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45 results on '"Fantin, Valeria R."'

2. Targeting the CXCR4 pathway using a novel anti-CXCR4 IgG1 antibody (PF-06747143) in chronic lymphocytic leukemia

Author

Kashyap, Manoj K, Amaya-Chanaga, Carlos I, Kumar, Deepak, Simmons, Brett, Huser, Nanni, Gu, Yin, Hallin, Max, Lindquist, Kevin, Yafawi, Rolla, Choi, Michael Y, Amine, Ale-Ali, Rassenti, Laura Z, Zhang, Cathy, Liu, Shu-Hui, Smeal, Tod, Fantin, Valeria R, Kipps, Thomas J, Pernasetti, Flavia, and Castro, Januario E

Subjects
Biomedical and Clinical Sciences, Oncology and Carcinogenesis, Clinical Research, Lymphoma, Cancer, Hematology, Orphan Drug, Rare Diseases, Animals, Antineoplastic Agents, Immunological, B-Lymphocytes, CHO Cells, Cell Death, Cricetulus, Female, Humans, Immunoglobulin G, Leukemia, Lymphocytic, Chronic, B-Cell, Mice, Inbred BALB C, Mice, SCID, Reactive Oxygen Species, Receptors, CXCR4, Signal Transduction, T-Lymphocytes, Tumor Cells, Cultured, Chronic lymphocytic leukemia, PF-06747143, CXCR4, CXCL12, Chemokine, ADCC, CDC, Cell death, Reactive oxygen species, Cardiorespiratory Medicine and Haematology, Cardiovascular medicine and haematology, Oncology and carcinogenesis
Abstract

BackgroundThe CXCR4-CXCL12 axis plays an important role in the chronic lymphocytic leukemia (CLL)-microenvironment interaction. Overexpression of CXCR4 has been reported in different hematological malignancies including CLL. Binding of the pro-survival chemokine CXCL12 with its cognate receptor CXCR4 induces cell migration. CXCL12/CXCR4 signaling axis promotes cell survival and proliferation and may contribute to the tropism of leukemia cells towards lymphoid tissues and bone marrow. Therefore, we hypothesized that targeting CXCR4 with an IgG1 antibody, PF-06747143, may constitute an effective therapeutic approach for CLL.MethodsPatient-derived primary CLL-B cells were assessed for cytotoxicity in an in vitro model of CLL microenvironment. PF-06747143 was analyzed for cell death induction and for its potential to interfere with the chemokine CXCL12-induced mechanisms, including migration and F-actin polymerization. PF-06747143 in vivo efficacy was determined in a CLL murine xenograft tumor model.ResultsPF-06747143, a novel-humanized IgG1 CXCR4 antagonist antibody, induced cell death of patient-derived primary CLL-B cells, in presence or absence of stromal cells. Moreover, cell death induction by the antibody was independent of CLL high-risk prognostic markers. The cell death mechanism was dependent on CXCR4 expression, required antibody bivalency, involved reactive oxygen species production, and did not require caspase activation, all characteristics reminiscent of programmed cell death (PCD). PF-06747143 also induced potent B-CLL cytotoxicity via Fc-driven antibody-dependent cell-mediated cytotoxicity (ADCC) and complement-dependent cytotoxicity activity (CDC). PF-06747143 had significant combinatorial effect with standard of care (SOC) agents in B-CLL treatment, including rituximab, fludarabine (F-ara-A), ibrutinib, and bendamustine. In a CLL xenograft model, PF-06747143 decreased tumor burden and improved survival as a monotherapy, and in combination with bendamustine.ConclusionsWe show evidence that PF-06747143 has biological activity in CLL primary cells, supporting a rationale for evaluation of PF-06747143 for the treatment of CLL patients.

Published
2017

3. Leveraging model-based study designs and serial micro-sampling techniques to understand the oral pharmacokinetics of the potent LTB4 inhibitor, CP-105696, for mouse pharmacology studies

Author

Spilker, Mary E, Chung, Heekyung, Visswanathan, Ravi, Bagrodia, Shubha, Gernhardt, Steven, Fantin, Valeria R, and Ellies, Lesley G

Subjects
Pharmacology and Pharmaceutical Sciences, Biomedical and Clinical Sciences, Nutrition, Administration, Oral, Animals, Benzopyrans, Carboxylic Acids, Diet, High-Fat, Half-Life, Inflammation, Leukotriene B4, Mice, Models, Biological, Neutrophils, BLT1 antagonist, high-fat diet, leukotriene B4, mathematical modeling, ovariectomized, Biochemistry and Cell Biology, Pharmacology & Pharmacy, Biochemistry and cell biology, Pharmacology and pharmaceutical sciences
Abstract

