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282 results on '"Fantin, Valeria"'

1. Collaborative Innovations in Childhood Cancer Therapies

Author

Valtingojer, Iris, Lièvre, Sasha, Bordes, Philippe, Paranjpe, Krupa, Thompson, Winifred, Shah, Sachin, Fantin, Valeria, Jacquemet-Ross, Wendy, Adamson, Peter C., Michel, Martin C., Editor-in-Chief, Barrett, James E., Editorial Board Member, Centurión, David, Editorial Board Member, Flockerzi, Veit, Editorial Board Member, Meier, Kathryn Elaine, Editorial Board Member, Page, Clive P., Series Editor, Seifert, Roland, Editorial Board Member, Wang, KeWei, Editorial Board Member, and Wieland, Heike A., editor

Published
2024
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3. 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

4. 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

5. Vorinostat

Author

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

Published
2017
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6. Abstract 6378: An in vitro human CD8 T cell exhaustion model for the functional screening of immune checkpoint inhibitors

Author

Carrio, Roberto, primary, Cucchetti, Margot, additional, Devonish, Mikielia, additional, Poisson, Louis, additional, Babiceanu, Mihaela, additional, Kettring, Andrew, additional, Liu, Yingchun, additional, Jackson, Donald, additional, Gomes, Evan, additional, Baudhuin, Jeremy, additional, Drake, Donald R., additional, Fantin, Valeria, additional, Byers, Anthony, additional, and Sassoon, Ingrid, additional

Published
2023
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7. 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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8. 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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9. 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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10. 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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11. 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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12. 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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13. 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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14. 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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15. 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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16. 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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17. 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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18. 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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19. 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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20. 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

21. 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

22. Vorinostat

Author

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

Published
2011
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23. Vorinostat

Author

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

Published
2009
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25. Leukemic IDH1 and IDH2 Mutations Result in a Hypermethylation Phenotype, Disrupt TET2 Function, and Impair Hematopoietic Differentiation

Author

Figueroa, Maria E., Abdel-Wahab, Omar, Lu, Chao, Ward, Patrick S., Patel, Jay, Shih, Alan, Li, Yushan, Bhagwat, Neha, Vasanthakumar, Aparna, Fernandez, Hugo F., Tallman, Martin S., Sun, Zhuoxin, Wolniak, Kristy, Peeters, Justine K., Liu, Wei, Choe, Sung E., Fantin, Valeria R., Paietta, Elisabeth, Löwenberg, Bob, Licht, Jonathan D., Godley, Lucy A., Delwel, Ruud, Valk, Peter J.M., Thompson, Craig B., Levine, Ross L., and Melnick, Ari

Published
2010
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27. 577 Non-clinical efficacy, pharmacokinetics, and pharmacodynamics of a novel bi-functional anti-CD73-TGFβRII-trap molecule in combination with immune checkpoint therapy

Author

Stinson, Susanna, primary, He, Jianhua, additional, Kim, Kyung-Hoon, additional, Yang, Becky, additional, Zavodovskaya, Marianna, additional, Yi, Ping, additional, Campigotto, Federico, additional, Sobczyk, Monika, additional, Dave, Rutwij, additional, Carr, Brian, additional, Mah, In Kyoung, additional, Zaboli, Shiva, additional, Brodbeck, Jens, additional, Turner, Scott, additional, Barry, Vivian, additional, Boyd, Kelli, additional, and Fantin, Valeria, additional

Published
2021
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28. Non-invasive detection of 2-hydroxyglutarate and other metabolites in IDH1 mutant glioma patients using magnetic resonance spectroscopy

Author

Pope, Whitney B., Prins, Robert M., Albert Thomas, M., Nagarajan, Rajakumar, Yen, Katharine E., Bittinger, Mark A., Salamon, Noriko, Chou, Arthur P., Yong, William H., Soto, Horacio, Wilson, Neil, Driggers, Edward, Jang, Hyun G., Su, Shinsan M., Schenkein, David P., Lai, Albert, Cloughesy, Timothy F., Kornblum, Harley I., Wu, Hong, Fantin, Valeria R., and Liau, Linda M.

Published
2012
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29. Phase 1 study of the histone deacetylase inhibitor vorinostat (suberoylanilide hydroxamic acid [SAHA]) in patients with advanced leukemias and myelodysplastic syndromes

Author

Garcia-Manero, Guillermo, Yang, Hui, Bueso-Ramos, Carlos, Ferrajoli, Alessandra, Cortes, Jorge, Wierda, William G., Faderl, Stefan, Koller, Charles, Morris, Gail, Rosner, Gary, Loboda, Andrey, Fantin, Valeria R., Randolph, Sophia S., Hardwick, James S., Reilly, John F., Chen, Cong, Ricker, Justin L., Secrist, J. Paul, Richon, Victoria M., Frankel, Stanley R., and Kantarjian, Hagop M.

