Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Xinlin Du"'
Autor:
Paul M. Wehn, Song Yang, Jonas A. Grina, James P. Rizzi, Stephen T. Schlachter, Bin Wang, Rui Xu, Hanbiao Yang, Xinlin Du, Guangzhou Han, Keshi Wang, Robert M. Czerwinski, Emily L. Ged, Heli Huang, Megan M. Halfmann, Melissa A. Maddie, Emily R. Morton, Sarah R. Olive, Huiling Tan, Shanhai Xie, John A. Josey, Eli M. Wallace
Pharmacokinetic properties of our first-generation HIF-2α antagonist PT2385, including modest solubility, resulted in a high recommended phase 2 dose (RP2D) of 800 mg BID and motivated the pursuit of novel scaffolds which could improve solubility an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::df873b27c3e83d093d39f5958023934e
https://doi.org/10.21203/rs.3.rs-2753648/v1
https://doi.org/10.21203/rs.3.rs-2753648/v1
Autor:
John A. Josey, Hanbiao Yang, Rui Xu, Shanhai Xie, Keshi Wang, Bin Wang, Huiling Tan, Stephen T. Schlachter, Sarah R. Olive, Melissa A. Maddie, Megan M. Halfmann, Jonas A. Grina, Barry S. Goggin, Darryl D. Dixon, Robert M. Czerwinski, Tzuling Cheng, Xinlin Du, Zhaodan Cao, Paul M. Wehn, Guangzhou Han, James P. Rizzi, Eli M. Wallace
Supplementary method includes detailed experimental procedure for the synthesis of PT2385. Supplementary Figures 1-7 - Lack of cytotoxicity of PT2385 in cultured 786-O and A498 cells (1); PT2385 pharmacokinetics in CD-1 mice (2); Inhibition of HIF-2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76ba58b87702663a6c4d7ea731902dd9
https://doi.org/10.1158/0008-5472.22411674.v1
https://doi.org/10.1158/0008-5472.22411674.v1
Autor:
John A. Josey, Hanbiao Yang, Rui Xu, Shanhai Xie, Keshi Wang, Bin Wang, Huiling Tan, Stephen T. Schlachter, Sarah R. Olive, Melissa A. Maddie, Megan M. Halfmann, Jonas A. Grina, Barry S. Goggin, Darryl D. Dixon, Robert M. Czerwinski, Tzuling Cheng, Xinlin Du, Zhaodan Cao, Paul M. Wehn, Guangzhou Han, James P. Rizzi, Eli M. Wallace
More than 90% of clear cell renal cell carcinomas (ccRCC) exhibit inactivation of the von Hippel–Lindau (pVHL) tumor suppressor, establishing it as the major underlying cause of this malignancy. pVHL inactivation results in stabilization of the hyp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1cb681633f0b5416aa695f9339844dfb
https://doi.org/10.1158/0008-5472.c.6508272.v1
https://doi.org/10.1158/0008-5472.c.6508272.v1
Autor:
James P. Rizzi, Xinlin Du, John A. Josey, Eli M. Wallace, Robert M. Czerwinski, Guangzhou Han, Rui Xu, Hanbiao Yang, Tai Wong, Shanhai Xie, Jonas Grina, Paul M. Wehn, Darryl D. Dixon, Stephen T. Schlachter, Emily L Ged, Keshi Wang, Heli Huang, Huiling Tan, Bin Wang
Publikováno v:
Journal of Medicinal Chemistry. 62:6876-6893
The hypoxia-inducible factor 2α (HIF-2α) is a key oncogenic driver in clear cell renal cell carcinoma (ccRCC). Our first HIF-2α inhibitor PT2385 demonstrated promising proof of concept clinical activity in heavily pretreated advanced ccRCC patient
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2b0ccbb708d114033b81f48d69ed5cb7
https://doi.org/10.1021/acs.jmedchem.9b00719
https://doi.org/10.1021/acs.jmedchem.9b00719
Autor:
Andrew S. Cowburn, Shanhai Xie, David Macías, Alexander J.T. Wood, Stephen Moore, Alexi Crosby, Xinlin Du, Wallace Eli M, Arlette Vassallo, Mark Southwood, Huiling Tan
Publikováno v:
The European Respiratory Journal
article-version (VoR) Version of Record
article-version (VoR) Version of Record
Pulmonary arterial hypertension (PAH) is a destructive disease of the pulmonary vasculature often leading to right heart failure and death. Current therapeutic intervention strategies only slow disease progression. The role of aberrant hypoxia-induci