1. Leukotriene B4 (LTB4) is a proinflammatory mediator important in the progression of a number of inflammatory diseases. Preclinical models can explore the role of LTB4 in pathophysiology using tool compounds, such as CP-105696, that modulate its activity. To support preclinical pharmacology studies, micro-sampling techniques and mathematical modeling were used to determine the pharmacokinetics of CP-105696 in mice within the context of systemic inflammation induced by a high-fat diet (HFD). 2. Following oral administration of doses > 35 mg/kg, CP-105696 kinetics can be described by a one-compartment model with first order absorption. The compound's half-life is 44-62 h with an apparent volume of distribution of 0.51-0.72 L/kg. Exposures in animals fed an HFD are within 2-fold of those fed a normal chow diet. Daily dosing at 100 mg/kg was not tolerated and resulted in a >20% weight loss in the mice. 3. CP-105696's long half-life has the potential to support a twice weekly dosing schedule. Given that most chronic inflammatory diseases will require long-term therapies, these results are useful in determining the optimal dosing schedules for preclinical studies using CP-105696.

Published
2017

4. Vorinostat

Author

Richon, Victoria M., Fantin, Valeria R., Ricker, Justin L., Frankel, Stanley R., and Schwab, Manfred, editor

Published
2017
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5. Table S1, Table S3, Figures S1-S8 from Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy

Author

Gomes, Bruno, primary, Driessens, Gregory, primary, Bartlett, Derek, primary, Cai, Danying, primary, Cauwenberghs, Sandra, primary, Crosignani, Stefano, primary, Dalvie, Deepak, primary, Denies, Sofie, primary, Dillon, Christopher P., primary, Fantin, Valeria R., primary, Guo, Jie, primary, Letellier, Marie-Claire, primary, Li, Wenlin, primary, Maegley, Karen, primary, Marillier, Reece, primary, Miller, Nichol, primary, Pirson, Romain, primary, Rabolli, Virginie, primary, Ray, Chad, primary, Streiner, Nicole, primary, Torti, Vince R., primary, Tsaparikos, Konstantinos, primary, Van den Eynde, Benoit J., primary, Wythes, Martin, primary, Yao, Li-Chin, primary, Zheng, Xianxian, primary, Tumang, Joseph, primary, and Kraus, Manfred, primary

Published
2023
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6. Data from Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy

Author

Gomes, Bruno, primary, Driessens, Gregory, primary, Bartlett, Derek, primary, Cai, Danying, primary, Cauwenberghs, Sandra, primary, Crosignani, Stefano, primary, Dalvie, Deepak, primary, Denies, Sofie, primary, Dillon, Christopher P., primary, Fantin, Valeria R., primary, Guo, Jie, primary, Letellier, Marie-Claire, primary, Li, Wenlin, primary, Maegley, Karen, primary, Marillier, Reece, primary, Miller, Nichol, primary, Pirson, Romain, primary, Rabolli, Virginie, primary, Ray, Chad, primary, Streiner, Nicole, primary, Torti, Vince R., primary, Tsaparikos, Konstantinos, primary, Van den Eynde, Benoit J., primary, Wythes, Martin, primary, Yao, Li-Chin, primary, Zheng, Xianxian, primary, Tumang, Joseph, primary, and Kraus, Manfred, primary

Published
2023
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7. Supplementary Methods from Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy

Author

Gomes, Bruno, primary, Driessens, Gregory, primary, Bartlett, Derek, primary, Cai, Danying, primary, Cauwenberghs, Sandra, primary, Crosignani, Stefano, primary, Dalvie, Deepak, primary, Denies, Sofie, primary, Dillon, Christopher P., primary, Fantin, Valeria R., primary, Guo, Jie, primary, Letellier, Marie-Claire, primary, Li, Wenlin, primary, Maegley, Karen, primary, Marillier, Reece, primary, Miller, Nichol, primary, Pirson, Romain, primary, Rabolli, Virginie, primary, Ray, Chad, primary, Streiner, Nicole, primary, Torti, Vince R., primary, Tsaparikos, Konstantinos, primary, Van den Eynde, Benoit J., primary, Wythes, Martin, primary, Yao, Li-Chin, primary, Zheng, Xianxian, primary, Tumang, Joseph, primary, and Kraus, Manfred, primary

Published
2023
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8. Table S2 from Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy

Author

Gomes, Bruno, primary, Driessens, Gregory, primary, Bartlett, Derek, primary, Cai, Danying, primary, Cauwenberghs, Sandra, primary, Crosignani, Stefano, primary, Dalvie, Deepak, primary, Denies, Sofie, primary, Dillon, Christopher P., primary, Fantin, Valeria R., primary, Guo, Jie, primary, Letellier, Marie-Claire, primary, Li, Wenlin, primary, Maegley, Karen, primary, Marillier, Reece, primary, Miller, Nichol, primary, Pirson, Romain, primary, Rabolli, Virginie, primary, Ray, Chad, primary, Streiner, Nicole, primary, Torti, Vince R., primary, Tsaparikos, Konstantinos, primary, Van den Eynde, Benoit J., primary, Wythes, Martin, primary, Yao, Li-Chin, primary, Zheng, Xianxian, primary, Tumang, Joseph, primary, and Kraus, Manfred, primary