Published
2008
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30. Cancer-associated IDH1 mutations produce 2-hydroxyglutarate

Author

Dang, Lenny, White, David W., Gross, Stefan, Bennett, Bryson D., Bittinger, Mark A., Driggers, Edward M., Fantin, Valeria R., Jang, Hyun Gyung, Jin, Shengfang, Keenan, Marie C., Marks, Kevin M., Prins, Robert M., Ward, Patrick S., Yen, Katharine E., Liau, Linda M., Rabinowitz, Joshua D., Cantley, Lewis C., Thompson, Craig B., Vander Heiden, Matthew G., and Su, Shinsan M.

Subjects
Gene mutations -- Health aspects, Isocitrate dehydrogenase -- Genetic aspects -- Health aspects, Gliomas -- Development and progression -- Genetic aspects, Brain tumors -- Development and progression -- Genetic aspects, Alpha hydroxy acids -- Genetic aspects -- Health aspects, Environmental issues, Science and technology, Zoology and wildlife conservation, Development and progression, Genetic aspects, Research, Health aspects
Abstract

Mutations in the enzyme cytosolic isocitrate dehydrogenase 1 (IDH1) are a common feature of a major subset of primary human brain cancers. These mutations occur at a single amino acid residue of the IDH1 active site, resulting in loss of the enzyme's ability to catalyse conversion of isocitrate to α-ketoglutarate. However, only a single copy of the gene is mutated in tumours, raising the possibility that the mutations do not result in a simple loss of function. Here we show that cancer-associated IDH1 mutations result in a new ability of the enzyme to catalyse the NADPH-dependent reduction of α-ketoglutarate to R(-)-2-hydroxyglutarate (2HG). Structural studies demonstrate that when arginine 132 is mutated to histidine, residues in the active site are shifted to produce structural changes consistent with reduced oxidative decarboxylation of isocitrate and acquisition of the ability to convert α-ketoglutarate to 2HG. Excess accumulation of 2HG has been shown to lead to an elevated risk of malignant brain tumours in patients with inborn errors of 2HG metabolism. Similarly, in human malignant gliomas harbouring IDH1 mutations, we find markedly elevated levels of 2HG. These data demonstrate that the IDH1 mutations result in production of the onco-metabolite 2HG, and indicate that the excess 2HG which accumulates in vivo contributes to the formation and malignant progression of gliomas., Mutations in the enzyme cytosolic isocitrate dehydrogenase 1 (IDH1) are found in approximately 80% of grade II-III gliomas and secondary glioblastomas in humans (1-3). These mutations occur at a single [...]

Published
2009
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31. Missense mutations in the BCS1L gene as a cause of the Bjornstad syndrome

Author

Hinson, J. Travis, Fantin, Valeria R., Schonberger, Jost, Breivik, Noralv, Siem, Geir, McDonough, Barbara, Sharma, Pankaj, Keogh, Ivan, Godinho, Ricardo, Santos, Felipe, Esparza, Alfonso, Nicolau, Yamileth, Selvaag, Edgar, Cohen, Bruce H., Hoppel, Charles L., Tranebjaerg, Lisbeth, Eavey, Roland D., Seidman, J.G., and Seidman, Christine E.

Subjects
Human chromosome abnormalities -- Research, Human chromosome abnormalities -- Diagnosis, Human chromosome abnormalities -- Care and treatment
Abstract

A study demonstrates that mutations in the BSC1L gene cause the Bjornstad syndrome by disrupting the assembly of mitochondrial respirasomes, which are the basic unit for respiration in human mitochondria. Mutations that cause the Bjornstad syndrome illustrate the acute sensitivity of ear and hair tissues to mitochondrial function, particularly to the production of reactive oxygen species.

Published
2007

32. Vorinostat

Author

Richon, Victoria M., primary, Fantin, Valeria R., additional, Ricker, Justin L., additional, and Frankel, Stanley R., additional

Published
2012
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34. Abstract B25: Development of a nanoparticle containing the PI3K/mTOR dual Inhibitor, gedatolisib, for cancer therapy

Author

Zhang, Lianglin, primary, Troche, Gabriel, additional, Visswanathan, Ravi, additional, Huang, Wenhu, additional, Song, Young-Ho, additional, Spilker, Mary E., additional, Wang, Zhenxiong, additional, Wang, Hui, additional, Giddabasappa, Anand, additional, Cadzow, Louise, additional, Low, Susan, additional, Troiano, Greg, additional, Lafontaine, Jennifer, additional, Fantin, Valeria, additional, Abraham, Robert T., additional, and Bagrodia, Shubha, additional

