G
Giovanni Cianchetta
Researcher at Agios Pharmaceuticals
Publications - 28
Citations - 1730
Giovanni Cianchetta is an academic researcher from Agios Pharmaceuticals. The author has contributed to research in topics: PKM2 & Pyruvate kinase. The author has an hindex of 19, co-authored 28 publications receiving 1438 citations. Previous affiliations of Giovanni Cianchetta include University of Düsseldorf & Lexicon Pharmaceuticals.
Papers
More filters
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.
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: In this article, the authors reported the discovery of PKM2 activators with a unique allosteric binding mode, which resulted in a metabolic rewiring of cancer cells manifested by a profound dependency on the amino acid serine for continued cell proliferation.
Patent
Therapeutically active compounds and their methods of use
Giovanni Cianchetta,Byron DeLaBarre,Janeta Popovici-Muller,Francesco G. Salituro,Jeffrey O. Saunders,Jeremy Travins,Shunqi Yan,Tao Guo,Li Zhang +8 more
TL;DR: In this paper, the authors provide a list of compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need of a compound described herein, provided that the subject is a cancer patient.