Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Thomas W. Gero"'
Autor:
Tyler Beyett, Ciric To, David E. Heppner, Thomas W. Gero, Nathanael S. Gray, David A. Scott, Pasi A. Jänne, Michael J. Eck
Publikováno v:
ASPET 2023 Annual Meeting Abstract - Drug Discovery and Development.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::99cd61c0f8e38d70ed2efc2910f3fff1
https://doi.org/10.1124/jpet.122.162040
https://doi.org/10.1124/jpet.122.162040
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
https://doi.org/10.1158/2159-8290.22532728
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
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
https://doi.org/10.1158/2159-8290.22532749.v1
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
https://doi.org/10.1158/2159-8290.c.6546814.v1
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
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
https://doi.org/10.1158/2159-8290.22532734.v1
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
https://doi.org/10.1016/j.freeradbiomed.2021.11.026
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
https://pubmed.ncbi.nlm.nih.gov/35378251
Autor:
Ciric To, Tyler S. Beyett, Jaebong Jang, William W. Feng, Magda Bahcall, Heidi M. Haikala, Bo H. Shin, David E. Heppner, Jaimin K. Rana, Brittaney A. Leeper, Kara M. Soroko, Michael J. Poitras, Prafulla C. Gokhale, Yoshihisa Kobayashi, Kamal Wahid, Kari J. Kurppa, Thomas W. Gero, Michael D. Cameron, Atsuko Ogino, Mierzhati Mushajiang, Chunxiao Xu, Yanxi Zhang, David A. Scott, Michael J. Eck, Nathanael S. Gray, Pasi A. Jänne
Publikováno v:
Nature cancer. 3(4)
Epidermal growth factor receptor (EGFR) therapy using small-molecule tyrosine kinase inhibitors (TKIs) is initially efficacious in patients with EGFR-mutant lung cancer, although drug resistance eventually develops. Allosteric EGFR inhibitors, which
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::975f0bd89dfda9f4a321a3cee14777cb
https://pubmed.ncbi.nlm.nih.gov/35484419
https://pubmed.ncbi.nlm.nih.gov/35484419
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
https://pubmed.ncbi.nlm.nih.gov/32739400
Autor:
Brian J. Groendyke, John Thomas Feutrill, Thomas W. Gero, Zhengnian Li, David A. Scott, Feru Frederic, Chelsea E. Powell, Hilary Szabo, Kevin Pang, Bailing Chen, Bin Li, Nathanael S. Gray
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(4)
The SAR of a series of benzopyrimidodiazepinone inhibitors of TNK2 was developed, starting from the potent and selective compound XMD8-87. A diverse set of anilines was introduced in an effort to improve the in vivo PK profile and minimize the risk o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::19fad4c04cad6c1f0bdde67bcc8337e5
https://pubmed.ncbi.nlm.nih.gov/31928839
https://pubmed.ncbi.nlm.nih.gov/31928839