Scientific Literature

Feb 13, 2017

AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations

K. Yen, J. Travins, F. Wang, M. D. David, E. Artin, K. Straley, A. Padyana, S. Gross, B. DeLaBarre, E. Tobin, Y. Chen, R. Nagaraja, S. Choe, L. Jin, Z. Konteatis, G. Cianchetta, J. O. Saunders, F. G. Salituro, C. Quivoron, P. Opolon, O. Bawa, V. Saada, A. Paci, S. Broutin, O. A. Bernard, S. de Botton, B. S. Marteyn, M. Pilichowska, Y. Xu, C. Fang, F. Jiang, W. Wei, S. Jin, L. Silverman, W. Liu, H. Yang, L. Dang, M. Dorsch, V. Penard-Lacronique, S. A. Biller, S.-S. M. Su , Cancer Discovery , DOI: 10.1158/2159-8290.CD-16-1034
Somatic gain-of-function mutations in isocitrate dehydrogenase (IDH) 1 and 2 are found in multiple hematologic and solid tumors, leading to accumulation of the oncometabolite, (R)-2-hydroxyglutarate (2HG). 2HG competitively inhibits α-ketoglutarate-dependent dioxygenases, including histone demethylases and methylcytosine dioxygenases of the Tet family, causing epigenetic dysregulation and a block in cellular differentiation....
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Feb 13, 2017

AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations

K. Yen, J. Travins, F. Wang, M. D. David, E. Artin, K. Straley, A. Padyana, S. Gross, B. DeLaBarre, E. Tobin, Y. Chen, R. Nagaraja, S. Choe, L. Jin, Z. Konteatis, G. Cianchetta, J. O. Saunders, F. G. Salituro, C. Quivoron, P. Opolon, O. Bawa, V. Saada, A. Paci, S. Broutin, O. A. Bernard, S. de Botton, B. S. Marteyn, M. Pilichowska, Y. Xu, C. Fang, F. Jiang, W. Wei, S. Jin, L. Silverman, W. Liu, H. Yang, L. Dang, M. Dorsch, V. Penard-Lacronique, S. A. Biller, S.- S. M. Su , Cancer Discovery , DOI: 10.1158/2159-8290.CD-16-1034
Somatic gain-of-function mutations in isocitrate dehydrogenase (IDH) 1 and 2 are found in multiple hematologic and solid tumors, leading to accumulation of the oncometabolite, (R)-2-hydroxyglutarate (2HG). 2HG competitively inhibits α-ketoglutarate-dependent dioxygenases, including histone demethylases and methylcytosine dioxygenases of the Tet family, causing epigenetic dysregulation and a block in cellular differentiation....
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Feb 11, 2017

Comparative Study of Xenobiotic-free Media for the Cultivation of Human Limbal Epithelial Stem/Progenitor Cells

Dr. S. Gonzalez, Dr. L. Chen, Dr. S. X. Deng , Tissue Engineering Part C: Methods , DOI:10.1089/ten.TEC.2016.0388
The culture of human limbal epithelial stem/progenitor cells (LSCs) in the presence of animal components poses the risk of cross-species contamination in clinical applications. We quantitatively compared different xenobiotic-free culture media for the cultivation of human LSCs. LSCs were cultured from 2x2 mm limbal tissue explants on denuded human amniotic...
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Feb 11, 2017

Comparative Study of Xenobiotic-free Media for the Cultivation of Human Limbal Epithelial Stem/Progenitor Cells

S. Gonzalez, L. Chen, S. X. Deng , Tissue Engineering Part C: Methods , DOI:10.1089/ten.TEC.2016.0388
The culture of human limbal epithelial stem/progenitor cells (LSCs) in the presence of animal components poses the risk of cross-species contamination in clinical applications. We quantitatively compared different xenobiotic-free culture media for the cultivation of human LSCs. LSCs were cultured from 2 × 2 mm limbal tissue explants on denuded...
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Feb 4, 2017

First-in-human studies of seletalisib, an orally bioavailable small-molecule PI3Kδ inhibitor for the treatment of immune and inflammatory diseases

E. Helmer, M. Watling, E. Jones, D. Tytgat, M. Jones, R. Allen, A. Payne, A. Koch, E. Healy , European Journal of Clinical Pharmacology , DOI: 10.1007/s00228-017-2205-7
Purpose: PI3Ks are potential therapeutic targets in immune-inflammatory diseases. These studies aimed to investigate the safety, tolerability and PK profile of seletalisib, a selective inhibitor of PI3Kδ in humans.Methods: These phase I, randomised, double-blind, placebo-controlled, single-centre studies (NCT02303509, NCT02207595) evaluated single and multiple oral doses of seletalisib (5–90 mg QD and...
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