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

doi:10.1158/2159-8290.CD-16-1034

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Community

Back to search

Article

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

Cancer discovery - 1 May 2017

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

Abstract excerpt

Somatic gain-of-function mutations in isocitrate dehydrogenases (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...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Aminopyridines

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Antineoplastic Agents

Share to Cell Line, Tumor

Share to Isocitrate Dehydrogenase

Share to Leukemia, Myeloid, Acute

Share to Mice

Share to Triazines

Share to Xenograft Model Antitumor Assays

Source

Open in PubMed

Identifiers

PMID: 28193778
DOI: 10.1158/2159-8290.CD-16-1034

Genes

IDH2
IDH1

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations.PMID 28193778Read ↗

The role of mutant IDH1 and IDH2 inhibitors in the treatment of acute myeloid leukemia.Semantic proximity Read ↗

AG-221, a Small Molecule Mutant IDH2 Inhibitor, Remodels the Epigenetic State of IDH2-Mutant Cells and Induces Alterations in Self-Renewal/Differentiation in IDH2-Mutant AML Model in VivoSemantic proximity Read ↗

Optimizing Next-Generation AML Therapy: Activity of Mutant IDH2 Inhibitor AG-221 in Preclinical Models.Semantic proximity Read ↗

Biological Role and Therapeutic Potential of IDH Mutations in Cancer.Semantic proximity Read ↗

Isocitrate dehydrogenase (IDH) inhibition as treatment of myeloid malignancies: Progress and future directions.Semantic proximity Read ↗

Targeting IDH1 and IDH2 Mutations in Acute Myeloid Leukemia.Semantic proximity Read ↗

Targeting IDH1 and IDH2 Mutations in Acute Myeloid Leukemia: Emerging Options and Pending QuestionsSemantic proximity Read ↗

Targeting the IDH2 Pathway in Acute Myeloid Leukemia.Semantic proximity Read ↗

Targeting IDH Mutations in AML: Wielding the Double-edged Sword of Differentiation.Semantic proximity Read ↗

IDH mutations in cancer and progress toward development of targeted therapeutics.Semantic proximity Read ↗

IDH1 and IDH2 Mutations in Tumorigenesis: Mechanistic Insights and Clinical PerspectivesSemantic proximity Read ↗

(R)-2-Hydroxyglutarate Inhibits KDM5 Histone Lysine Demethylases to Drive Transformation in IDH-Mutant Cancers.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.