Supplementary Tables 1 - 8 from AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations

Autor: Shin-San Michael Su, Scott A. Biller, Virginie Penard-Lacronique, Marion Dorsch, Lenny Dang, Hua Yang, Wei Liu, Lee Silverman, Shengfang Jin, Wentao Wei, Fan Jiang, Cheng Fang, YingXia Xu, Monika Pilichowska, Benoît S. Marteyn, Stéphane de Botton, Olivier A. Bernard, Sophie Broutin, Angelo Paci, Véronique Saada, Olivia Bawa, Paule Opolon, Cyril Quivoron, Francesco G. Salituro, Jeffrey O. Saunders, Giovanni Cianchetta, Zenon Konteatis, Lei Jin, Sung Choe, Raj Nagaraja, Yue Chen, Erica Tobin, Byron DeLaBarre, Stefan Gross, Anil Padyana, Kimberly Straley, Erin Artin, Muriel D. David, Fang Wang, Jeremy Travins, Katharine Yen

Supplementary Table 1. Drug metabolism and pharmacokinetic attributes of AG-221. Supplementary Table 2. Selectivity of AG-221 confirmed by testing against a panel of kinases. Supplementary Table 3. Clinical characteristics of patients with IDH2R140Q-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9bd472a11c8ff29b3f26438ea494ea5d
https://doi.org/10.1158/2159-8290.22531936

Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma

Autor: Brandon Nicolay, Ingo K. Mellinghoff, Paolo Codega, Hua Yang, Zenon D. Konteatis, Janeta Popovici-Muller, Katharine E. Yen, Rohini Narayaraswamy, Raj Nagaraja, Zhihua Sui, Shinsan M. Su, Erin Artin, Kimberly Straley, Zhenwei Cai, Feng Wang, Shuilong Tong, Lei Jin, Yue Chen, Cui Dawei, Carl Campos, Zhiyong Luo, Cheng Fang, Xiaobing Lv, Lenny Dang, Ding Zhou, Anil K. Padyana, Huachun Tang, Scott A. Biller

Publikováno v: ACS Medicinal Chemistry Letters

Inhibitors of mutant isocitrate dehydrogenase (mIDH) 1 and 2 cancer-associated enzymes prevent the accumulation of the oncometabolite d-2-hydroxyglutarate (2-HG) and are under clinical investigation for the treatment of several cancers harboring an I

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::43b32007fc702636fdd2a4b9ade51afa
https://doi.org/10.1021/acsmedchemlett.9b00509

Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers

Autor: Hua Yang, Muriel D. David, Jeffrey O. Saunders, Lemieux Rene M, Gui Yao, Luke Utley, Véronique Saada, Xiaobing Lv, Yue Chen, Fang Wang, Shengfang Jin, Ping Chen, Erin Artin, Stéphane de Botton, Cheng Fang, Hyeryun Kim, Giovanni Cianchetta, Stefan Gross, Lenny Dang, Zhenwei Cai, Scott A. Biller, Andrew J. Olaharski, Erica Tobin, Cui Dawei, Katharine E. Yen, Virginie Penard-Lacronique, Liping Yan, Ding Zhou, Lee Silverman, Cyril Quivoron, Zhiyong Luo, Jeremy Travins, Janeta Popovici-Muller, Shinsan M. Su, Kimberly Straley, Zhiwei Gu, Francesco G. Salituro

Publikováno v: ACS Medicinal Chemistry Letters

Somatic point mutations at a key arginine residue (R132) within the active site of the metabolic enzyme isocitrate dehydrogenase 1 (IDH1) confer a novel gain of function in cancer cells, resulting in the production of d-2-hydroxyglutarate (2-HG), an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc0eaa35709cac29ca18fde3960dca69
https://doi.org/10.1021/acsmedchemlett.7b00421

A small molecule inhibitor of mutant IDH2 rescues cardiomyopathy in a D-2-hydroxyglutaric aciduria type II mouse model

Autor: Gajja S. Salomons, Yong Cang, Scott A. Biller, Hua Yang, Josh Powe, Dongwei Zhu, Stefan Gross, Stuart Murray, Kimberly Straley, Samuel V. Agresta, Karen S. Regan, Katharine E. Yen, Yaguang Si, Mya Steadman, Wei Liu, Lenny Dang, Ana Pop, Yue Chen, Erin Artin, Marion Dorsch, Jeremy Travins, Stephanie Santiago, Shengfang Jin, Muriel D. David, Cyril Quivoron, Andrew Kernytsky, Virginie Penard-Lacronique, Lee Silverman, Chenming Lu, Shin San Michael Su, Zhizhong Lin, Erwin E.W. Jansen, Fang Wang, Eduard A. Struys

Publikováno v: Journal of Inherited Metabolic Disease
Journal of Inherited Metabolic Disease, 39(6), 807-820. Springer Netherlands
Wang, F, Travins, J, Lin, Z, Si, Y, Chen, Y, Powe, J, Murray, S, Zhu, D, Artin, E, Gross, S, Santiago, S, Steadman, M, Kernytsky, A, Straley, K, Lu, C, Pop, A, Struys, E A, Jansen, E E W, Salomons, G S, David, M D, Quivoron, C, Penard-Lacronique, V, Regan, K S, Liu, W, Dang, L, Yang, H, Silverman, L, Agresta, S, Dorsch, M, Biller, S, Yen, K, Cang, Y, Su, S S M & Jin, S 2016, ' A small molecule inhibitor of mutant IDH2 rescues cardiomyopathy in a D-2-hydroxyglutaric aciduria type II mouse model ', Journal of Inherited Metabolic Disease, vol. 39, no. 6, pp. 807-820 . https://doi.org/10.1007/s10545-016-9960-y

D-2-hydroxyglutaric aciduria (D2HGA) type II is a rare neurometabolic disorder caused by germline gain-of-function mutations in isocitrate dehydrogenase 2 (IDH2), resulting in accumulation of D-2-hydroxyglutarate (D2HG). Patients exhibit a wide spect

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http://europepmc.org/articles/PMC5065612

Biochemical, Cellular, and Biophysical Characterization of a Potent Inhibitor of Mutant Isocitrate Dehydrogenase IDH1

Autor: Zhuyin Li, Anton Simeonov, Douglas S. Auld, Lenny Dang, Mindy I. Davis, Rajan Pragani, Erin Artin, Min Shen, Matthew B. Boxer, Janeta Popovici-Muller, Kimberly Straley, Wendy A. Lea, Natasha Thorne, Byron DeLaBarre, Stefan Gross

Publikováno v: Journal of Biological Chemistry. 289:13717-13725

Two mutant forms (R132H and R132C) of isocitrate dehydrogenase 1 (IDH1) have been associated with a number of cancers including glioblastoma and acute myeloid leukemia. These mutations confer a neomorphic activity of 2-hydroxyglutarate (2-HG) product

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e376e467bd08b4ee964f82f3fa066e4b
https://doi.org/10.1074/jbc.m113.511030