Article

H3B-8800, an Orally Bioavailable Modulator of the SF3b Complex, Shows Efficacy in Spliceosome-Mutant Myeloid Malignancies

2016-12-02

Abstract excerpt

Abstract Mutations in RNA splicing factors confer an alteration of function and are common in patients with myelodysplastic syndrome (MDS, ~45%), chronic myelomonocytic leukemia (CMML, ~60%), and acute myeloid leukemia (AML) derived from these conditions. Recent data suggest that spliceosome-mutant cells are preferentially sensitive to genetic or pharmacologic splicing modulation compared with wildtype (WT) counte...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work: 4a1de588-4969-5a2b-baa7-ed7457db6e4a
DOI: 10.1182/blood.v128.22.966.966

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

H3B-8800, an Orally Bioavailable Modulator of the SF3b Complex, Shows Efficacy in Spliceosome-Mutant Myeloid MalignanciesDOI 10.1182/blood.v128.22.966.966Read

H3B-8800, an orally available small-molecule splicing modulator, induces lethality in spliceosome-mutant cancers.Semantic proximity Read

SF3B1 mutation-mediated sensitization to H3B-8800 splicing inhibitor in chronic lymphocytic leukemia.Semantic proximity Read

Investigating the Molecular Mechanism of H3B-8800: A Splicing Modulator Inducing Preferential Lethality in Spliceosome-Mutant Cancers.Semantic proximity Read

Comprehensive Analyses of the Effects of the Small-Molecule Inhibitor of the UHM Domain in the Splicing Factor U2AF1 in Leukemia CellsSemantic proximity Read

The cryo-EM structure of the SF3b spliceosome complex bound to a splicing modulator reveals a pre-mRNA substrate competitive mechanism of action.Semantic proximity Read

Splicing modulators impair DNA damage response and induce killing of cohesin-mutant MDS/AMLSemantic proximity Read

E7820, an anti-cancer sulfonamide, degrades RBM39 in patients with splicing factor mutant myeloid malignancies: a phase II clinical trialSemantic proximity Read

Therapeutic approaches targeting splicing factor mutations in myelodysplastic syndromes and acute myeloid leukemia.Semantic proximity Read

Molecular Pathways: Understanding and Targeting Mutant Spliceosomal Proteins.Semantic proximity Read

Modulation of splicing catalysis for therapeutic targeting of leukemia with mutations in genes encoding spliceosomal proteins.Semantic proximity Read

Spliceosome Inhibition in <i>SF3B1</i>-Mutated Uveal MelanomaSemantic proximity Read

A Yeast-Based High-Throughput Screening Platform for the Discovery of Novel pre-mRNA Splicing ModulatorsSemantic proximity Read