Small Molecule Modulators of Pre-mRNA Splicing in Cancer Therapy.

No abstract is available for this paper.

• Publication year

  2016

• Venue

  Trends in Molecular Medicine

• Publication date

  Unknown publication date

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.1016/j.molmed.2015.11.005PMID 26700537PMCID PMC4707101
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Aberrant RNA splicing in cancer; expression changes and driver mutations of splicing factor genes

  2016cited by this paper
• Transcriptome Sequencing Reveals Potential Mechanism of Cryptic 3’ Splice Site Selection in SF3B1-mutated Cancers

  2015cited by this paper
• Mechanisms and Regulation of Alternative Pre-mRNA Splicing.

  2015cited by this paper
• Inhibition of vemurafenib-resistant melanoma by interference with pre-mRNA splicing

  2015influential reference
• The Natural Product N-Palmitoyl-l-leucine Selectively Inhibits Late Assembly of Human Spliceosomes*

  2015cited by this paper
• The spliceosome is a therapeutic vulnerability in MYC-driven cancer

  2015influential reference
• MYC regulates the core pre-mRNA splicing machinery as an essential step in lymphomagenesis

  2015cited by this paper
• SF3B1 association with chromatin determines splicing outcomes.

  2015cited by this paper
• CD44 Acts as a Signaling Platform Controlling Tumor Progression and Metastasis

  2015cited by this paper
• Silent mutations make some noise.

  2014cited by this paper
• CD44v6 is a marker of constitutive and reprogrammed cancer stem cells driving colon cancer metastasis.

  2014cited by this paper
• Identification of Small Molecule Inhibitors of Pre-mRNA Splicing

  2014cited by this paper
• Splicing factor hnRNP A2 activates the Ras-MAPK-ERK pathway by controlling A-Raf splicing in hepatocellular carcinoma development

  2014cited by this paper
• Disruption of SF3B1 results in deregulated expression and splicing of key genes and pathways in myelodysplastic syndrome hematopoietic stem and progenitor cells

  2014cited by this paper
• Identification by high-throughput imaging of the histone methyltransferase EHMT2 as an epigenetic regulator of VEGFA alternative splicing

  2014influential reference
• A common alternative splicing signature is associated with SF3B1 mutations in malignancies from different cell lineages

  2014cited by this paper
• Bromodomain and extraterminal domain inhibitors (BETi) for cancer therapy: chemical modulation of chromatin structure.

  2014cited by this paper
• Total synthesis of 6-deoxypladienolide D and Assessment of Splicing Inhibitory Activity in a Mutant SF3B1 cancer cell line.

  2014cited by this paper
• Splicing factor mutations and cancer

  2014cited by this paper
• Regulation of HPV16 E6 and MCL1 by SF3B1 inhibitor in head and neck cancer cells

  2014cited by this paper
• The functional consequences of intron retention: alternative splicing coupled to NMD as a regulator of gene expression.

  2014cited by this paper
• Distinct iron architecture in SF3B1-mutant myelodysplastic syndrome patients is linked to an SLC25A37 splice variant with a retained intron

  2014cited by this paper
• Test-Firing Ammunition for Spliceosome Inhibition in Cancer

  2013cited by this paper
• S6K1 alternative splicing modulates its oncogenic activity and regulates mTORC1.

  2013cited by this paper
• High antitumor activity of pladienolide B and its derivative in gastric cancer

  2013cited by this paper
• Phase I Pharmacokinetic and Pharmacodynamic Study of the First-in-Class Spliceosome Inhibitor E7107 in Patients with Advanced Solid Tumors

  2013cited by this paper
• Optimization of antitumor modulators of pre-mRNA splicing.