Published
2023
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9. Supplementary Figure 7 from Constitutive Activation of Signal Transducers and Activators of Transcription Predicts Vorinostat Resistance in Cutaneous T-Cell Lymphoma

Author

Fantin, Valeria R., primary, Loboda, Andrey, primary, Paweletz, Cloud P., primary, Hendrickson, Ronald C., primary, Pierce, Jacqueline W., primary, Roth, Jennifer A., primary, Li, Lixia, primary, Gooden, Frank, primary, Korenchuk, Susan, primary, Hou, Xiaoli S., primary, Harrington, Elizabeth A., primary, Randolph, Sophia, primary, Reilly, John F., primary, Ware, Christopher M., primary, Kadin, Marshall E., primary, Frankel, Stanley R., primary, and Richon, Victoria M., primary

Published
2023
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10. Data from Constitutive Activation of Signal Transducers and Activators of Transcription Predicts Vorinostat Resistance in Cutaneous T-Cell Lymphoma

Author

Fantin, Valeria R., primary, Loboda, Andrey, primary, Paweletz, Cloud P., primary, Hendrickson, Ronald C., primary, Pierce, Jacqueline W., primary, Roth, Jennifer A., primary, Li, Lixia, primary, Gooden, Frank, primary, Korenchuk, Susan, primary, Hou, Xiaoli S., primary, Harrington, Elizabeth A., primary, Randolph, Sophia, primary, Reilly, John F., primary, Ware, Christopher M., primary, Kadin, Marshall E., primary, Frankel, Stanley R., primary, and Richon, Victoria M., primary

Published
2023
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11. Supplementary Figure 2 from Constitutive Activation of Signal Transducers and Activators of Transcription Predicts Vorinostat Resistance in Cutaneous T-Cell Lymphoma

Author

Fantin, Valeria R., primary, Loboda, Andrey, primary, Paweletz, Cloud P., primary, Hendrickson, Ronald C., primary, Pierce, Jacqueline W., primary, Roth, Jennifer A., primary, Li, Lixia, primary, Gooden, Frank, primary, Korenchuk, Susan, primary, Hou, Xiaoli S., primary, Harrington, Elizabeth A., primary, Randolph, Sophia, primary, Reilly, John F., primary, Ware, Christopher M., primary, Kadin, Marshall E., primary, Frankel, Stanley R., primary, and Richon, Victoria M., primary

Published
2023
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12. Supplementary Figure 8 from Constitutive Activation of Signal Transducers and Activators of Transcription Predicts Vorinostat Resistance in Cutaneous T-Cell Lymphoma

Author

Fantin, Valeria R., primary, Loboda, Andrey, primary, Paweletz, Cloud P., primary, Hendrickson, Ronald C., primary, Pierce, Jacqueline W., primary, Roth, Jennifer A., primary, Li, Lixia, primary, Gooden, Frank, primary, Korenchuk, Susan, primary, Hou, Xiaoli S., primary, Harrington, Elizabeth A., primary, Randolph, Sophia, primary, Reilly, John F., primary, Ware, Christopher M., primary, Kadin, Marshall E., primary, Frankel, Stanley R., primary, and Richon, Victoria M., primary

Published
2023
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13. Supplementary Figure 1 from Constitutive Activation of Signal Transducers and Activators of Transcription Predicts Vorinostat Resistance in Cutaneous T-Cell Lymphoma

Author

Fantin, Valeria R., primary, Loboda, Andrey, primary, Paweletz, Cloud P., primary, Hendrickson, Ronald C., primary, Pierce, Jacqueline W., primary, Roth, Jennifer A., primary, Li, Lixia, primary, Gooden, Frank, primary, Korenchuk, Susan, primary, Hou, Xiaoli S., primary, Harrington, Elizabeth A., primary, Randolph, Sophia, primary, Reilly, John F., primary, Ware, Christopher M., primary, Kadin, Marshall E., primary, Frankel, Stanley R., primary, and Richon, Victoria M., primary

Published
2023
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14. Supplementary Figure 6 from Constitutive Activation of Signal Transducers and Activators of Transcription Predicts Vorinostat Resistance in Cutaneous T-Cell Lymphoma

Author

Fantin, Valeria R., primary, Loboda, Andrey, primary, Paweletz, Cloud P., primary, Hendrickson, Ronald C., primary, Pierce, Jacqueline W., primary, Roth, Jennifer A., primary, Li, Lixia, primary, Gooden, Frank, primary, Korenchuk, Susan, primary, Hou, Xiaoli S., primary, Harrington, Elizabeth A., primary, Randolph, Sophia, primary, Reilly, John F., primary, Ware, Christopher M., primary, Kadin, Marshall E., primary, Frankel, Stanley R., primary, and Richon, Victoria M., primary

Published
2023
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15. Supplementary Figure 5 from Constitutive Activation of Signal Transducers and Activators of Transcription Predicts Vorinostat Resistance in Cutaneous T-Cell Lymphoma