Published
2020
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35. 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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36. 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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39. 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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40. 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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41. 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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43. 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

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

Published
2018

44. Additional file 6: Figure S6. of Targeting the CXCR4 pathway using a novel anti-CXCR4 IgG1 antibody (PF-06747143) in chronic lymphocytic leukemia

Author

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

Abstract

m15-IgG1-induced LR or HR CLL-B cell death is independent of caspase activation. CLL-B cells were treated for 6 h with m15-IgG1 (1, 10, or 100 nM) or IgG1 control antibody. Caspases 3, 8, and 9 were measured using a colometric detection method. The data shown is derived from four high-risk (HR) and four low-risk (LR) CLL patients. The HR patients are denoted by triangles and LR patients denoted by circles. The individual data points for each group are shown. The horizontal lines represent the mean for each group. Statistical comparisons were performed using Bonferroni’s correction test. (PDF 915 kb)

Published
2017
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45. Additional file 3: Figure S3. of Targeting the CXCR4 pathway using a novel anti-CXCR4 IgG1 antibody (PF-06747143) in chronic lymphocytic leukemia

Author

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

Subjects
immune system diseases, hemic and lymphatic diseases
Abstract

The PF-06747143 parent IgG1 antibody (m15 IgG1) induces cell death and this activity is similar in HR and LR CLL patients. Primary CLL-B cells derived from CLL patients were incubated either alone (n = 10) or co-cultured with stroma-NK-tert cells (n = 10) and treated with vehicle, IgG1 control Ab, or m15-IgG1 antibody for 48 h. Cell death was measured using CD19/CD5/Annexin V staining followed by flow cytometry analysis. The data is derived from five high-risk (HR) and five low-risk (LR) CLL patients. The HR patients are presented with solid symbols (•) and LR patients denoted with hollow symbols (○). The individual data points for each group are shown. The horizontal lines represent the mean for each group Statistical comparisons were performed using Bonferroni’s correction test. (PDF 744 kb)

Published
2017
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46. Additional file 4: Figure S4. of Targeting the CXCR4 pathway using a novel anti-CXCR4 IgG1 antibody (PF-06747143) in chronic lymphocytic leukemia

Author

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

Subjects
hemic and lymphatic diseases
Abstract

m15-IgG1 and m15-IgG4 have similar cell death activity in HR and LR CLL patients, in presence or absence of stromal cells. The primary CLL-B cells derived from CLL patients were incubated either alone (n = 4) or co-cultured with stroma-NK-tert cells (n = 4) and treated with vehicle, m15-IgG1, m15-IgG4, IgG1 control antibody, or IgG4 control antibody for 48 h. Cell death was measured using CD19/CD5/Annexin V staining followed by flow cytometry analysis. The data is presented as % specific induced cell death (% SICD). The data shown is derived from two high-risk (HR) and two low-risk (LR) CLL patients. The HR patients are presented with solid symbols (•) and LR patients denoted with hollow symbols (○). The individual data points for each group are shown. The horizontal lines represent the mean for each group. Statistical comparisons were performed using Bonferroni’s correction test. (PDF 1032 kb)

Published
2017
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47. 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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48. Abstract 1968: A novel glucocorticoid receptor (GR) antagonist overcomes GR-mediated chemoresistance in triple-negative breast cancer

Author

Jahchan, Nadine, primary, Zhou, Haiying, additional, Kong, Wayne, additional, Weeney, Dan Mc, additional, Tracy, Ted, additional, Stice, James, additional, Sutimantanapi, Dena, additional, Chen, Chelsea, additional, Huang, Tom, additional, Rew, Yosup, additional, Du, Xiauhui, additional, Zavorotinskaya, Tatiana, additional, Sun, Daqing, additional, Ye, Qiuping, additional, Jackson, Erica, additional, and Fantin, Valeria, additional

Published
2018
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49. 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, Mazurek, Anthony, additional, Dann, Stephen, additional, VanArsdale, Todd, additional, Fantin, Valeria, additional, Shields, David, additional, Siuzdak, Gary, additional, and Johnson, Caroline H., additional

Published
2018
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50. Abstract A133: Development of murine models to evaluate the impact of glucocorticoid receptor (GR) inhibition on chemotherapy response

Author

Jahchan, Nadine, primary, Zhou, Haiying, additional, Stice, James, additional, Kong, Wayne, additional, McWeeney, Dan, additional, Sun, Daqing, additional, Rew, Yosup, additional, Du, Xiaohui, additional, Zhu, Liusheng, additional, Ye, Qiuping, additional, Jackson, Erica L., additional, and Fantin, Valeria, additional

Published
2018
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