Zobrazeno 1 - 10
of 32
pro vyhledávání: '"Kirk Robarge"'
Autor:
Frederic J. de Sauvage, Robert L. Yauch, Stephen E. Gould, Suzie J. Scales, Dan Sutherlin, Kirk Robarge, Richard Goldsmith, Dan Burdick, Zora Modrusan, Kristina West, Thomas Januario, Lasse Weinmann, Bruno Alicke, Gerrit J. P. Dijkgraaf
Inappropriate Hedgehog (Hh) signaling has been directly linked to medulloblastoma (MB), a common malignant brain tumor in children. GDC-0449 is an Hh pathway inhibitor (HPI) currently under clinical investigation as an anticancer agent. Treatment of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bd80db1f9d1b999661f6a494b03c5e21
https://doi.org/10.1158/0008-5472.c.6502772
https://doi.org/10.1158/0008-5472.c.6502772
Autor:
Frederic J. de Sauvage, Robert L. Yauch, Stephen E. Gould, Suzie J. Scales, Dan Sutherlin, Kirk Robarge, Richard Goldsmith, Dan Burdick, Zora Modrusan, Kristina West, Thomas Januario, Lasse Weinmann, Bruno Alicke, Gerrit J. P. Dijkgraaf
Supplementary Table 1 from Small Molecule Inhibition of GDC-0449 Refractory Smoothened Mutants and Downstream Mechanisms of Drug Resistance
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::756df7575425785d5cd447ebe4a28bd7
https://doi.org/10.1158/0008-5472.22389962
https://doi.org/10.1158/0008-5472.22389962
Autor:
Frederic J. de Sauvage, Robert L. Yauch, Stephen E. Gould, Suzie J. Scales, Dan Sutherlin, Kirk Robarge, Richard Goldsmith, Dan Burdick, Zora Modrusan, Kristina West, Thomas Januario, Lasse Weinmann, Bruno Alicke, Gerrit J. P. Dijkgraaf
Supplementary Figures 1-6 from Small Molecule Inhibition of GDC-0449 Refractory Smoothened Mutants and Downstream Mechanisms of Drug Resistance
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b05f5d20f7e4dd28d59546d16be17fef
https://doi.org/10.1158/0008-5472.22389968.v1
https://doi.org/10.1158/0008-5472.22389968.v1
Autor:
Frederic J. de Sauvage, Robert L. Yauch, Stephen E. Gould, Suzie J. Scales, Dan Sutherlin, Kirk Robarge, Richard Goldsmith, Dan Burdick, Zora Modrusan, Kristina West, Thomas Januario, Lasse Weinmann, Bruno Alicke, Gerrit J. P. Dijkgraaf
Supplementary Methods, Figure Legends 1-6 from Small Molecule Inhibition of GDC-0449 Refractory Smoothened Mutants and Downstream Mechanisms of Drug Resistance
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::088e879ff92888701d72858a98dc149d
https://doi.org/10.1158/0008-5472.22389965
https://doi.org/10.1158/0008-5472.22389965
Autor:
BinQing Wei, Kirk Robarge, Sharada S. Labadie, Jinhua Chen, Laura B. Corson, Antonio DiPasquale, Peter S. Dragovich, Charles Eigenbrot, Marie Evangelista, Benjamin P. Fauber, Anna Hitz, Rebecca Hong, Kwong Wah Lai, Wenfeng Liu, Shuguang Ma, Shiva Malek, Thomas O'Brien, Jodie Pang, David Peterson, Laurent Salphati, Deepak Sampath, Steven Sideris, Mark Ultsch, Zijin Xu, Ivana Yen, Dong Yu, Qin Yue, Aihe Zhou, Hans E. Purkey
Publikováno v:
Bioorganicmedicinal chemistry letters. 59
Structure-based design was utilized to optimize 6,6-diaryl substituted dihydropyrone and hydroxylactam to obtain inhibitors of lactate dehydrogenase (LDH) with low nanomolar biochemical and single-digit micromolar cellular potencies. Surprisingly the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0770db4a66cefb70bb9bee4bcf37ca52
https://pubmed.ncbi.nlm.nih.gov/35065235
https://pubmed.ncbi.nlm.nih.gov/35065235
Autor:
Charles Z. Ding, Laurent Salphati, Hans E. Purkey, HongXiu Ge, Qin Yue, Antonio G. DiPasquale, Charles Eigenbrot, Qunh Ho, Kwong Wah Lai, Thomas O'Brien, Sharada Labadie, Zhongguo Chen, David A. Peterson, Shiva Malek, Laura Corson, Wenfeng Liu, Mark Ultsch, Jinhua Chen, Anna Hitz, Yajing Liu, Kirk Robarge, Jodie Pang, Chiho Li, Peter S. Dragovich, Binqing Wei, Shuguang Ma, Huihui Zhang, Steve Sideris, Zhenting Gao, Marie Evangelista, Ivana Yen, Aihe Zhou, Benjamin Fauber