Author

Fantin, Valeria R., primary, Loboda, Andrey, primary, Paweletz, Cloud P., primary, Hendrickson, Ronald C., primary, Pierce, Jacqueline W., primary, Roth, Jennifer A., primary, Li, Lixia, primary, Gooden, Frank, primary, Korenchuk, Susan, primary, Hou, Xiaoli S., primary, Harrington, Elizabeth A., primary, Randolph, Sophia, primary, Reilly, John F., primary, Ware, Christopher M., primary, Kadin, Marshall E., primary, Frankel, Stanley R., primary, and Richon, Victoria M., primary

Published
2023
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16. Supplementary Figure 3 from Constitutive Activation of Signal Transducers and Activators of Transcription Predicts Vorinostat Resistance in Cutaneous T-Cell Lymphoma

Author

Fantin, Valeria R., primary, Loboda, Andrey, primary, Paweletz, Cloud P., primary, Hendrickson, Ronald C., primary, Pierce, Jacqueline W., primary, Roth, Jennifer A., primary, Li, Lixia, primary, Gooden, Frank, primary, Korenchuk, Susan, primary, Hou, Xiaoli S., primary, Harrington, Elizabeth A., primary, Randolph, Sophia, primary, Reilly, John F., primary, Ware, Christopher M., primary, Kadin, Marshall E., primary, Frankel, Stanley R., primary, and Richon, Victoria M., primary

Published
2023
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17. Supplementary Figure 4 from Constitutive Activation of Signal Transducers and Activators of Transcription Predicts Vorinostat Resistance in Cutaneous T-Cell Lymphoma

Author

Fantin, Valeria R., primary, Loboda, Andrey, primary, Paweletz, Cloud P., primary, Hendrickson, Ronald C., primary, Pierce, Jacqueline W., primary, Roth, Jennifer A., primary, Li, Lixia, primary, Gooden, Frank, primary, Korenchuk, Susan, primary, Hou, Xiaoli S., primary, Harrington, Elizabeth A., primary, Randolph, Sophia, primary, Reilly, John F., primary, Ware, Christopher M., primary, Kadin, Marshall E., primary, Frankel, Stanley R., primary, and Richon, Victoria M., primary

Published
2023
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18. Macroautophagy is dispensable for growth of KRAS mutant tumors and chloroquine efficacy

Author

Eng, Christina H., Wang, Zuncai, Tkach, Diane, Toral-Barza, Lourdes, Ugwonali, Savuth, Liu, Shanming, Fitzgerald, Stephanie L., George, Elizabeth, Frias, Elizabeth, Cochran, Nadire, De Jesus, Rowena, McAllister, Gregory, Hoffman, Gregory R., Bray, Kevin, Lemon, LuAnna, Lucas, Judy, Fantin, Valeria R., Abraham, Robert T., Murphy, Leon O., and Nyfeler, Beat

Published
2016

19. PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations

Author

Zou, Helen Y., Li, Qiuhua, Engstrom, Lars D., West, Melissa, Appleman, Vicky, Wong, Katy A., McTigue, Michele, Deng, Ya-Li, Liu, Wei, Brooun, Alexei, Timofeevski, Sergei, McDonnell, Scott R. P., Jiang, Ping, Falk, Matthew D., Lappin, Patrick B., Affolter, Timothy, Nichols, Tim, Hu, Wenyue, Lam, Justine, Johnson, Ted W., Smeal, Tod, Charest, Al, and Fantin, Valeria R.

Published
2015

20. Orally Bioavailable Small-Molecule CD73 Inhibitor (OP-5244) Reverses Immunosuppression through Blockade of Adenosine Production

Author

Du, Xiaohui, primary, Moore, Jared, additional, Blank, Brian R., additional, Eksterowicz, John, additional, Sutimantanapi, Dena, additional, Yuen, Natalie, additional, Metzger, Todd, additional, Chan, Brenda, additional, Huang, Tom, additional, Chen, Xi, additional, Chen, Yuping, additional, Duong, Frank, additional, Kong, Wayne, additional, Chang, Jae H., additional, Sun, Jessica, additional, Zavorotinskaya, Tatiana, additional, Ye, Qiuping, additional, Junttila, Melissa R., additional, Ndubaku, Chudi, additional, Friedman, Lori S., additional, Fantin, Valeria R., additional, and Sun, Daqing, additional

Published
2020
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21. Abstract LB-A19: Intratumoral immunosuppression is reversed by blocking adenosine production with an oral inhibitor of CD73

Author

Metzger, Todd C, primary, Blank, Brian R, additional, Chan, Brenda, additional, Chen, Chelsea, additional, Chen, Yuping, additional, Du, Xiaohui, additional, Duong, Frank L, additional, Fantin, Valeria R., additional, Friedman, Lori S, additional, Moore, Jared T, additional, Sun, Daqing, additional, Sun, Jessica, additional, Sutimantanapi, Dena, additional, Ye, Qiuping, additional, Yuen, Natalie, additional, and Zavorotinskaya, Tatiana, additional