  2013cited by this paper
• A High-Throughput Splicing Assay Identifies New Classes of Inhibitors of Human and Yeast Spliceosomes

  2013cited by this paper
• Correlation of CD44v6 expression with ovarian cancer progression and recurrence

  2013cited by this paper
• A phase I, open-label, single-arm, dose-escalation study of E7107, a precursor messenger ribonucleic acid (pre-mRNA) splicesome inhibitor administered intravenously on days 1 and 8 every 21 days to patients with solid tumors

  2013cited by this paper
• RNA therapeutics: beyond RNA interference and antisense oligonucleotides

  2012cited by this paper
• Psoromic Acid Derivatives: A New Family of Small‐Molecule Pre‐mRNA Splicing Inhibitors Discovered by a Stage‐Specific High‐Throughput in Vitro Splicing Assay

  2012cited by this paper
• The spliceosome as a target of novel antitumour drugs

  2012cited by this paper
• The cardiotonic steroid digitoxin regulates alternative splicing through depletion of the splicing factors SRSF3 and TRA2B.

  2012cited by this paper
• A Quantitative High-Throughput In Vitro Splicing Assay Identifies Inhibitors of Spliceosome Catalysis

  2012cited by this paper
• Deletion of the proline-rich region of the murine metastasis susceptibility gene Brd4 promotes epithelial-to-mesenchymal transition- and stem cell-like conversion.

  2011cited by this paper
• Small Molecule Amiloride Modulates Oncogenic RNA Alternative Splicing to Devitalize Human Cancer Cells

  2011cited by this paper
• RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)

  2011cited by this paper
• Identification of Evolutionarily Conserved Exons as Regulated Targets for the Splicing Activator Tra2β in Development

  2011cited by this paper
• Synthesis and Characterization of Pseudocantharidins, Novel Phosphatase Modulators That Promote the Inclusion of Exon 7 into the SMN (Survival of Motoneuron) pre-mRNA*

  2011cited by this paper
• Histone Deacetylase Activity Modulates Alternative Splicing

  2011cited by this paper
• Identification of SAP155 as the target of GEX1A (Herboxidiene), an antitumor natural product.

  2011influential reference
• Reduced fidelity of branch point recognition and alternative splicing induced by the anti-tumor drug spliceostatin A.

  2011influential reference
• The anti-tumor drug E7107 reveals an essential role for SF3b in remodeling U2 snRNP to expose the branch point-binding region.

  2011cited by this paper
• Sudemycins, novel small molecule analogues of FR901464, induce alternative gene splicing.

  2011cited by this paper
• Evaluation of FR901464 analogues in vitro and in vivo

  2011cited by this paper
• Rapid-Response Splicing Reporter Screens Identify Differential Regulators of Constitutive and Alternative Splicing

  2010cited by this paper
• Spliceostatin A inhibits spliceosome assembly subsequent to prespliceosome formation

  2010cited by this paper
• CD44, a therapeutic target for metastasising tumours.

  2010cited by this paper
• HnRNP proteins controlled by c-Myc deregulate pyruvate kinase mRNA splicing in cancer

  2010cited by this paper
• Modification of alternative splicing of Mcl-1 pre-mRNA using antisense morpholino oligonucleotides induces apoptosis in basal cell carcinoma cells.

  2009cited by this paper
• Meayamycin inhibits pre–messenger RNA splicing and exhibits picomolar activity against multidrug-resistant cells

  2009cited by this paper
• The spliceosome: design principles of a dynamic RNP machine.

  2009influential reference
• Bromodomain 4 activation predicts breast cancer survival

  2008cited by this paper
• A high-throughput screening strategy identifies cardiotonic steroids as alternative splicing modulators

  2008cited by this paper
• The Biflavonoid Isoginkgetin Is a General Inhibitor of Pre-mRNA Splicing

  2008cited by this paper
• Stalling of spliceosome assembly at distinct stages by small-molecule inhibitors of protein acetylation and deacetylation.

  2008cited by this paper
• Physico-chemical Properties and Structure Elucidation

  2008cited by this paper
• Splicing factor SF3b as a target of the antitumor natural product pladienolide

  2007influential reference
• The gene encoding the splicing factor SF2/ASF is a proto-oncogene

  2007cited by this paper
• Spliceostatin A targets SF3b and inhibits both splicing and nuclear retention of pre-mRNA

  2007cited by this paper
• A positive feedback loop couples Ras activation and CD44 alternative splicing.

