Screening Approaches for Targeting Ribonucleoprotein Complexes: A New Dimension for Drug Discovery

Measuring RNA–Ligand Interactions with Microscale Thermophoresis

(2018) Michelle H. Moon et al.   BIOCHEMISTRY

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

(2018) Lorenzo I. Finci et al.   GENES & DEVELOPMENT

Interfering with HuR–RNA Interaction: Design, Synthesis and Biological Characterization of Tanshinone Mimics as Novel, Effective HuR Inhibitors

(2018) Leonardo Manzoni et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pathomechanisms of TDP-43 in neurodegeneration

(2018) Ju Gao et al.   JOURNAL OF NEUROCHEMISTRY

Thermophoresis for characterizing biomolecular interaction

(2018) Mufarreh Asmari et al.   METHODS

The PPARγ agonist rosiglitazone sensitizes the BH3 mimetic (−)-gossypol to induce apoptosis in cancer cells with high level of Bcl-2

(2018) Xinzhe Li et al.   MOLECULAR CARCINOGENESIS

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

(2018) Michael Seiler et al.   NATURE MEDICINE

Principles for targeting RNA with drug-like small molecules

(2018) Katherine Deigan Warner et al.   NATURE REVIEWS DRUG DISCOVERY

A brave new world of RNA-binding proteins

(2018) Matthias W. Hentze et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Small-Molecule Inhibitors Disrupt let-7 Oligouridylation and Release the Selective Blockade of let-7 Processing by LIN28

(2018) Longfei Wang et al.   Cell Reports

Gossypol Inhibits Non-small Cell Lung Cancer Cells Proliferation by Targeting EGFRL858R/T790M

(2018) Yuwei Wang et al.   Frontiers in Pharmacology

Anti-inflammatory Effects of Gossypol on Human Lymphocytic Jurkat Cells via Regulation of MAPK Signaling and Cell Cycle

(2018) Chien-Wei Chen et al.   INFLAMMATION

Discovery of BAZ2A bromodomain ligands

(2017) Dimitrios Spiliotopoulos et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The role of RNA-binding protein tristetraprolin in cancer and immunity

(2017) Jian Guo et al.   MEDICAL ONCOLOGY

Integrated structural biology to unravel molecular mechanisms of protein-RNA recognition

(2017) Andreas Schlundt et al.   METHODS

Gossypol induces cell death by activating apoptosis and autophagy in HT-29 cells

(2017) Ming-Dong Lu et al.   Molecular Medicine Reports

Structural Insight into the Recognition of r(UAG) by Musashi-1 RBD2, and Construction of a Model of Musashi-1 RBD1-2 Bound to the Minimum Target RNA

(2017) Ryo Iwaoka et al.   MOLECULES

Regulation of HuR structure and function by dihydrotanshinone-I

(2017) Preet Lal et al.   NUCLEIC ACIDS RESEARCH

Therapeutic targeting of RNA splicing in myelodysplasia

(2017) Young Joon Kim et al.   SEMINARS IN HEMATOLOGY

Overexpression of Musashi-1 protein is associated with progression and poor prognosis of gastric cancer

(2017) Zhangxuan Shou et al.   Oncology Letters

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

(2017) Cara Lunn Shirai et al.   Nature Communications

LIN28 Zinc Knuckle Domain Is Required and Sufficient to Induce let-7 Oligouridylation

(2017) Longfei Wang et al.   Cell Reports

The LIN28/let-7 Pathway in Cancer

(2017) Julien Balzeau et al.   Frontiers in Genetics

Applying a high-throughput fluorescence polarization assay for the discovery of chemical probes blocking La:RNA interactions in vitro and in cells

(2017) Gunhild Sommer et al.   PLoS One

Natural Product Gossypol and its Derivatives in Precision Cancer Medicine

(2017) Yun Zeng et al.   CURRENT MEDICINAL CHEMISTRY

High-Throughput Fragment Docking into the BAZ2B Bromodomain: Efficient in Silico Screening for X-Ray Crystallography

(2016) Graziano Lolli et al.   ACS Chemical Biology

A Small-Molecule Inhibitor of Lin28

(2016) Martina Roos et al.   ACS Chemical Biology

Targeting transcription factors by small compounds—Current strategies and future implications

(2016) Judith Hagenbuchner et al.   BIOCHEMICAL PHARMACOLOGY

Sensing of biomolecular interactions using fluorescence complementing systems in living cells

