On-target efficacy of a HIF-2α antagonist in preclinical kidney cancer models
Cho, Hyejin, Du, Xinlin, Rizzi, James P., Liberzon, Ella, Chakraborty, Abhishek A., Gao, Wenhua, Carvo, Ingrid, Signoretti, Sabina, Bruick, Richard K., Josey, John A., Wallace, Eli M., Kaelin, William G.
Published in Nature (London) (03.11.2016)
Published in Nature (London) (03.11.2016)
Get full text
Journal Article
Targeting renal cell carcinoma with a HIF-2 antagonist
Chen, Wenfang, Hill, Haley, Christie, Alana, Kim, Min Soo, Holloman, Eboni, Pavia-Jimenez, Andrea, Homayoun, Farrah, Ma, Yuanqing, Patel, Nirav, Yell, Paul, Hao, Guiyang, Yousuf, Qurratulain, Joyce, Allison, Pedrosa, Ivan, Geiger, Heather, Zhang, He, Chang, Jenny, Gardner, Kevin H., Bruick, Richard K., Reeves, Catherine, Hwang, Tae Hyun, Courtney, Kevin, Frenkel, Eugene, Sun, Xiankai, Zojwalla, Naseem, Wong, Tai, Rizzi, James P., Wallace, Eli M., Josey, John A., Xie, Yang, Xie, Xian-Jin, Kapur, Payal, McKay, Renée M., Brugarolas, James
Published in Nature (London) (03.11.2016)
Published in Nature (London) (03.11.2016)
Get full text
Journal Article
3‑[(1S,2S,3R)‑2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma
Xu, Rui, Wang, Keshi, Rizzi, James P, Huang, Heli, Grina, Jonas A, Schlachter, Stephen T, Wang, Bin, Wehn, Paul M, Yang, Hanbiao, Dixon, Darryl D, Czerwinski, Robert M, Du, Xinlin, Ged, Emily L, Han, Guangzhou, Tan, Huiling, Wong, Tai, Xie, Shanhai, Josey, John A, Wallace, Eli M
Published in Journal of medicinal chemistry (08.08.2019)
Published in Journal of medicinal chemistry (08.08.2019)
Get full text
Journal Article
A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma
Wallace, Eli M, Rizzi, James P, Han, Guangzhou, Wehn, Paul M, Cao, Zhaodan, Du, Xinlin, Cheng, Tzuling, Czerwinski, Robert M, Dixon, Darryl D, Goggin, Barry S, Grina, Jonas A, Halfmann, Megan M, Maddie, Melissa A, Olive, Sarah R, Schlachter, Stephen T, Tan, Huiling, Wang, Bin, Wang, Keshi, Xie, Shanhai, Xu, Rui, Yang, Hanbiao, Josey, John A
Published in Cancer research (Chicago, Ill.) (15.09.2016)
Published in Cancer research (Chicago, Ill.) (15.09.2016)
Get full text
Journal Article
Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)
Wehn, Paul M, Rizzi, James P, Dixon, Darryl D, Grina, Jonas A, Schlachter, Stephen T, Wang, Bin, Xu, Rui, Yang, Hanbiao, Du, Xinlin, Han, Guangzhou, Wang, Keshi, Cao, Zhaodan, Cheng, Tzuling, Czerwinski, Robert M, Goggin, Barry S, Huang, Heli, Halfmann, Megan M, Maddie, Melissa A, Morton, Emily L, Olive, Sarah R, Tan, Huiling, Xie, Shanhai, Wong, Tai, Josey, John A, Wallace, Eli M
Published in Journal of medicinal chemistry (08.11.2018)
Published in Journal of medicinal chemistry (08.11.2018)
Get full text
Journal Article
Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (S)‑3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro‑1H‑inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)
Wehn, Paul M, Rizzi, James P, Dixon, Darryl D, Grina, Jonas A, Schlachter, Stephen T, Wang, Bin, Xu, Rui, Yang, Hanbiao, Du, Xinlin, Han, Guangzhou, Wang, Keshi, Cao, Zhaodan, Cheng, Tzuling, Czerwinski, Robert M, Goggin, Barry S, Huang, Heli, Halfmann, Megan M, Maddie, Melissa A, Morton, Emily L, Olive, Sarah R, Tan, Huiling, Xie, Shanhai, Wong, Tai, Josey, John A, Wallace, Eli M
Published in Journal of medicinal chemistry (08.11.2018)
Published in Journal of medicinal chemistry (08.11.2018)
Get full text
Journal Article
Spirocyclic β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors: From Hit to Lowering of Cerebrospinal Fluid (CSF) Amyloid β in a Higher Species
Hunt, Kevin W, Cook, Adam W, Watts, Ryan J, Clark, Christopher T, Vigers, Guy, Smith, Darin, Metcalf, Andrew T, Gunawardana, Indrani W, Burkard, Michael, Cox, April A, Geck Do, Mary K, Dutcher, Darrin, Thomas, Allen A, Rana, Sumeet, Kallan, Nicholas C, DeLisle, Robert K, Rizzi, James P, Regal, Kelly, Sammond, Douglas, Groneberg, Robert, Siu, Michael, Purkey, Hans, Lyssikatos, Joseph P, Marlow, Allison, Liu, Xingrong, Tang, Tony P
Published in Journal of medicinal chemistry (25.04.2013)
Published in Journal of medicinal chemistry (25.04.2013)
Get full text
Journal Article
Lead change of a HIF-2α antagonist guided by multiparameter optimization and utilization of an Olp→πAr interaction
Wehn, Paul M., Yang, Song, Grina, Jonas A., Rizzi, James P., Schlachter, Stephen T., Wang, Bin, Xu, Rui, Yang, Hanbiao, Du, Xinlin, Han, Guangzhou, Wang, Keshi, Czerwinski, Robert M., Ged, Emily L., Huang, Heli, Halfmann, Megan M., Maddie, Melissa A., Morton, Emily R., Olive, Sarah R., Tan, Huiling, Xie, Shanhai, Josey, John A., Wallace, Eli M.
