Výsledky vyhledávání - "Dries J.H. De Clercq"

Table S2 from Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

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

KINOMEscan selectivity profiling of JBJ-04-125-02 and IC50 of EAI045, JBJ-02-112-05 and JBJ-04-125-02 in BaF3 cells.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e81530eeb21ecfab480815cc6e91ed2
https://doi.org/10.1158/2159-8290.22532728

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Figure S1 from Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

JBJ-04-125-02 is more potent than EAI045 and JBJ-02-112-05 in the presence of cetuximab and is effective in inhibiting EGFR-dependent proliferation and phosphorylation in L858R/ C797S Ba/F3 cells.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0047199fa8a3c461d280306081cb4878
https://doi.org/10.1158/2159-8290.22532749.v1

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Figure S5 from Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

The combination treatment of JBJ-04-125-02 and osimertinib do not result in any toxicity issues associated with weight loss but osimertinib at clinically relevant dose (25 mg/kg) is too potent to exhibit additive effect when combined with JBJ-04-125-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4832fc287da782a8c6fe272ef963e362
https://doi.org/10.1158/2159-8290.22532737

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Figure S2 from Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

JBJ-04-125-02 as a single agent does not result in any toxicity issues associated with weight loss.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7602590529859e8029dcf364248b3e30
https://doi.org/10.1158/2159-8290.22532746

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Data from Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

Allosteric kinase inhibitors offer a potentially complementary therapeutic strategy to ATP-competitive kinase inhibitors due to their distinct sites of target binding. In this study, we identify and study a mutant-selective EGFR allosteric inhibitor,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::67a91c6e4372be275b6fa33231d73e76
https://doi.org/10.1158/2159-8290.c.6546814.v1

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Supplemental Methods from Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

Supplemental methods for structural modeling of inhibitor binding, pharmacokinetic assays, in vivo studies, crosslinking and biotinylated drug pull-down assays.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::11fec344ee662167eb1f937a273d678d
https://doi.org/10.1158/2159-8290.22532734.v1

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Table S1 from Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

Crystallographic data collection and refinement statistics.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3bd0b7a4aa6c7dbdcfa28b14ae4f5849
https://doi.org/10.1158/2159-8290.22532731.v1

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Figure S4 from Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

Not all tyrosine kinase inhibitors (TKIs) can enhance or bind at the same time as an allosteric inhibitor (AI) and co-binding of TKIs and AIs do not necessarily translate into increased drug potency.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1b311ce1f5f035c647848181f0199478
https://doi.org/10.1158/2159-8290.22532740.v1

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Figure S3 from Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

The relative allelic fraction of T790M does not change the potency of JBJ-04-125-02 in H3255 cells but the presence of EGF blunts the efficacy of JBJ-04-125-02 in Ba/F3 and H1975 cells.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a0e13e974ba2c6df71ae8a62c4d523f7
https://doi.org/10.1158/2159-8290.22532743

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