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Data 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

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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Discovery of sterically-hindered phenol compounds with potent cytoprotective activities against ox-LDL–induced retinal pigment epithelial cell death as a potential pharmacotherapy

Autor: Franco Aparecido Rossato, Eun Young Choi, Andrew J. Urquhart, David A. Scott, Yin Shan E. Ng, Gopalan Gnanaguru, Ashley Mackey, Anthoula Arta, Patricia A. D'Amore, Thomas W. Gero

Publikováno v: Free Radic Biol Med

Late-stage dry age-related macular degeneration (AMD) or geographic atrophy (GA) is an irreversible blinding condition characterized by degeneration of retinal pigment epithelium (RPE) and the associated photoreceptors. Clinical and genetic evidence

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::691e14ee0f6eb5eaca0221237af4d0e9
https://doi.org/10.1016/j.freeradbiomed.2021.11.026

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Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC

Autor: Thomas W. Gero, David E. Heppner, Tyler S. Beyett, Ciric To, Seth C. Azevedo, Jaebong Jang, Thomas Bunnell, Frederic Feru, Zhengnian Li, Bo Hee Shin, Kara M. Soroko, Prafulla C. Gokhale, Nathanael S. Gray, Pasi A. Jänne, Michael J. Eck, David A. Scott

Publikováno v: Bioorganicmedicinal chemistry letters. 68

The C797S mutation confers resistance to covalent EGFR inhibitors used in the treatment of lung tumors with the activating L858R mutation. Isoindolinones such as JBJ-4-125-02 bind in an allosteric pocket and are active against this mutation, with hig

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f1bfb1415ffe44876f18b0e35b149a21
https://pubmed.ncbi.nlm.nih.gov/35378251

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A photoredox catalysed Heck reaction

Autor: Marta, Rosenthal, Jörg K N, Lindner, Uwe, Gerstmann, Armin, Meier, W Gero, Schmidt, René, Wilhelm

Publikováno v: RSC advances. 10(70)

The attachment of homoleptic Ru bis-terpy complexes on graphene oxide significantly improved the photocatalytic activity of the complexes. These straightforward complexes were applied as photocatalysts in a Heck reaction. Due to covalent functionaliz

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::13abd6b256a0ddaccf07f29a53463496
https://pubmed.ncbi.nlm.nih.gov/35514879

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Discovery of a series of benzopyrimidodiazepinone TNK2 inhibitors via scaffold morphing

Autor: Thomas W. Gero, John Thomas Feutrill, Bailing Chen, Nathanael S. Gray, Feru Frederic, Brian J. Groendyke, Hilary Szabo, Zhengnian Li, Bin Li, David A. Scott, Chelsea E. Powell

Publikováno v: Bioorganicmedicinal chemistry letters. 30(19)

The protein kinase TNK2 (ACK1) is an emerging drug target for a variety of indications, in particular for cancer where it plays a key role transmitting cell survival, growth and proliferative signals via modification of multiple downstream effectors

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::220bb5eba35eecf2c507de3c0f2c8533
https://pubmed.ncbi.nlm.nih.gov/32739400

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