Published
2019
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23. Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633)

Author

Du, Xiaohui, primary, Eksterowicz, John, additional, Zhou, Haiying, additional, Rew, Yosup, additional, Zhu, Liusheng, additional, Yan, Xuelei, additional, Medina, Julio C., additional, Huang, Tom, additional, Chen, Xi, additional, Sutimantanapi, Dena, additional, Jahchan, Nadine, additional, Kong, Wayne, additional, Sun, Jessica, additional, Zavorotinskaya, Tatiana, additional, Ye, Qiuping, additional, Fantin, Valeria R., additional, and Sun, Daqing, additional

Published
2019
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24. Palbociclib and Fulvestrant Act in Synergy to Modulate Central Carbon Metabolism in Breast Cancer Cells

Author

Warth, Benedikt, primary, Palermo, Amelia, additional, Rattray, Nicholas J.W., additional, Lee, Nathan V., additional, Zhu, Zhou, additional, Hoang, Linh T., additional, Cai, Yuping, additional, Mazurek, Anthony, additional, Dann, Stephen, additional, VanArsdale, Todd, additional, Fantin, Valeria R., additional, Shields, David, additional, Siuzdak, Gary, additional, and Johnson, Caroline H., additional

Published
2019
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25. Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy

Author

Gomes, Bruno, primary, Driessens, Gregory, additional, Bartlett, Derek, additional, Cai, Danying, additional, Cauwenberghs, Sandra, additional, Crosignani, Stefano, additional, Dalvie, Deepak, additional, Denies, Sofie, additional, Dillon, Christopher P., additional, Fantin, Valeria R., additional, Guo, Jie, additional, Letellier, Marie-Claire, additional, Li, Wenlin, additional, Maegley, Karen, additional, Marillier, Reece, additional, Miller, Nichol, additional, Pirson, Romain, additional, Rabolli, Virginie, additional, Ray, Chad, additional, Streiner, Nicole, additional, Torti, Vince R., additional, Tsaparikos, Konstantinos, additional, Van den Eynde, Benoit J., additional, Wythes, Martin, additional, Yao, Li-Chin, additional, Zheng, Xianxian, additional, Tumang, Joseph, additional, and Kraus, Manfred, additional

Published
2018
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26. Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101)

Author

Rew, Yosup, primary, Du, Xiaohui, additional, Eksterowicz, John, additional, Zhou, Haiying, additional, Jahchan, Nadine, additional, Zhu, Liusheng, additional, Yan, Xuelei, additional, Kawai, Hiroyuki, additional, McGee, Lawrence R., additional, Medina, Julio C., additional, Huang, Tom, additional, Chen, Chelsea, additional, Zavorotinskaya, Tatiana, additional, Sutimantanapi, Dena, additional, Waszczuk, Joanna, additional, Jackson, Erica, additional, Huang, Elizabeth, additional, Ye, Qiuping, additional, Fantin, Valeria R., additional, and Sun, Daqing, additional

Published
2018
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27. Abstract 2649: Fc-effector function activity of the CXCR4 IgG1 antibody PF-06747143: a novel clinical candidate for the treatment of hematologic malignancies

Author

Pernasetti, Flavia, primary, Liu, Shu-Hui, additional, Yin, Gu, additional, Pascual, Bernadette, additional, Yan, Zhengming, additional, Hallin, Max, additional, Yafawi, Rolla, additional, Zhang, Cathy, additional, Fang, Connie, additional, Wang, Wenlian, additional, Lam, Justine, additional, Spilker, Mary E., additional, Blasi, Eileen, additional, Simmons, Brett, additional, Huser, Nanni, additional, Ho, Wei-Hsien, additional, Lindquist, Kevin, additional, Tran, Thomas-Toan, additional, Kudaravalli, Jyothirmayee, additional, Ma, Jing-Tyan, additional, Jimenez, Gretchen, additional, Barman, Ishita, additional, Brown, Colleen, additional, Chin, Sherman-Michael, additional, Costa, Maria, additional, Shelton, David, additional, Smeal, Tod, additional, and Fantin, Valeria R., additional

Published
2017
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28. A novel CXCR4 antagonist IgG1 antibody (PF-06747143) for the treatment of hematologic malignancies

Author

Liu, Shu-Hui, primary, Gu, Yin, additional, Pascual, Bernadette, additional, Yan, Zhengming, additional, Hallin, Max, additional, Zhang, Cathy, additional, Fan, Conglin, additional, Wang, Wenlian, additional, Lam, Justine, additional, Spilker, Mary E., additional, Yafawi, Rolla, additional, Blasi, Eileen, additional, Simmons, Brett, additional, Huser, Nanni, additional, Ho, Wei-Hsien, additional, Lindquist, Kevin, additional, Tran, Thomas-Toan, additional, Kudaravalli, Jyothirmayee, additional, Ma, Jing-Tyan, additional, Jimenez, Gretchen, additional, Barman, Ishita, additional, Brown, Colleen, additional, Chin, Sherman Michael, additional, Costa, Maria J., additional, Shelton, David, additional, Smeal, Tod, additional, Fantin, Valeria R., additional, and Pernasetti, Flavia, additional