  2006cited by this paper
• Isoginkgetin inhibits tumor cell invasion by regulating phosphatidylinositol 3-kinase/Akt–dependent matrix metalloproteinase-9 expression

  2006cited by this paper
• The spliceosome: a novel multi-faceted target for therapy.

  2005cited by this paper
• Selective modification of alternative splicing by indole derivatives that target serine-arginine-rich protein splicing factors.

  2005cited by this paper
• Pladienolides, new substances from culture of Streptomyces platensis Mer-11107. I. Taxonomy, fermentation, isolation and screening.

  2004cited by this paper
• Pladienolides, new substances from culture of Streptomyces platensis Mer-11107. III. In vitro and in vivo antitumor activities.

  2004cited by this paper
• Manipulation of Alternative Splicing by a Newly Developed Inhibitor of Clks*

  2004cited by this paper
• Identification of peptide inhibitors of pre-mRNA splicing derived from the essential interaction domains of CDC5L and PLRG1.

  2003cited by this paper
• GEX1 compounds, novel antitumor antibiotics related to herboxidiene, produced by Streptomyces sp. I. Taxonomy, production, isolation, physicochemical properties and biological activities.

  2002influential reference
• GEX1 compounds, novel antitumor antibiotics related to herboxidiene, produced by Streptomyces sp. II. The effects on cell cycle progression and gene expression.

  2002cited by this paper
• Enhanced expression of cyclin E and cyclin A in human hepatocellular carcinomas.

  2001cited by this paper
• Expression and role of Bcl‐xL in human hepatocellular carcinomas

  2001cited by this paper
• Over‐expression of cyclin a is highly associated with early relapse and reduced survival in patients with primary breast carcinomas

  2001cited by this paper
• Human STAGA Complex Is a Chromatin-Acetylating Transcription Coactivator That Interacts with Pre-mRNA Splicing and DNA Damage-Binding Factors In Vivo

  2001cited by this paper
• The sequence of the human genome (abstract only)

  2001cited by this paper
• Alternative splicing: increasing diversity in the proteomic world.

  2001cited by this paper
• Specific inhibition of serine- and arginine-rich splicing factors phosphorylation, spliceosome assembly, and splicing by the antitumor drug NB-506.

  2001cited by this paper
• Exon Skipping in Mcl-1 Results in a Bcl-2 Homology Domain 3 Only Gene Product That Promotes Cell Death*

  2000cited by this paper
• MCL-1S, a Splicing Variant of the Antiapoptotic BCL-2 Family Member MCL-1, Encodes a Proapoptotic Protein Possessing Only the BH3 Domain*

  2000cited by this paper
• BCL-X and the apoptotic machinery of lymphoma cells.

  1998cited by this paper
• New antitumor substances, FR901463, FR901464 and FR901465. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities.

  1997cited by this paper
• New antitumor substances, FR901463, FR901464 and FR901465. III. Structures of FR901463, FR901464 and FR901465.

  1997cited by this paper
• New Antitumor Substances, FR901463, FR901464 and FR901465

  1996cited by this paper
• New antitumor substances, FR901463, FR901464 and FR901465. II. Activities against experimental tumors in mice and mechanism of action.

  1996cited by this paper
• bcl-x, a bcl-2-related gene that functions as a dominant regulator of apoptotic cell death.

  1993influential reference
• Ser/Thr-specific protein phosphatases are required for both catalytic steps of pre-mRNA splicing.

  1992cited by this paper
• CD44 splice variants confer metastatic behavior in rats: homologous sequences are expressed in human tumor cell lines.

  1991cited by this paper
• A new variant of glycoprotein CD44 confers metastatic potential to rat carcinoma cells.

  1991cited by this paper
• Sequence the Human Genome

  1986cited by this paper

• Alternative Splicing in Lung Adenocarcinoma: From Bench to Bedside

  2025cites this paper
• CDC40 suppression induces CDCA5 splicing defects and anti-proliferative effects in lung cancer cells

  2025cites this paper
• Alternative splicing: from tumorigenesis to neoantigen-mediated cancer immunotherapy

  2025cites this paper
• Nano-conjugation of small molecule modulators of protein aggregation: Enhancing the therapeutic precision.

