Zobrazeno 1 - 10
of 35
pro vyhledávání: '"James P, Rizzi"'
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
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
Autor:
Paul Yell, Farrah Homayoun, Xiankai Sun, Ivan Pedrosa, Naseem J. Zojwalla, Tae Hyun Hwang, Andrea Pavia-Jimenez, Wallace Eli M, Tai Wong, Wenfang Chen, Allison Joyce, Nirav V. Patel, Renée M. McKay, Xian Jin Xie, James Brugarolas, Kevin D. Courtney, James P. Rizzi, Payal Kapur, Kevin H. Gardner, Eboni Holloman, Haley Hill, Min Kim, Richard K. Bruick, John A. Josey, Alana Christie, Jenny Chang, He Zhang, Eugene P. Frenkel, Yuanqing Ma, Heather Geiger, Guiyang Hao, Yang Xie, Qurratulain Yousuf, Catherine Reeves
Publikováno v:
Nature. 539:112-117
Clear cell renal cell carcinoma (ccRCC) is characterized by inactivation of the von Hippel-Lindau tumour suppressor gene (VHL). Because no other gene is mutated as frequently in ccRCC and VHL mutations are truncal, VHL inactivation is regarded as the
Autor:
Mark C. Munson, Dale Wright, Sanchari Bhattacharyya, Kith Pradhan, Ioannis Mantzaris, Nandini Ramachandra, Yiting Yu, David Chantry, Jennifer Garrus, Aditi Shastri, Ulrich Steidl, Grant Hogeland, Lance Wollenberg, Chandan Guha, Shanisha Gordon-Mitchell, Matthias Bartenstein, Vineeth Sukrithan, Lohith S. Bachegowda, George Nwankwo, Andrea Pellagatti, Amer Assal, Mareli Rodriguez, Tushar D. Bhagat, Shannon L. Winski, Suzy Brown, Orsolya Giricz, Yiyu Zou, Carolina Schinke, Amit Verma, Kerry Morrone, Jacqueline Boultwood, James P. Rizzi, Stefan Gross, Leonidas C. Platanias, Samira Shahnaz, Laurence E. Burgess
Publikováno v:
Cancer Research. 76:4841-4849
Myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML) suppress normal hematopoietic activity in part by enabling a pathogenic inflammatory milieu in the bone marrow. In this report, we show that elevation of angiopoietin-1 in myelodysplast
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
Autor:
Xinlin Du, James P. Rizzi, Sabina Signoretti, Wallace Eli M, William G. Kaelin, Abhishek A. Chakraborty, Hyejin Cho, Ella Liberzon, Ingrid Carvo, John A. Josey, Richard K. Bruick, Wenhua Gao
The transcription factor HIF-2, an important driver of clear cell renal cell carcinoma, has been called 'undruggable'. However, in this issue of Nature, two groups report on the development and testing of a novel HIF-2 inhibitor, termed PT2399. Willi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02b8909a9504bb5bb7d98176ebe6b984
https://europepmc.org/articles/PMC5499381/
https://europepmc.org/articles/PMC5499381/
Autor:
Melissa A. Maddie, Rui Xu, Guangzhou Han, Paul M. Wehn, Sarah R. Olive, Huiling Tan, Eli M. Wallace, Zhaodan Cao, Keshi Wang, Bin Wang, Megan M. Halfmann, Jonas Grina, Robert M. Czerwinski, Barry Goggin, Tzuling Cheng, Darryl D. Dixon, Hanbiao Yang, Stephen T. Schlachter, Xinlin Du, John A. Josey, Shanhai Xie, James P. Rizzi
Publikováno v:
Cancer research. 76(18)
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