Published
2017
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29. Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A

Author

Quinlan, Casey L, primary, Kaiser, Stephen E, additional, Bolaños, Ben, additional, Nowlin, Dawn, additional, Grantner, Rita, additional, Karlicek-Bryant, Shannon, additional, Feng, Jun Li, additional, Jenkinson, Stephen, additional, Freeman-Cook, Kevin, additional, Dann, Stephen G, additional, Wang, Xiaoli, additional, Wells, Peter A, additional, Fantin, Valeria R, additional, Stewart, Al E, additional, and Grant, Stephan K, additional

Published
2017
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30. Correction to Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors

Author

Kung, Pei-Pei, primary, Rui, Eugene, additional, Bergqvist, Simon, additional, Bingham, Patrick, additional, Braganza, John, additional, Collins, Michael, additional, Cui, Mei, additional, Diehl, Wade, additional, Dinh, Dac, additional, Fan, Connie, additional, Fantin, Valeria R., additional, Gukasyan, Hovhannes J., additional, Hu, Wenyue, additional, Huang, Buwen, additional, Kephart, Susan, additional, Krivacic, Cody, additional, Kumpf, Robert A., additional, Li, Gary, additional, Maegley, Karen A., additional, McAlpine, Indrawan, additional, Nguyen, Lisa, additional, Ninkovic, Sacha, additional, Ornelas, Martha, additional, Ryskin, Michael, additional, Scales, Stephanie, additional, Sutton, Scott, additional, Tatlock, John, additional, Verhelle, Dominique, additional, Wang, Fen, additional, Wells, Peter, additional, Wythes, Martin, additional, Yamazaki, Shinji, additional, Yip, Brian, additional, Yu, Xiu, additional, Zehnder, Luke, additional, Zhang, Wei-Guo, additional, Rollins, Robert A., additional, and Edwards, Martin, additional

Published
2016
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31. PF-06463922, an ALK/ROS1 inhibitor, overcomes resistance to 1st and 2nd generation ALK inhibitors in pre-clinical models

Author

Zou, Helen Y., Friboulet, Luc, Kodack, David P., Engstrom, Lars D., Li, Qiuhua, West, Melissa, Tang, Ruth W., Wang, Hui, Tsaparikos, Konstantinos, Wang, Jinwei, Timofeevski, Sergei, Katayama, Ryohei, Dinh, Dac M., Lam, Hieu, Lam, Justine L., Yamazaki, Shinji, Hu, Wenyue, Patel, Bhushankumar, Bezwada, Divya, Frias, Rosa L., Lifshits, Eugene, Mahmood, Sidra, Gainor, Justin F., Affolter, Timothy, Lappin, Patrick B., Gukasyan, Hovhannes, Lee, Nathan, Deng, Shibing, Jain, Rakesh K, Johnson, Ted W., Shaw, Alice T., Fantin, Valeria R., and Smeal, Tod

Subjects
Lactams, Brain Neoplasms, Lactams, Macrocyclic, Aminopyridines, Receptor Protein-Tyrosine Kinases, Antineoplastic Agents, Xenograft Model Antitumor Assays, Article, Mice, Drug Resistance, Neoplasm, hemic and lymphatic diseases, Cell Line, Tumor, Neoplasms, Mutation, NIH 3T3 Cells, Animals, Humans, Pyrazoles, Anaplastic Lymphoma Kinase, Protein Kinase Inhibitors, Cell Proliferation
Abstract

We report the preclinical evaluation of PF-06463922, a potent and brain penetrant ALK/ROS1 inhibitor. Compared to other clinically available ALK inhibitors, PF-06463922 displayed superior potency against all known clinically acquired ALK mutations, including the highly resistant G1202R mutant. Furthermore, PF-06463922 treatment led to regression of EML4-ALK driven brain metastases, leading to prolonged mouse survival, in a superior manner. Finally, PF-06463922 demonstrated high selectivity and safety margins in a variety of preclinical studies. These results suggest that PF-06463922 will be highly effective for the treatment of patients with ALK-driven lung cancers, including those who relapsed on clinically available ALK inhibitors due to secondary ALK kinase domain mutations and/or due to the failed control of brain metastases.