  2025cites this paper
• The competition between splicing and 3′ processing shapes the human transcriptome

  2025cites this paper
• Discovery of RNA‐Targeting Small Molecules: Challenges and Future Directions

  2025cites this paper
• MicroRNA biogenesis is broadly disrupted by inhibition of the splicing factor SF3B1

  2024cites this paper
• N-Benzylated 5-Hydroxybenzothiophene-2-carboxamides as Multi-Targeted Clk/Dyrk Inhibitors and Potential Anticancer Agents

  2024cites this paper
• Genomic deletions explain the generation of alternative BRAF isoforms conferring resistance to MAPK inhibitors in melanoma.

  2024cites this paper
• A common cellular response to broad splicing perturbations is characterized by metabolic transcript downregulation driven by the Mdm2–p53 axis

  2024cites this paper
• Small molecules modulating RNA splicing: a review of targets and future perspectives.

  2024cites this paper
• Modification of BCLX pre-mRNA splicing has antitumor efficacy alone or in combination with radiotherapy in human glioblastoma cells

  2024cites this paper
• Perturbation of mRNA splicing in liver cancer: insights, opportunities and challenges

  2024cites this paper
• Generation of Transcript Length Variants and Reprogramming of mRNA Splicing During Atherosclerosis Progression in ApoE-Deficient Mice

  2024cites this paper
• Generation of tumor neoantigens by RNA splicing perturbation.

  2024cites this paper
• Alternative Splicing in Glioblastoma and its Clinical Implication in Outcome Prediction.

  2024cites this paper
• Alternative Splicing Landscape of Head and Neck Squamous Cell Carcinoma

  2024cites this paper
• Azaindole derivatives as potential kinase inhibitors and their SARs elucidation.

  2023cites this paper
• Eukaryotic splicing machinery in the plant–virus battleground

  2023cites this paper
• Aberrant Cyclin D1 splicing in cancer: from molecular mechanism to therapeutic modulation

  2023cites this paper
• Chemistry, structure and function of approved oligonucleotide therapeutics

  2023cites this paper
• Splicing factor SNRPA associated with microvascular invasion promotes hepatocellular carcinoma metastasis through activating NOTCH1/Snail pathway and is mediated by circSEC62/miR‐625‐5p axis

  2023cites this paper
• Genetically engineered mouse models for hereditary cancer syndromes

  2023cites this paper
• Cardiac splicing as a diagnostic and therapeutic target

  2023cites this paper
• Development of novel conformationally restricted selective Clk1/4 inhibitors through creating an intramolecular hydrogen bond involving an imide linker.

  2022cites this paper
• Splicing deregulation, microRNA and notch aberrations: fighting the three-headed dog to overcome drug resistance in malignant mesothelioma

  2022cites this paper
• Alternative Splicing in Cancer and Immune Cells

  2022cites this paper
• Alternative RNA Splicing Defects in Pediatric Cancers: New Insights in Tumorigenesis and Potential Therapeutic Vulnerabilities.

  2022cites this paper
• Discovery of novel 5-methoxybenzothiophene hydrazides as metabolically stable Clk1 inhibitors with high potency and unprecedented Clk1 isoenzyme selectivity.

  2022cites this paper
• Structure-based drug design with geometric deep learning

  2022cites this paper
• Medical Swimming Cellbots

  2022cites this paper
• Emerging Gene Manipulation Strategies for the Treatment of Monogenic Eye Disease

  2022cites this paper
• Targeting the "undruggable": RNA-binding proteins in the spotlight in cancer therapy.

  2022cites this paper
• VEGFA’s distal enhancer regulates its alternative splicing in CML

  2021cites this paper
• Coumarins and Gastrointestinal Cancer: A New Therapeutic Option?