(2016) Xian-En Zhang et al.   BIOSENSORS & BIOELECTRONICS

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

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

Discovery of Dual Inhibitors of MDM2 and XIAP for Cancer Treatment

(2016) Lubing Gu et al.   CANCER CELL

The Ribonucleic Complex HuR-MALAT1 Represses CD133 Expression and Suppresses Epithelial-Mesenchymal Transition in Breast Cancer

(2016) E. Latorre et al.   CANCER RESEARCH

Discovery of the first small-molecule CsrA–RNA interaction inhibitors using biophysical screening technologies

(2016) Christine K Maurer et al.   Future Medicinal Chemistry

RNA regulation went wrong in neurodevelopmental disorders: The example of Msi/Elavl RNA binding proteins

(2016) Masato Yano et al.   INTERNATIONAL JOURNAL OF DEVELOPMENTAL NEUROSCIENCE

Musashi-2 is a novel regulator of paclitaxel sensitivity in ovarian cancer cells

(2016) Jeongsuk Lee et al.   INTERNATIONAL JOURNAL OF ONCOLOGY

Derivatives of 3-Amino-2-methylpyridine as BAZ2B Bromodomain Ligands: In Silico Discovery and in Crystallo Validation

(2016) Jean-Rémy Marchand et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Small-Molecule Inhibitor of Protein–MicroRNA Interaction Using Binding Assay with a Site-Specifically Labeled Lin28

(2016) Donghyun Lim et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Molecular Architecture of SF3b and Structural Consequences of Its Cancer-Related Mutations

(2016) Constantin Cretu et al.   MOLECULAR CELL

Musashi-2 attenuates AHR signalling to expand human haematopoietic stem cells

(2016) Stefan Rentas et al.   NATURE

Targeting renal cell carcinoma with a HIF-2 antagonist

(2016) Wenfang Chen et al.   NATURE

Genomic analyses identify molecular subtypes of pancreatic cancer

(2016) Peter Bailey et al.   NATURE

Modulation of splicing catalysis for therapeutic targeting of leukemia with mutations in genes encoding spliceosomal proteins

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

Therapeutic targeting of splicing in cancer

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

Musashi RNA-binding protein 2 regulates estrogen receptor 1 function in breast cancer

(2016) M-H Kang et al.   ONCOGENE

Identification of small molecule inhibitors of the Lin28-mediated blockage of pre-let-7g processing

(2016) Helen L. Lightfoot et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Discovery of Novel Small Molecule Inhibitors of VEGF Expression in Tumor Cells Using a Cell-Based High Throughput Screening Platform

(2016) Liangxian Cao et al.   PLoS One

Musashi-2 (MSI2) supports TGF-β signaling and inhibits claudins to promote non-small cell lung cancer (NSCLC) metastasis

(2016) Alexander E. Kudinov et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structure of a yeast activated spliceosome at 3.5 A resolution

(2016) C. Yan et al.   SCIENCE

Tristetraprolin as a Therapeutic Target in Inflammatory Disease

(2016) Sonika Patial et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Identification and Validation of Novel Small Molecule Disruptors of HuR-mRNA Interaction

(2015) Xiaoqing Wu et al.   ACS Chemical Biology

Musashi Signaling in Stem Cells and Cancer

(2015) Raymond G. Fox et al.   Annual Review of Cell and Developmental Biology

Comprehensive Molecular Portraits of Invasive Lobular Breast Cancer

(2015) Giovanni Ciriello et al.   CELL

Targeting the Multifaceted HuR Protein, Benefits and Caveats

(2015) Chiara Zucal et al.   CURRENT DRUG TARGETS

B Cell–Intrinsic Expression of the HuR RNA-Binding Protein Is Required for the T Cell–Dependent Immune Response In Vivo

(2015) Amy DeMicco et al.   JOURNAL OF IMMUNOLOGY

New Frontiers in Druggability

(2015) Dima Kozakov et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of recurrent regulated alternative splicing events across human solid tumors

(2015) Miri Danan-Gotthold et al.   NUCLEIC ACIDS RESEARCH

Musashi-2 Silencing Exerts Potent Activity against Acute Myeloid Leukemia and Enhances Chemosensitivity to Daunorubicin

(2015) Yixiang Han et al.   PLoS One

Correlation of Musashi-1, Lgr5, and pEGFR expressions in human small intestinal adenocarcinomas