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d32b00f5971d07524076e05a9913a5a2
http://europepmc.org/articles/PMC7930471
http://europepmc.org/articles/PMC7930471
Autor:
John A. Josey, Zhaodan Cao, Tai Wong, Megan M. Halfmann, Heli Huang, Barry Goggin, Robert M. Czerwinski, Hanbiao Yang, Paul M. Wehn, Bin Wang, Shanhai Xie, Sarah R. Olive, Huiling Tan, Eli M. Wallace, Darryl D. Dixon, Melissa A. Maddie, Xinlin Du, Rui Xu, Stephen T. Schlachter, James P. Rizzi, Emily L. Morton, Tzuling Cheng, Jonas Grina, Keshi Wang, Guangzhou Han
Publikováno v:
Journal of Medicinal Chemistry. 61:9691-9721
HIF-2α, a member of the HIF family of transcription factors, is a key oncogenic driver in cancers such as clear cell renal cell carcinoma (ccRCC). A signature feature of these cancers is the overaccumulation of HIF-2α protein, often by inactivation
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9bf4fbb16ea14332bdd9c2e58a806b92
https://doi.org/10.1021/acs.jmedchem.8b01196
https://doi.org/10.1021/acs.jmedchem.8b01196
Autor:
Rui Xu, Wallace Eli M, Paul Wehn, Jim Rizzi, Robert M. Czerwinski, Xinlin Du, Carlos Huerta, Emily R. Morton, Deepak Nijhawan, Oleg A. Volkov, Hui Ling Tan
E7820 and indisulam are two examples of aryl sulfonamides that recruit RBM39 to Rbx-Cul4-DDA1-DDB1-DCAF15 E3 ligase complex, leading to its ubiquitination and degradation by the proteasome. In order to understand their mechanism of action, we carried
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bbbfe8f46247b0a1e1401f631d681900
Autor:
Jim Rizzi, Robert M. Czerwinski, Xinlin Du, Hui Ling Tan, Emily R. Morton, Wallace Eli M, Carlos Huerta, Paul Wehn, Oleg A. Volkov, Deepak Nijhawan, Rui Xu
Publikováno v:
Structure (London, England : 1993). 27(11)
E7820 and indisulam are two examples of aryl sulfonamides that recruit RBM39 to Rbx-Cul4-DDA1-DDB1-DCAF15 E3 ligase complex, leading to its ubiquitination and degradation by the proteasome. To understand their mechanism of action, we performed kineti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e8be1827294dd2e1fee04195a35d55b5
https://pubmed.ncbi.nlm.nih.gov/31693911
https://pubmed.ncbi.nlm.nih.gov/31693911
Autor:
Paul M, Wehn, James P, Rizzi, Darryl D, Dixon, Jonas A, Grina, Stephen T, Schlachter, Bin, Wang, Rui, Xu, Hanbiao, Yang, Xinlin, Du, Guangzhou, Han, Keshi, Wang, Zhaodan, Cao, Tzuling, Cheng, Robert M, Czerwinski, Barry S, Goggin, Heli, Huang, Megan M, Halfmann, Melissa A, Maddie, Emily L, Morton, Sarah R, Olive, Huiling, Tan, Shanhai, Xie, Tai, Wong, John A, Josey, Eli M, Wallace
Publikováno v:
Journal of medicinal chemistry. 61(21)
HIF-2α, a member of the HIF family of transcription factors, is a key oncogenic driver in cancers such as clear cell renal cell carcinoma (ccRCC). A signature feature of these cancers is the overaccumulation of HIF-2α protein, often by inactivation
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::4a0d9ca94f8b248f10acd7cb52b365e8
https://pubmed.ncbi.nlm.nih.gov/30289716
https://pubmed.ncbi.nlm.nih.gov/30289716
Autor:
R. Max Wynn, Yang Li, Xinlin Du, Hong Zhang, Kosaku Uyeda, Bonnie C. Miller, Niang Huang, Qiang Ge
Publikováno v:
Journal of Biological Chemistry. 287:41914-41921
Carbohydrate response element-binding protein (ChREBP) is an insulin-independent, glucose-responsive transcription factor that is expressed at high levels in liver hepatocytes where it plays a critical role in converting excess carbohydrates to fat f
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::707bc527c9f0e516a7c18d4b9ff652f4
https://doi.org/10.1074/jbc.m112.418855
https://doi.org/10.1074/jbc.m112.418855