Published
2015

32. Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors

Author

Kung, Pei-Pei, primary, Rui, Eugene, additional, Bergqvist, Simon, additional, Bingham, Patrick, additional, Braganza, John, additional, Collins, Michael, additional, Cui, Mei, additional, Diehl, Wade, additional, Dinh, Dac, additional, Fan, Connie, additional, Fantin, Valeria R., additional, Gukasyan, Hovhannes J., additional, Hu, Wenyue, additional, Huang, Buwen, additional, Kephart, Susan, additional, Krivacic, Cody, additional, Kumpf, Robert A., additional, Li, Gary, additional, Maegley, Karen A., additional, McAlpine, Indrawan, additional, Nguyen, Lisa, additional, Ninkovic, Sacha, additional, Ornelas, Martha, additional, Ryskin, Michael, additional, Scales, Stephanie, additional, Sutton, Scott, additional, Tatlock, John, additional, Verhelle, Dominique, additional, Wang, Fen, additional, Wells, Peter, additional, Wythes, Martin, additional, Yamazaki, Shinji, additional, Yip, Brian, additional, Yu, Xiu, additional, Zehnder, Luke, additional, Zhang, Wei-Guo, additional, Rollins, Robert A., additional, and Edwards, Martin, additional

Published
2016
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36. Macroautophagy is dispensable for growth of KRAS mutant tumors and chloroquine efficacy

Author

Eng, Christina H., primary, Wang, Zuncai, additional, Tkach, Diane, additional, Toral-Barza, Lourdes, additional, Ugwonali, Savuth, additional, Liu, Shanming, additional, Fitzgerald, Stephanie L., additional, George, Elizabeth, additional, Frias, Elizabeth, additional, Cochran, Nadire, additional, De Jesus, Rowena, additional, McAllister, Gregory, additional, Hoffman, Gregory R., additional, Bray, Kevin, additional, Lemon, LuAnna, additional, Lucas, Judy, additional, Fantin, Valeria R., additional, Abraham, Robert T., additional, Murphy, Leon O., additional, and Nyfeler, Beat, additional

Published
2015
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37. Abstract 130: PF-06463922, a novel next generation ALK/ROS1 inhibitor, overcomes resistance to 1st and 2nd generation ALK inhibitors in pre-clinical models

Author

Friboulet, Luc, primary, Zou, Helen, additional, Kodack, David P., additional, Engstrom, Lars D., additional, Li, Qiuhua, additional, West, Melissa, additional, Tang, Ruth W., additional, Wang, Hui, additional, Tsaparikos, Konstantinos, additional, Wang, Jinwei, additional, Timofeevski, Sergei, additional, Dinh, Dac M., additional, Lam, Hieu, additional, Lam, Justine L., additional, Yamazaki, Shinji, additional, Hu, Wenyue, additional, Patel, Bhushankumar, additional, Bezwada, Divya, additional, Mahmood, Sidra, additional, Lifshits, Eugene, additional, Affolter, Timothy, additional, Lappin, Patrick B., additional, Gukasyan, Hovhannes, additional, Lee, Nathan, additional, Deng, Shibing, additional, Jain, Rakesh K., additional, Johnson, Ted W., additional, Shaw, Alice T., additional, Fantin, Valeria R., additional, and Smeal, Tod, additional

Published
2015
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38. PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models

Author

Zou, Helen Y., primary, Friboulet, Luc, additional, Kodack, David P., additional, Engstrom, Lars D., additional, Li, Qiuhua, additional, West, Melissa, additional, Tang, Ruth W., additional, Wang, Hui, additional, Tsaparikos, Konstantinos, additional, Wang, Jinwei, additional, Timofeevski, Sergei, additional, Katayama, Ryohei, additional, Dinh, Dac M., additional, Lam, Hieu, additional, Lam, Justine L., additional, Yamazaki, Shinji, additional, Hu, Wenyue, additional, Patel, Bhushankumar, additional, Bezwada, Divya, additional, Frias, Rosa L., additional, Lifshits, Eugene, additional, Mahmood, Sidra, additional, Gainor, Justin F., additional, Affolter, Timothy, additional, Lappin, Patrick B., additional, Gukasyan, Hovhannes, additional, Lee, Nathan, additional, Deng, Shibing, additional, Jain, Rakesh K., additional, Johnson, Ted W., additional, Shaw, Alice T., additional, Fantin, Valeria R., additional, and Smeal, Tod, additional

Published
2015
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39. Redox-Mediated Suberoylanilide Hydroxamic Acid Sensitivity in Breast Cancer

Author

Chiaradonna, Ferdinando, primary, Barozzi, Iros, additional, Miccolo, Claudia, additional, Bucci, Gabriele, additional, Palorini, Roberta, additional, Fornasari, Lorenzo, additional, Botrugno, Oronza A., additional, Pruneri, Giancarlo, additional, Masullo, Michele, additional, Passafaro, Alfonso, additional, Galimberti, Viviana E., additional, Fantin, Valeria R., additional, Richon, Victoria M., additional, Pece, Salvatore, additional, Viale, Giuseppe, additional, Di Fiore, Pier Paolo, additional, Draetta, Giulio, additional, Pelicci, Pier Giuseppe, additional, Minucci, Saverio, additional, and Chiocca, Susanna, additional

Published
2015
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40. Reciprocal regulation of amino acid import and epigenetic state through Lat1 and EZH 2

