F
Francesco G. Salituro
Researcher at Agios Pharmaceuticals
Publications - 45
Citations - 2804
Francesco G. Salituro is an academic researcher from Agios Pharmaceuticals. The author has contributed to research in topics: PKM2 & Pyruvate kinase. The author has an hindex of 16, co-authored 45 publications receiving 2414 citations.
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Journal ArticleDOI
Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation
Fang Wang,Jeremy Travins,Byron DeLaBarre,Virginie Penard-Lacronique,Virginie Penard-Lacronique,Virginie Penard-Lacronique,Stefanie Schalm,Erica Hansen,Kimberly Straley,Andrew Kernytsky,Wei Liu,Camelia Gliser,Hua Yang,Stefan Gross,Erin Artin,Véronique Saada,Elena Mylonas,Elena Mylonas,Elena Mylonas,Cyril Quivoron,Cyril Quivoron,Cyril Quivoron,Janeta Popovici-Muller,Jeffrey O. Saunders,Francesco G. Salituro,Shunqi Yan,Stuart Murray,Wentao Wei,Yi Gao,Lenny Dang,Marion Dorsch,Sam Agresta,David P. Schenkein,Scott A. Biller,Shinsan M. Su,Stéphane de Botton,Stéphane de Botton,Stéphane de Botton,Katharine E. Yen +38 more
TL;DR: Evidence is provided that inhibitors targeting mutant IDH2/R140Q could have potential applications as a differentiation therapy for cancer, and a small molecule, AGI-6780, that potently and selectively inhibits the tumor-associated mutant IDh2/ R140Q is developed.
Journal ArticleDOI
Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis.
Dimitrios Anastasiou,Yimin Yu,William J. Israelsen,Jian-kang Jiang,Matthew B. Boxer,Bum Soo Hong,Wolfram Tempel,Svetoslav Dimov,Min Shen,Abhishek K. Jha,Hua Yang,Katherine R. Mattaini,Christian M. Metallo,Brian P. Fiske,Kevin D. Courtney,Scott E. Malstrom,Tahsin M. Khan,Charles Kung,Amanda P. Skoumbourdis,Henrike Veith,Noel Southall,Martin J. Walsh,Kyle R. Brimacombe,William Leister,Sophia Y. Lunt,Zachary R. Johnson,Katharine E. Yen,Kaiko Kunii,Shawn M. Davidson,Heather R. Christofk,Christopher P. Austin,James Inglese,Marian H. Harris,John M. Asara,Gregory Stephanopoulos,Francesco G. Salituro,Shengfang Jin,Lenny Dang,Douglas S. Auld,Hee-Won Park,Lewis C. Cantley,Craig J. Thomas,Matthew G. Vander Heiden,Matthew G. Vander Heiden +43 more
TL;DR: It is shown that expression of PKM1, the pyruvate kinase isoform with high constitutive activity, or exposure to published small molecule PKM2 activators inhibit growth of xenograft tumors and support the notion that small molecule activation ofPKM2 can interfere with anabolic metabolism.
Journal ArticleDOI
AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations
Katharine E. Yen,Jeremy Travins,Fang Wang,Muriel D. David,Muriel D. David,Erin Artin,Kimberly Straley,Anil K. Padyana,Stefan Gross,Byron DeLaBarre,Erica Tobin,Yue Chen,Raj Nagaraja,Sung Choe,Lei Jin,Zenon D. Konteatis,Giovanni Cianchetta,Jeffrey O. Saunders,Francesco G. Salituro,Cyril Quivoron,Cyril Quivoron,Paule Opolon,Olivia Bawa,Véronique Saada,Véronique Saada,Angelo Paci,Sophie Broutin,Olivier Bernard,Olivier Bernard,Stéphane de Botton,Stéphane de Botton,Benoit S. Marteyn,Benoit S. Marteyn,Monika Pilichowska,Yingxia Xu,Cheng Fang,Fan Jiang,Wentao Wei,Shengfang Jin,Lee Silverman,Wei Liu,Hua Yang,Lenny Dang,Marion Dorsch,Virginie Penard-Lacronique,Virginie Penard-Lacronique,Scott A. Biller,Shin-San Michael Su +47 more
TL;DR: It is shown that the targeted inhibitor AG-221 suppresses the mutant IDH2 enzyme in multiple preclinical models and induces differentiation of malignant blasts, supporting its clinical development.
Journal ArticleDOI
Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers
Janeta Popovici-Muller,Lemieux Rene M,Erin Artin,Jeffrey O. Saunders,Francesco G. Salituro,Jeremy Travins,Giovanni Cianchetta,Zhenwei Cai,Ding Zhou,Cui Dawei,Ping Chen,Kimberly Straley,Erica Tobin,Fang Wang,Muriel D. David,Virginie Penard-Lacronique,Cyril Quivoron,Véronique Saada,Stéphane de Botton,Stefan Gross,Lenny Dang,Hua Yang,Luke Utley,Yue Chen,Hyeryun Kim,Shengfang Jin,Zhiwei Gu,Gui Yao,Zhiyong Luo,Xiaobing Lv,Cheng Fang,Liping Yan,Andrew J. Olaharski,Lee Silverman,Scott A. Biller,Shinsan M. Su,Katharine E. Yen +36 more
TL;DR: AG-120 (ivosidenib), an inhibitor of the IDH1 mutant enzyme that exhibits profound 2-HG lowering in tumor models and the ability to effect differentiation of primary patient AML samples ex vivo is reported.
Journal ArticleDOI
Small Molecule Activation of PKM2 in Cancer Cells Induces Serine Auxotrophy
Charles Kung,Jeff Hixon,Sung Choe,Kevin Marks,Stefan Gross,Erin Murphy,Byron DeLaBarre,Giovanni Cianchetta,Shalini Sethumadhavan,Xiling Wang,Shunqi Yan,Yi Gao,Cheng Fang,Wentao Wei,Fan Jiang,Shaohui Wang,Kevin Qian,Jeffrey O. Saunders,Ed Driggers,Hin Koon Woo,Kaiko Kunii,Stuart Murray,Hua Yang,Katharine E. Yen,Wei Liu,Lewis C. Cantley,Lewis C. Cantley,Matthew G. Vander Heiden,Matthew G. Vander Heiden,Shinsan M. Su,Shengfang Jin,Francesco G. Salituro,Lenny Dang +32 more
TL;DR: Induction of serine auxotrophy by PKM2 activation was accompanied by reduced carbon flow into the serine biosynthetic pathway and increased expression of high affinity serine transporters, supporting the hypothesis that PKM1 expression confers metabolic flexibility to cancer cells that allows adaptation to nutrient stress.