  2021cites this paper
• Modulation of SF3B1 in the pre-mRNA spliceosome induces a RIG-I-dependent type I IFN response

  2021cites this paper
• Systematic Profiling of mRNA Splicing Reveals the Prognostic Predictor and Potential Therapeutic Target for Glioblastoma Multiforme

  2021cites this paper
• Structural basis of intron selection by U2 snRNP in the presence of covalent inhibitors

  2021cites this paper
• Requirement of splicing factor hnRNP A2B1 for tumorigenesis of melanoma stem cells

  2021cites this paper
• Genome-Wide Profiling of Alternative Splicing Signatures Associated with Prognosis and Immune Microenvironment of Hepatocellular Carcinoma

  2021cites this paper
• Impact of Alternative Splicing Variants on Liver Cancer Biology

  2021cites this paper
• Therapeutic Targeting of Alternative RNA Splicing in Gastrointestinal Malignancies and Other Cancers

  2021cites this paper
• Selective therapeutic benefit of X-rays and inhibitors of EGFR, PI3K/mTOR, and Bcl-2 in breast, lung, and cervical cancer cells.

  2021cites this paper
• SF3B1 modulators affect key genes in metastasis and drug influx: a new approach to fight pancreatic cancer chemoresistance

  2021cites this paper
• The Regulatory Role of RNA Metabolism Regulator TDP-43 in Human Cancer

  2021cites this paper
• Impact of alternative splicing on mechanisms of resistance to anticancer drugs.

  2021cites this paper
• Identification of heterogeneous nuclear ribonucleoprotein as a candidate biomarker for diagnosis and prognosis of hepatocellular carcinoma.

  2021cites this paper
• Total Syntheses of Pladienolide-Derived Spliceosome Modulators

  2021cites this paper
• The splicing regulatory factor hnRNPU is a novel transcriptional target of c‐Myc in hepatocellular carcinoma

  2020cites this paper
• Cell Biology International

  2020influential citation
• Clinical and functional significance of CHK1-S, an alternatively spliced isoform of the CHK1 gene, in hepatocellular carcinoma

  2020cites this paper
• Splice Modulation Synergizes Cell Cycle Inhibition.

  2020cites this paper
• Systemic Analysis of RNA Alternative Splicing Signals Related to the Prognosis for Head and Neck Squamous Cell Carcinoma

  2020cites this paper
• Chemical Modulation of Pre-mRNA Splicing in Mammalian Systems.

  2020cites this paper
• Systemic Analysis of the Prognosis-Related RNA Alternative Splicing Signals in Melanoma

  2020cites this paper
• Identification of survival-associated alternative splicing events and signatures in adrenocortical carcinoma based on TCGA SpliceSeq data

  2020cites this paper
• Targeting the spliceosome machinery: A new therapeutic axis in cancer?

  2020cites this paper
• Prognostic alternative splicing signature in cervical squamous cell carcinoma.

  2020cites this paper
• Chemoresistance-associated alternative splicing signatures in serous ovarian cancer.

  2020cites this paper
• Hallmarks of Splicing Defects in Cancer: Clinical Applications in the Era of Personalized Medicine

  2020cites this paper
• Silencing Core Spliceosome Sm Gene Expression Induces a Cytotoxic Splicing Switch in the Proteasome Subunit Beta 3 mRNA in Non-Small Cell Lung Cancer Cells

  2020cites this paper
• The Roles of Alternative Splicing in Tumor-immune Cell Interactions

  2020cites this paper
• LncRNA NR_030777 Alleviates Paraquat-induced Neurotoxicity by Regulating Zfp326 and Cpne5.

  2020cites this paper
• Features of alternative splicing in stomach adenocarcinoma and their clinical implication: a research based on massive sequencing data

  2020cites this paper
• RNA Splicing: Basic Aspects Underlie Antitumor Targeting.

  2020cites this paper
• Splicing to Keep Cycling: The Importance of Pre-mRNA Splicing during the Cell Cycle.