Publikováno v:
ACS Medicinal Chemistry Letters. 7:896-901
A series of trisubstituted hydroxylactams was identified as potent enzymatic and cellular inhibitors of human lactate dehydrogenase A. Utilizing structure-based design and physical property optimization, multiple inhibitors were discovered with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f0532bd0e9287d033f18781fd7cf755
https://doi.org/10.1021/acsmedchemlett.6b00190
https://doi.org/10.1021/acsmedchemlett.6b00190
Autor:
Gary Salmon, Harvey Wong, Maxine Norman, Adrian Barnard, Aihe Zhou, Julie Hawkins, Benjamin Fauber, Adam R. Johnson, Arunima Ganguli, Yuzhong Deng, Susan Summerhill, Kirk Robarge, Celine Eidenschenk, Wenjun Ouyang, Christine Everett, Jianhua Cao, Wei Tang, Hank La, Alberto Gobbi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:2907-2912
The nuclear receptor (NR) retinoic acid receptor-related orphan receptor gamma (RORγ, RORc, or NR1F3) is a promising target for the treatment of autoimmune diseases. RORc is a critical regulator in the production of the pro-inflammatory cytokine int
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fa9c3898f9ddd336ebaff802da33874c
https://doi.org/10.1016/j.bmcl.2015.05.055
https://doi.org/10.1016/j.bmcl.2015.05.055
Autor:
Binqing Wei, Erica VanderPorten, Mark Ultsch, Jason Boggs, Peter S. Dragovich, S. Sideris, Jinhua Chen, Huihui Zhang, Sharada Labadie, Qin Yue, Charles Z. Ding, Kirk Robarge, David Peterson, Shuguang Ma, Hans E. Purkey, Benjamin Fauber, HongXiu Ge, Aihe Zhou, Kwong Wah Lai, Qunh Ho, Shiva Malek, Xuying Zhang, Ivana Yen, Laura Corson, Charles Eigenbrot, Qing Xu, Laurent Salphati
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:75-82
Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enone using structure-based design strategies resulted in inhibitors with considerable improvement in biochemical potency against human lactate dehydrogenase A (LDHA). These potent
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::921f2e384863aba9482741802d507295
https://doi.org/10.1016/j.bmcl.2014.11.008
https://doi.org/10.1016/j.bmcl.2014.11.008
Autor:
Philip Stephen Jackson, Pascal Savy, Jodie Pang, Wendy Lee, April Yang, Mark Ultsch, Robert Heald, Jason Boggs, Edna F. Choo, Charles Eigenbrot, Xioaye Yang, Kirk Robarge, Matthew Baumgardner, Joanne Hewitt, Steve Price, Brenda Burton, Christian Wiesmann
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:4714-4723
Use of the tools of SBDD including crystallography led to the discovery of novel and potent 6,5 heterobicyclic MEKi's [J. Med. Chem.2012, 55, 4594]. The core change from a 5,6 heterobicycle to a 6,5 heterobicycle was driven by the desire for increase
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5a1ebaa13120fa34ee18794315152d4d
https://doi.org/10.1016/j.bmcl.2014.08.008
https://doi.org/10.1016/j.bmcl.2014.08.008
Autor:
Peter S. Dragovich, Benjamin P. Fauber, Jason Boggs, Jinhua Chen, Laura B. Corson, Charles Z. Ding, Charles Eigenbrot, HongXiu Ge, Anthony M. Giannetti, Thomas Hunsaker, Sharada Labadie, Chiho Li, Yichin Liu, Yingchun Liu, Shuguang Ma, Shiva Malek, David Peterson, Keith E. Pitts, Hans E. Purkey, Kirk Robarge, Laurent Salphati, Steve Sideris, Mark Ultsch, Erica VanderPorten, Jing Wang, BinQing Wei, Qing Xu, Ivana Yen, Qin Yue, Huihui Zhang, Xuying Zhang, Aihe Zhou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:3764-3771
A novel class of 3-hydroxy-2-mercaptocyclohex-2-enone-containing inhibitors of human lactate dehydrogenase (LDH) was identified through a high-throughput screening approach. Biochemical and surface plasmon resonance experiments performed with a scree
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4ed0191d5c5ad01b10f95a841198637
https://doi.org/10.1016/j.bmcl.2014.06.076
https://doi.org/10.1016/j.bmcl.2014.06.076