(2015) Yan Wang et al.   TUMOR BIOLOGY

Dihydrotanshinone-I interferes with the RNA-binding activity of HuR affecting its post-transcriptional function

(2015) Vito Giuseppe D’Agostino et al.   Scientific Reports

Widespread intron retention diversifies most cancer transcriptomes

(2015) Heidi Dvinge et al.   Genome Medicine

Ligand induced stabilization of the melting temperature of the HSV-1 single-strand DNA binding protein using the thermal shift assay

(2014) Kanchi Ravi Rupesh et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Lin28b Is Sufficient to Drive Liver Cancer and Necessary for Its Maintenance in Murine Models

(2014) Liem H. Nguyen et al.   CANCER CELL

Intestinal Epithelial HuR Modulates Distinct Pathways of Proliferation and Apoptosis and Attenuates Small Intestinal and Colonic Tumor Development

(2014) A. Giammanco et al.   CANCER RESEARCH

A 1536-Well Fluorescence Polarization Assay to Screen for Modulators of the MUSASHI Family of RNA-Binding Proteins

(2014) Gerard Minuesa et al.   COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING

Lin28 sustains early renal progenitors and induces Wilms tumor

(2014) A. Urbach et al.   GENES & DEVELOPMENT

A Conserved Three-nucleotide Core Motif Defines Musashi RNA Binding Specificity

(2014) N. Ruth Zearfoss et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Present and future of NMR for RNA–protein complexes: A perspective of integrated structural biology

(2014) Teresa Carlomagno   JOURNAL OF MAGNETIC RESONANCE

Clinical significance of HuR expression in human malignancy

(2014) Ioly Kotta-Loizou et al.   MEDICAL ONCOLOGY

RNA-binding protein HuR promotes growth of small intestinal mucosa by activating the Wnt signaling pathway

(2014) Lan Liu et al.   MOLECULAR BIOLOGY OF THE CELL

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(2014) Matthew Gubin et al.   MOLECULAR MEDICINE

Integrative analysis of cancer imaging readouts by networks

(2014) Marco Dominietto et al.   Molecular Oncology

Post-transcriptional coordination of immunological responses by RNA-binding proteins

(2014) Panagiota Kafasla et al.   NATURE IMMUNOLOGY

A census of human RNA-binding proteins

(2014) Stefanie Gerstberger et al.   NATURE REVIEWS GENETICS

Resveratrol post-transcriptionally regulates pro-inflammatory gene expression via regulation of KSRP RNA binding activity

(2014) Franziska Bollmann et al.   NUCLEIC ACIDS RESEARCH

In vivoimaging of protein–protein and RNA–protein interactions using novel far-red fluorescence complementation systems

(2014) Yu Han et al.   NUCLEIC ACIDS RESEARCH

Advantages of crystallographic fragment screening: Functional and mechanistic insights from a powerful platform for efficient drug discovery

(2014) Disha Patel et al.   PROGRESS IN BIOPHYSICS & MOLECULAR BIOLOGY

Pre-mRNA Splicing-Modulatory Pharmacophores: The Total Synthesis of Herboxidiene, a Pladienolide–Herboxidiene Hybrid Analog and Related Derivatives

(2013) Chandraiah Lagisetti et al.   ACS Chemical Biology

The structure of the ARE-binding domains of Hu antigen R (HuR) undergoes conformational changes during RNA binding

(2013) Hong Wang et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Screening for inhibitors of the hepatitis C virus internal ribosome entry site RNA

(2013) Shou Zhou et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Predictive and prognostic significance of cytoplasmic expression of ELAV-like protein HuR in invasive breast cancer treated with neoadjuvant chemotherapy

(2013) Jun Wang et al.   BREAST CANCER RESEARCH AND TREATMENT

Lin28: Primal Regulator of Growth and Metabolism in Stem Cells

(2013) Ng Shyh-Chang et al.   Cell Stem Cell

HTS by NMR of Combinatorial Libraries: A Fragment-Based Approach to Ligand Discovery

(2013) Bainan Wu et al.   CHEMISTRY & BIOLOGY

Phase I Pharmacokinetic and Pharmacodynamic Study of the First-in-Class Spliceosome Inhibitor E7107 in Patients with Advanced Solid Tumors

(2013) F. A. L. M. Eskens et al.   CLINICAL CANCER RESEARCH

LIN28/LIN28B: An emerging oncogenic driver in cancer stem cells

(2013) Jianbiao Zhou et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

An Overview of Biological Macromolecule Crystallization

(2013) Irene Russo Krauss et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

