An exon skipping screen identifies antitumor drugs that are potent modulators of pre-mRNA splicing, suggesting new therapeutic applications

Sensitivity to splicing modulation of BCL2 family genes defines cancer therapeutic strategies for splicing modulators

(2019) Daniel Aird et al.   Nature Communications

Inhibition of SF3B1 by molecules targeting the spliceosome results in massive aberrant exon skipping

(2018) Gang Wu et al.   RNA

USP39 Deubiquitinase Is Essential forKRASOncogene-driven Cancer

(2017) Julia M. Fraile et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The target landscape of clinical kinase drugs

(2017) Susan Klaeger et al.   SCIENCE

Mutant U2AF1-expressing cells are sensitive to pharmacological modulation of the spliceosome

(2017) Cara Lunn Shirai et al.   Nature Communications

Copy-number and gene dependency analysis reveals partial copy loss of wild-type SF3B1 as a novel cancer vulnerability

(2017) Brenton R Paolella et al.   eLife

Selectivity in Small Molecule Splicing Modulation

(2016) Deepak Kumar et al.   ACS Chemical Biology

Physiologic Expression of Sf3b1 K700E Causes Impaired Erythropoiesis, Aberrant Splicing, and Sensitivity to Therapeutic Spliceosome Modulation

(2016) Esther A. Obeng et al.   CANCER CELL

Therapeutic targeting of splicing in cancer

(2016) Stanley Chun-Wei Lee et al.   NATURE MEDICINE

Pharmacology of Modulators of Alternative Splicing

(2016) David O. Bates et al.   PHARMACOLOGICAL REVIEWS

Interchangeable SF3B1 inhibitors interfere with pre-mRNA splicing at multiple stages

(2016) Kerstin A. Effenberger et al.   RNA

Modulation of Alternative Splicing with Chemical Compounds in New Therapeutics for Human Diseases

(2015) Kenji Ohe et al.   ACS Chemical Biology

The promise and peril of chemical probes

(2015) Cheryl H Arrowsmith et al.   Nature Chemical Biology

Inhibitors of CLK Protein Kinases Suppress Cell Growth and Induce Apoptosis by Modulating Pre-mRNA Splicing

(2015) Shinsuke Araki et al.   PLoS One

Alternative splicing in cancer: implications for biology and therapy

(2014) J Chen et al.   ONCOGENE

A Pan-Cancer Analysis of Transcriptome Changes Associated with Somatic Mutations in U2AF1 Reveals Commonly Altered Splicing Events

(2014) Angela N. Brooks et al.   PLoS One

Identification of a Novel Function of CX-4945 as a Splicing Regulator

(2014) Hyeongki Kim et al.   PLoS One

Pyrido[2,3-d]pyrimidines: Discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors

(2013) Kevin Anderson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Optimization of Antitumor Modulators of Pre-mRNA Splicing

(2013) Chandraiah Lagisetti et al.   JOURNAL OF MEDICINAL CHEMISTRY

The spliceosome as a target of novel antitumour drugs

(2012) Sophie Bonnal et al.   NATURE REVIEWS DRUG DISCOVERY

Sudemycins, Novel Small Molecule Analogues of FR901464, Induce Alternative Gene Splicing

(2011) Liying Fan et al.   ACS Chemical Biology

Reduced fidelity of branch point recognition and alternative splicing induced by the anti-tumor drug spliceostatin A

(2011) A. Corrionero et al.   GENES & DEVELOPMENT

Recurrent mutations in the U2AF1 splicing factor in myelodysplastic syndromes

(2011) Timothy A Graubert et al.   NATURE GENETICS

Inhibition of Hepatitis C Virus Replication by a Specific Inhibitor of Serine-Arginine-Rich Protein Kinase

(2010) Y. Karakama et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth

(2010) B. W. Murray et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases

(2010) Kamil Paruch et al.   ACS Medicinal Chemistry Letters

The Spliceosome: Design Principles of a Dynamic RNP Machine

(2009) Markus C. Wahl et al.   CELL

Identification ofN,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor

(2009) Maria Gabriella Brasca et al.   JOURNAL OF MEDICINAL CHEMISTRY

Antitumor Activity and Pharmacology of a Selective Focal Adhesion Kinase Inhibitor, PF-562,271

(2008) W. G. Roberts et al.   CANCER RESEARCH