

Abstract

Probably every cellular process is governed by protein-protein interaction (PPIs), which are often highly dynamic in nature being modulated by in- or external stimuli. Here we present KISS, for KInase Substrate Sensor, a mammalian two-hybrid approach designed to map intracellular PPIs and some of the dynamic features they exhibit. Benchmarking experiments indicate that in terms of sensitivity and specificity KISS is on par with other binary protein interaction technologies while being complementary with regard to the subset of PPIs it is able to detect. We used KISS to evaluate interactions between different types of proteins, including transmembrane proteins, expressed at their native subcellular location. In situanalysis of endoplasmic reticulum stress-induced clustering of the endoplasmic reticulum stress sensor ERN1 and ligand-dependent β-arrestin recruitment to GPCRs illustrated the method's potential to study functional PPI modulation in complex cellular processes. Exploring its use as a tool for in cell evaluation of pharmacological interference with PPIs, we showed that reported effects of known GPCR antagonists and PPI inhibitors are properly recapitulated. In a three-hybrid setup, KISS was able to map interactions between small molecules and proteins. Taken together, we established KISS as a sensitive approach for in situanalysis of protein interactions and their modulation in a changing cellular context or in response to pharmacological challenges.

Published
2014
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29. Mutant-Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug-Resistant Mutations.

Author

Jang J, To C, De Clercq DJH, Park E, Ponthier CM, Shin BH, Mushajiang M, Nowak RP, Fischer ES, Eck MJ, Jänne PA, and Gray NS

Subjects
Allosteric Regulation, Cell Line, Tumor, ErbB Receptors antagonists & inhibitors, ErbB Receptors genetics, ErbB Receptors metabolism, Humans, Proteolysis, Drug Resistance, Neoplasm drug effects, Mutation, Protein Kinase Inhibitors pharmacology
Abstract

Targeting epidermal growth factor receptor (EGFR) through an allosteric mechanism provides a potential therapeutic strategy to overcome drug-resistant EGFR mutations that emerge within the ATP binding site. Here, we develop an allosteric EGFR degrader, DDC-01-163, which can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells while leaving wildtype EGFR Ba/F3 cells unaffected. DDC-01-163 is also effective against osimertinib-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. When combined with an ATP-site EGFR inhibitor, osimertinib, the anti-proliferative activity of DDC-01-163 against L858R/T790M EGFR-Ba/F3 cells is enhanced. Collectively, DDC-01-163 is a promising allosteric EGFR degrader with selective activity against various clinically relevant EGFR mutants as a single agent and when combined with an ATP-site inhibitor. Our data suggests that targeted protein degradation is a promising drug development approach for mutant EGFR., (© 2020 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Published
2020
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30. Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor.

Author

Jang J, Son J, Park E, Kosaka T, Saxon JA, De Clercq DJH, Choi HG, Tanizaki J, Eck MJ, Jänne PA, and Gray NS

Subjects
Cell Line, Tumor, Cell Proliferation drug effects, ErbB Receptors antagonists & inhibitors, ErbB Receptors chemistry, ErbB Receptors genetics, Exons, Humans, Lung Neoplasms drug therapy, Lung Neoplasms genetics, Molecular Docking Simulation, Mutation, Receptor, ErbB-2 chemistry, Receptor, ErbB-2 genetics, Fluorobenzenes chemistry, Fluorobenzenes pharmacology, Protein Kinase Inhibitors chemistry, Protein Kinase Inhibitors pharmacology, Receptor, ErbB-2 antagonists & inhibitors
Abstract

Exon 20 insertion (Ex20Ins) mutations are the third most prevalent epidermal growth factor receptor (EGFR) activating mutation and the most prevalent HER2 mutation in non-small cell lung cancer (NSCLC). Novel therapeutics for the patients with Ex20Ins mutations are urgently needed, due to their poor responses to the currently approved EGFR and HER2 inhibitors. Here we report the discovery of highly potent and broadly effective EGFR and HER2 Ex20Ins mutant inhibitors. The co-crystal structure of compound 1 b in complex with wild type EGFR clearly revealed an additional hydrophobic interaction of 4-fluorobenzene ring within a deep hydrophobic pocket, which has not been widely exploited in the development of EGFR and HER2 inhibitors. As compared with afatinib, compound 1 a exhibited superior inhibition of proliferation and signaling pathways in Ba/F3 cells harboring either EGFR or HER2 Ex20Ins mutations, and in the EGFR P772_H773insPNP patient-derived lung cancer cell line DFCI127. Our study identifies promising strategies for development of EGFR and HER2 Ex20Ins mutant inhibitors., (© 2018 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Published
2018
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