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

(2013) D. S. Hong et al.   INVESTIGATIONAL NEW DRUGS

Screening protein – Single stranded RNA complexes by NMR spectroscopy for structure determination

(2013) Jaelle N. Foot et al.   METHODS

A compendium of RNA-binding motifs for decoding gene regulation

(2013) Debashish Ray et al.   NATURE

Recurrent mutations at codon 625 of the splicing factor SF3B1 in uveal melanoma

(2013) J William Harbour et al.   NATURE GENETICS

A Novel High Throughput Biochemical Assay to Evaluate the HuR Protein-RNA Complex Formation

(2013) Vito G. D’Agostino et al.   PLoS One

Imaging of mRNA–Protein Interactions in Live Cells Using Novel mCherry Trimolecular Fluorescence Complementation Systems

(2013) Juan Yin et al.   PLoS One

TDP-43-mediated neurodegeneration: towards a loss-of-function hypothesis?

(2013) Lies Vanden Broeck et al.   TRENDS IN MOLECULAR MEDICINE

Mapping the Hallmarks of Lung Adenocarcinoma with Massively Parallel Sequencing

(2012) Marcin Imielinski et al.   CELL

The Protein Zfand5 Binds and Stabilizes mRNAs with AU-rich Elements in Their 3′-Untranslated Regions

(2012) Guoan He et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Analysis of Small Molecule Ligands Targeting the HIV-1 Matrix Protein-RNA Binding Site

(2012) Ayna Alfadhli et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

LIN28 Binds Messenger RNAs at GGAGA Motifs and Regulates Splicing Factor Abundance

(2012) Melissa L. Wilbert et al.   MOLECULAR CELL

LIN28B induces neuroblastoma and enhances MYCN levels via let-7 suppression

(2012) Jan J Molenaar et al.   NATURE GENETICS

The Lin28 cold-shock domain remodels pre-let-7 microRNA

(2012) Florian Mayr et al.   NUCLEIC ACIDS RESEARCH

Lin28-mediated control of let-7 microRNA expression by alternative TUTases Zcchc11 (TUT4) and Zcchc6 (TUT7)

(2012) J. E. Thornton et al.   RNA

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

(2011) Liying Fan et al.   ACS Chemical Biology

MSI2 protein expression predicts unfavorable outcome in acute myeloid leukemia

(2011) R. J. Byers et al.   BLOOD

Molecular Basis for Interaction of let-7 MicroRNAs with Lin28

(2011) Yunsun Nam et al.   CELL

HuR function in disease

(2011) Subramanya Srikantan   Frontiers in Bioscience-Landmark

Combining Global and Local Measures for Structure-Based Druggability Predictions

(2011) Andrea Volkamer et al.   Journal of Chemical Information and Modeling

Myeloid cell expression of the RNA-binding protein HuR protects mice from pathologic inflammation and colorectal carcinogenesis

(2011) Anthie Yiakouvaki et al.   JOURNAL OF CLINICAL INVESTIGATION

Role of RNA binding protein HuR in ductal carcinoma in situ of the breast

(2011) Mira Heinonen et al.   JOURNAL OF PATHOLOGY

Integrative Regulatory Mapping Indicates that the RNA-Binding Protein HuR Couples Pre-mRNA Processing and mRNA Stability

(2011) Neelanjan Mukherjee et al.   MOLECULAR CELL

From unwinding to clamping — the DEAD box RNA helicase family

(2011) Patrick Linder et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

SF3B1and Other Novel Cancer Genes in Chronic Lymphocytic Leukemia

(2011) Lili Wang et al.   NEW ENGLAND JOURNAL OF MEDICINE

Structure of Musashi1 in a complex with target RNA: the role of aromatic stacking interactions

(2011) Takako Ohyama et al.   NUCLEIC ACIDS RESEARCH

Small molecule enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2-mediated microRNA processing

(2011) S. Melo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Analysis of in vitro bioactivity data extracted from drug discovery literature and patents: Ranking 1654 human protein targets by assayed compounds and molecular scaffolds

(2011) Christopher Southan et al.   Journal of Cheminformatics

Aptamer sandwich assays: label-free and fluorescence investigations of heterogeneous binding events