Published in Medicinal chemistry research (01.07.2023)
Published in Medicinal chemistry research (01.07.2023)
Get full text
Journal Article
Discovery of a Novel Class of Imidazo[1,2‑a]Pyridines with Potent PDGFR Activity and Oral Bioavailability
Hicken, Erik J, Marmsater, Fred P, Munson, Mark C, Schlachter, Stephen T, Robinson, John E, Allen, Shelley, Burgess, Laurence E, DeLisle, Robert Kirk, Rizzi, James P, Topalov, George T, Zhao, Qian, Hicks, Julie M, Kallan, Nicholas C, Tarlton, Eugene, Allen, Andrew, Callejo, Michele, Cox, April, Rana, Sumeet, Klopfenstein, Nathalie, Woessner, Richard, Lyssikatos, Joseph P
Published in ACS medicinal chemistry letters (09.01.2014)
Published in ACS medicinal chemistry letters (09.01.2014)
Get full text
Journal Article
An initial three-component pharmacophore for specific serotonin-3 receptor ligands
Rizzi, James P, Nagel, Arthur A, Rosen, Terry, McLean, Stafford, Seeger, Thomas
Published in Journal of medicinal chemistry (01.10.1990)
Published in Journal of medicinal chemistry (01.10.1990)
Get full text
Journal Article
ARYL ETHER AND USE THEREOF
YANG HANBIAO, XU RUI, PAUL WHEN, JAMES P RIZZI, JONAS GRINA, STEPHEN T SCHLACHTER, JOHN A JOSEY, WALLACE ELI W, DARRYL DAVID DIXON, WANG BIN
Year of Publication 13.06.2019
Get full text
Year of Publication 13.06.2019
Patent
ARYL ETHER AND USE THEREOF
YANG HANBIAO, XU RUI, PAUL WHEN, JAMES P RIZZI, JONAS GRINA, STEPHEN T SCHLACHTER, JOHN A JOSEY, WALLACE ELI W, DARRYL DAVID DIXON, WANG BIN
Year of Publication 13.06.2019
Get full text
Year of Publication 13.06.2019
Patent
ARYL ETHER AND USE THEREOF
YANG HANBIAO, XU RUI, PAUL WHEN, JAMES P RIZZI, JONAS GRINA, STEPHEN T SCHLACHTER, JOHN A JOSEY, WALLACE ELI W, DARRYL DAVID DIXON, WANG BIN
Year of Publication 09.05.2019
Get full text
Year of Publication 09.05.2019
Patent
UK‐78,282, a novel piperidine compound that potently blocks the Kv1.3 voltage‐gated potassium channel and inhibits human T cell activation
Hanson, Douglas C, Nguyen, Angela, Mather, Robert J, Rauer, Heiko, Koch, Kevin, Burgess, Laurence E, Rizzi, James P, Donovan, Carol B, Bruns, Matthew J, Canniff, Paul C, Cunningham, Ann C, Verdries, Kimberly A, Mena, Edward, Kath, John C, Gutman, George A, Cahalan, Michael D, Grissmer, Stephan, Chandy, K George
Published in British journal of pharmacology (01.04.1999)
Published in British journal of pharmacology (01.04.1999)
Get full text
Journal Article
SUBSTITUTED N-(1H-INDAZOL-4-YL)IMIDAZO[1,2-a]PYRIDINE-3-CARBOXAMIDE COMPOUNDS AS TYPE III RECEPTOR TYROSINE KINASE INHIBITORS
MARESKA DAVID A, RAST BRYSON, APRIL L KENNEDY, JAMES P RIZZI, ERIK JAMES HICKEN, GEORGE T TOPALOV, ZHAO QIAN, BRAD NEWHOUSE, MARTHA E RODRIGUEZ, ROBERT KIRK DELISLE, MUNSON MARK C, FREDRIK P MARMSATER, MARK LAURENCE BOYS
Year of Publication 26.04.2018
Get full text
Year of Publication 26.04.2018
Patent
SUBSTITUTED N-(1H-INDAZOL-4-YL)IMIDAZO[1,2-a]PYRIDINE-3-CARBOXAMIDE COMPOUNDS AS TYPE III RECEPTOR TYROSINE KINASE INHIBITORS
MARESKA DAVID A, RAST BRYSON, APRIL L KENNEDY, JAMES P RIZZI, ERIK JAMES HICKEN, GEORGE T TOPALOV, ZHAO QIAN, BRAD NEWHOUSE, MARTHA E RODRIGUEZ, ROBERT KIRK DELISLE, MUNSON MARK C, FREDRIK P MARMSATER, MARK LAURENCE BOYS
Year of Publication 24.03.2016
Get full text
Year of Publication 24.03.2016
Patent