  2020cites this paper
• Identification of Survival-Associated Alternative Splicing Signatures in Lung Squamous Cell Carcinoma

  2020cites this paper
• An interactive network of alternative splicing events with prognostic value in geriatric lung adenocarcinoma via the regulation of splicing factors

  2020cites this paper
• A Comprehensive Overview of Structure‐Activity Relationships of Small‐Molecule Splicing Modulators Targeting SF3B1 as Anticancer Agents

  2020cites this paper
• Clusterization in acute myeloid leukemia based on prognostic alternative splicing signature to reveal the clinical characteristics in the bone marrow microenvironment

  2020cites this paper
• Aberrant RNA Splicing Events Driven by Mutations of RNA-Binding Proteins as Indicators for Skin Cutaneous Melanoma Prognosis

  2020cites this paper
• Modification of Mcl-1 alternative splicing induces apoptosis and suppresses tumor proliferation in gastric cancer

  2020cites this paper
• The role of alternative splicing in cancer: From oncogenesis to drug resistance.

  2020cites this paper
• Targeting RNA-binding proteins in acute and chronic leukemia

  2020cites this paper
• Requirement of splicing factor hnRNP A2B1 of hnRNPs for tumorigenesis of melanoma stem cells

  2020cites this paper
• Prognostic alternative mRNA splicing signature in hepatocellular carcinoma: a study based on large-scale sequencing data.

  2019cites this paper
• Survival-Associated Alternative Messenger RNA Splicing Signatures in Pancreatic Ductal Adenocarcinoma: A Study Based on RNA-Sequencing Data

  2019cites this paper
• Identification of prognosis‐related alternative splicing events in kidney renal clear cell carcinoma

  2019cites this paper
• Construction of a model to predict the prognosis of patients with cholangiocarcinoma using alternative splicing events

  2019cites this paper
• Advanced Evanescent-Wave Optical Biosensors for the Detection of Nucleic Acids: An Analytic Perspective

  2019cites this paper
• Circular RNAs and RNA Splice Variants as Biomarkers for Prognosis and Therapeutic Response in the Liquid Biopsies of Lung Cancer Patients

  2019cites this paper
• Destabilization of the human RED–SMU1 splicing complex as a basis for host-directed antiinfluenza strategy

  2019cites this paper
• Structures of SF3b1 reveal a dynamic Achilles heel of spliceosome assembly: Implications for cancer-associated abnormalities and drug discovery.

  2019cites this paper
• Systematic analysis of alternative splicing signature unveils prognostic predictor for kidney renal clear cell carcinoma

  2019cites this paper
• Prognostic index of aberrant mRNA splicing profiling acts as a predictive indicator for hepatocellular carcinoma based on TCGA SpliceSeq data

  2019cites this paper
• Systematic analysis of survival‐associated alternative splicing signatures in clear cell renal cell carcinoma

  2019cites this paper
• Licocoumarone induces BxPC-3 pancreatic adenocarcinoma cell death by inhibiting DYRK1A.

  2019cites this paper
• Uncovering the signaling landscape controlling breast cancer cell migration identifies novel metastasis driver genes

  2019cites this paper
• DIS3L2 promotes progression of hepatocellular carcinoma via hnRNP U-mediated alternative splicing.

  2019cites this paper
• Systematic analysis of survival‐associated alternative splicing signatures uncovers prognostic predictors for head and neck cancer

  2019cites this paper
• Altered splicing and cytoplasmic levels of tRNA synthetases in SF3B1-mutant myelodysplastic syndromes as a therapeutic vulnerability

  2019cites this paper
• Food-Derived Compounds Apigenin and Luteolin Modulate mRNA Splicing of Introns with Weak Splice Sites

  2019cites this paper
• Emerging Therapeutic Opportunities Based on Current Knowledge of Uveal Melanoma Biology

  2019cites this paper
• Alternative splicing, RNA-seq and drug discovery.

  2019cites this paper
• Prognostic Signature of Alternative Splicing Events in Bladder Urothelial Carcinoma Based on Spliceseq Data from 317 Cases

  2018cites this paper
• Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics.

  2018cites this paper
• Therapy-induced stress response is associated with downregulation of pre-mRNA splicing in cancer cells

  2018cites this paper
• Small-molecule flunarizine increases SMN protein in nuclear Cajal bodies and motor function in a mouse model of spinal muscular atrophy

  2018cites this paper
• Anti‐tumor efficacy of a novel CLK inhibitor via targeting RNA splicing and MYC‐dependent vulnerability

  2018cites this paper
• Alternative pre‐mRNA splicing

  2018cites this paper