Author

Dann, Stephen G, primary, Ryskin, Michael, additional, Barsotti, Anthony M, additional, Golas, Jonathon, additional, Shi, Celine, additional, Miranda, Miriam, additional, Hosselet, Christine, additional, Lemon, Luanna, additional, Lucas, Judy, additional, Karnoub, Maha, additional, Wang, Fang, additional, Myers, Jeremy S, additional, Garza, Scott J, additional, Follettie, Maximillian T, additional, Geles, Kenneth G, additional, Klippel, Anke, additional, Rollins, Robert A, additional, and Fantin, Valeria R, additional

Published
2015
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41. Preclinical target validation using patient-derived cells

Author

Edwards, Aled M., primary, Arrowsmith, Cheryl H., additional, Bountra, Chas, additional, Bunnage, Mark E., additional, Feldmann, Marc, additional, Knight, Julian C., additional, Patel, Dhavalkumar D., additional, Prinos, Panagiotis, additional, Taylor, Michael D., additional, Sundström, Michael, additional, Barker, Phil, additional, Barsyte, Dalia, additional, Bengtson, Mario H., additional, Bell, Cindy, additional, Bowness, Paul, additional, Boycott, Kym M., additional, Buser-Doepner, Carolyn, additional, Carpenter, Christopher L., additional, Carr, Andrew J., additional, Clark, Kirk, additional, Das, Anuk M., additional, Dhanak, Dashyant, additional, Dirks, Peter, additional, Ellis, James, additional, Fantin, Valeria R., additional, Flores, Christopher, additional, Fon, Edward A., additional, Frail, Donald E., additional, Gileadi, Opher, additional, O'Hagan, Ronan C., additional, Howe, Trevor, additional, Isaac, John T. R., additional, Jabado, Nada, additional, Jakobsson, Per-Johan, additional, Klareskog, Lars, additional, Knapp, Stefan, additional, Lee, Wen Hwa, additional, Lima-Fernandes, Evelyne, additional, Lundberg, Ingrid E., additional, Marshall, John, additional, Massirer, Katlin B., additional, MacKenzie, Alex E., additional, Maruyama, Tetsuyuki, additional, Mueller-Fahrnow, Anke, additional, Muthuswamy, Senthil, additional, Nanchahal, Jagdeep, additional, O'Brien, Catherine, additional, Oppermann, Udo, additional, Ostermann, Nils, additional, Petrecca, Kevin, additional, Pollock, Bruce G., additional, Poupon, Viviane, additional, Prinjha, Rab K., additional, Rosenberg, Saul H., additional, Rouleau, Guy, additional, Skingle, Malcolm, additional, Slutsky, Arthur S., additional, Smith, Garth A. M., additional, Verhelle, Dominique, additional, Widmer, Hans, additional, and Young, L. Trevor, additional

Published
2015
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42. Epigenetic reprogramming by tumor-derived EZH2 gain-of-function mutations promotes aggressive 3D cell morphologies and enhances melanoma tumor growth

Author

Barsotti, Anthony M., primary, Ryskin, Michael, additional, Zhong, Wenyan, additional, Zhang, Wei-Guo, additional, Giannakou, Andreas, additional, Loreth, Christine, additional, Diesl, Veronica, additional, Follettie, Maximillian, additional, Golas, Jonathon, additional, Lee, Michelle, additional, Nichols, Timothy, additional, Fan, Conglin, additional, Li, Gang, additional, Dann, Stephen, additional, Fantin, Valeria R., additional, Arndt, Kim, additional, Verhelle, Dominique, additional, and Rollins, Robert A., additional

Published
2015
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43. Resistance to dual blockade of the kinases PI3K and mTOR in KRAS -mutant colorectal cancer models results in combined sensitivity to inhibition of the receptor tyrosine kinase EGFR

Author

Belmont, Peter J., primary, Jiang, Ping, additional, McKee, Trevor D., additional, Xie, Tao, additional, Isaacson, Jason, additional, Baryla, Nicole E., additional, Roper, Jatin, additional, Sinnamon, Mark J., additional, Lee, Nathan V., additional, Kan, Julie L. C., additional, Guicherit, Oivin, additional, Wouters, Bradly G., additional, O’Brien, Catherine A., additional, Shields, David, additional, Olson, Peter, additional, VanArsdale, Todd, additional, Weinrich, Scott L., additional, Rejto, Paul, additional, Christensen, James G., additional, Fantin, Valeria R., additional, Hung, Kenneth E., additional, and Martin, Eric S., additional

Published
2014
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45. Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.

Author

Pei-Pei Kung, Rui, Eugene, Bergqvist, Simon, Bingham, Patrick, Braganza, John, Collins, Michael, Mei Cui, Diehl, Wade, Dinh, Dac, Fan, Connie, Fantin, Valeria R., Gukasyan, Hovhannes J., Wenyue Hu, Buwen Huang, Kephart, Susan, Krivacic, Cody, Kumpf, Robert A., Li, Gary, Maegley, Karen A., and McAlpine, Indrawan

Published
2016
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