(2010) Katie A. Edwards et al.   ANALYTICAL AND BIOANALYTICAL CHEMISTRY

Assessing protein–RNA interactions using microfluidic capillary mobility shift assays

(2010) Jimmy Fourtounis et al.   ANALYTICAL BIOCHEMISTRY

TDP-43: A DNA and RNA binding protein with roles in neurodegenerative diseases

(2010) Sadaf T. Warraich et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Grand Challenge Commentary: Accessing new chemical space for 'undruggable' targets

(2010) Sivaraman Dandapani et al.   Nature Chemical Biology

Musashi-2 regulates normal hematopoiesis and promotes aggressive myeloid leukemia

(2010) Michael G Kharas et al.   NATURE MEDICINE

Quantitative approaches to monitor protein-nucleic acid interactions using fluorescent probes

(2010) J. M. Pagano et al.   RNA

Posttranscriptional regulation of cancer traits by HuR

(2010) Kotb Abdelmohsen et al.   Wiley Interdisciplinary Reviews-RNA

Chemical inhibitors destabilize HuR binding to the AU-rich element of TNF-α mRNA

(2009) Min-Ju Chae et al.   EXPERIMENTAL AND MOLECULAR MEDICINE

The RNA-Binding Protein Elavl1/HuR Is Essential for Placental Branching Morphogenesis and Embryonic Development

(2009) V. Katsanou et al.   MOLECULAR AND CELLULAR BIOLOGY

Regulation of Bcl-2 Expression by HuR in HL60 Leukemia Cells and A431 Carcinoma Cells

(2009) D. Ishimaru et al.   MOLECULAR CANCER RESEARCH

Coordinated posttranscriptional mRNA population dynamics during T-cell activation

(2009) Neelanjan Mukherjee et al.   Molecular Systems Biology

Lin28 promotes transformation and is associated with advanced human malignancies

(2009) Srinivas R Viswanathan et al.   NATURE GENETICS

Lin28 recruits the TUTase Zcchc11 to inhibit let-7 maturation in mouse embryonic stem cells

(2009) John P Hagan et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Alternative polyadenylation variants of the RNA binding protein, HuR: abundance, role of AU-rich elements and auto-Regulation

(2009) Wijdan Al-Ahmadi et al.   NUCLEIC ACIDS RESEARCH

In vivo detection of RNA-binding protein interactions with cognate RNA sequences by fluorescence resonance energy transfer

(2009) M. Huranova et al.   RNA

Applications of isothermal titration calorimetry in protein science

(2008) Yi Liang   ACTA BIOCHIMICA ET BIOPHYSICA SINICA

High-throughput assays probing protein–RNA interactions of eukaryotic translation initiation factors

(2008) Gabriela Galicia-Vázquez et al.   ANALYTICAL BIOCHEMISTRY

Posttranscriptional gene regulation by RNA-binding proteins during oxidative stress: implications for cellular senescence

(2008) Kotb Abdelmohsen et al.   BIOLOGICAL CHEMISTRY

Diverse molecular functions of Hu proteins

(2008) M. N. Hinman et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

The role of transactive response DNA-binding protein-43 in amyotrophic lateral sclerosis and frontotemporal dementia

(2008) Ian RA Mackenzie et al.   CURRENT OPINION IN NEUROLOGY

RNA recognition motifs: boring? Not quite

(2008) Antoine Cléry et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Structure and function of KH domains

(2008) Roberto Valverde et al.   FEBS Journal

Hu Antigen R (HuR) Functions as an Alternative Pre-mRNA Splicing Regulator of Fas Apoptosis-promoting Receptor on Exon Definition

(2008) José M. Izquierdo   JOURNAL OF BIOLOGICAL CHEMISTRY

Lin28 Mediates the Terminal Uridylation of let-7 Precursor MicroRNA

(2008) Inha Heo et al.   MOLECULAR CELL

A feedback loop comprising lin-28 and let-7 controls pre-let-7 maturation during neural stem-cell commitment

(2008) Agnieszka Rybak et al.   NATURE CELL BIOLOGY

Lin-28 interaction with the Let-7 precursor loop mediates regulated microRNA processing

(2008) M. A. Newman et al.   RNA

Selective Blockade of MicroRNA Processing by Lin28

(2008) S. R. Viswanathan et al.   SCIENCE

Multiple roles of TDP-43 in gene expression, splicing regulation, and human disease

(2007) Emanuele Buratti   Frontiers in Bioscience-Landmark