Current Status of Oligonucleotide-Based Protein Degraders

Inducible Degradation of Oncogenic Nucleolin Using an Aptamer-Based PROTAC

(2023) Miao Chen et al.   Journal of Medicinal Chemistry

DNA-modularized construction of bivalent ligands precisely regulates receptor binding and activation

(2023) Na Zhao et al.   Chem

Small molecules and their impact in drug discovery: A perspective on the occasion of the 125th anniversary of the Bayer Chemical Research Laboratory

(2022) Hartmut Beck et al.   DRUG DISCOVERY TODAY

PROTAC targeted protein degraders: the past is prologue

(2022) Miklós Békés et al.   NATURE REVIEWS DRUG DISCOVERY

Progress in cancer drug delivery based on AS1411 oriented nanomaterials

(2022) Xin Tong et al.   JOURNAL OF NANOBIOTECHNOLOGY

Driving E3 Ligase Substrate Specificity for Targeted Protein Degradation: Lessons from Nature and the Laboratory

(2022) Angus D Cowan et al.   Annual Review of Biochemistry

Targeted protein degradation and drug discovery

(2022) Mikihiko Naito   JOURNAL OF BIOCHEMISTRY

Recent advances in IAP-based PROTACs (SNIPERs) as potential therapeutic agents

(2022) Chao Wang et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Behavioural and functional evidence revealing the role of RBFOX1 variation in multiple psychiatric disorders and traits

(2022) Aet O’Leary et al.   MOLECULAR PSYCHIATRY

Development of Gilteritinib-Based Chimeric Small Molecules that Potently Induce Degradation of FLT3-ITD Protein

(2022) Nobumichi Ohoka et al.   ACS Medicinal Chemistry Letters

Apt-clean: aptamer-mediated cleavage of extracellular antigens for the inhibition of membrane protein functions

(2022) Junya Hoshiyama et al.   Biomaterials Science

Development of a novel PROTAC using the nucleic acid aptamer as a targeting ligand for tumor selective degradation of nucleolin

(2022) Lin Zhang et al.   Molecular Therapy-Nucleic Acids

Radiosensitization of breast cancer cells using AS1411 aptamer-conjugated gold nanoparticles

(2021) Somayeh Sadat Mehrnia et al.   Radiation Oncology

Locking up the AS1411 Aptamer with a Flanking Duplex: Towards an Improved Nucleolin-Targeting

(2021) André Miranda et al.   Pharmaceuticals

PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy

(2021) Si-Min Qi et al.   Frontiers in Pharmacology

Aptamer‐PROTAC Conjugates (APCs) for Tumor‐Specific Targeting in Breast Cancer

(2021) Shipeng He et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Aptamer‐mediated synthesis of multifunctional nano‐hydroxyapatite for active tumour bioimaging and treatment

(2021) Wenqing Zhang et al.   CELL PROLIFERATION

Characterization of a DNA Aptamer with High Specificity toward Fibroblast Growth Factor Receptor 1

(2021) Junya Hoshiyama et al.   CHEMISTRY LETTERS

New approaches to target RNA binding proteins

(2021) Ashley R. Julio et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

TF-PROTACs Enable Targeted Degradation of Transcription Factors

(2021) Jing Liu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Destruction of DNA‐Binding Proteins by Programmable Oligonucleotide PROTAC (O'PROTAC): Effective Targeting of LEF1 and ERG

(2021) Jingwei Shao et al.   Advanced Science

Aptamer-Functionalized Gold Nanoparticles for Drug Delivery to Gynecological Carcinoma Cells

(2021) Jessica Lopes-Nunes et al.   Cancers

The Functions of BET Proteins in Gene Transcription of Biology and Diseases

(2021) Ka Lung Cheung et al.   Frontiers in Molecular Biosciences

Self-assembly of an aptamer-decorated chimeric peptide nanocarrier for targeted cancer gene delivery

(2021) Sadegh Dehghani et al.   COLLOIDS AND SURFACES B-BIOINTERFACES

Exosite Binding in Thrombin: A Global Structural/Dynamic Overview of Complexes with Aptamers and Other Ligands

(2021) Romualdo Troisi et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

The PROTAC gold rush

(2021) Ken Garber   NATURE BIOTECHNOLOGY

Fabrication of G-quadruplex/porphyrin conjugated gold/persistent luminescence theranostic nanoprobe for imaging-guided photodynamic therapy

(2021) Yu-Bin Su et al.   TALANTA

Development of Chimeric Molecules That Degrade the Estrogen Receptor Using Decoy Oligonucleotide Ligands

(2021) Miyako Naganuma et al.   ACS Medicinal Chemistry Letters

AS1411 Aptamer Linked to DNA Nanostructures Diverts Its Traffic Inside Cancer Cells and Improves Its Therapeutic Efficacy

(2021) Giulia Vindigni et al.   Pharmaceutics

Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC)

(2020) Hao Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Transcription Factor Inhibition: Lessons Learned and Emerging Targets

(2020) Andrew Chen et al.   TRENDS IN MOLECULAR MEDICINE

Proximity-induced caspase-9 activation on a DNA origami-based synthetic apoptosome

(2020) Bas J. H. M. Rosier et al.   Nature Catalysis

Chemical Synthesis and Biological Application of Modified Oligonucleotides

(2020) Daniel A. Glazier et al.   BIOCONJUGATE CHEMISTRY

Fundamental aspects of DMPK optimization of targeted protein degraders

(2020) Carina Cantrill et al.   DRUG DISCOVERY TODAY

Programming Cell–Cell Communications with Engineered Cell Origami Clusters

(2020) Zhilei Ge et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Molecular mechanisms and cellular functions of cGAS–STING signalling

(2020) Karl-Peter Hopfner et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Design and synthesis of peptide-based chimeric molecules to induce degradation of the estrogen and androgen receptors

(2020) Hidetomo Yokoo et al.   BIOORGANIC & MEDICINAL CHEMISTRY

The Role of Tissue-Specific Ubiquitin Ligases, RNF183, RNF186, RNF182 and RNF152, in Disease and Biological Function

(2020) Takumi Okamoto et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Role of nanoscale antigen organization on B-cell activation probed using DNA origami

(2020) Rémi Veneziano et al.   Nature Nanotechnology

Advances in oligonucleotide drug delivery

(2020) Thomas C. Roberts et al.   NATURE REVIEWS DRUG DISCOVERY

DNA Analogues Modified at the Nonlinking Positions of Phosphorus

(2020) Pawan Kumar et al.   ACCOUNTS OF CHEMICAL RESEARCH

Therapeutic Interventions into Innate Immune Diseases by Means of Aptamers

(2020) Farzana Yasmeen et al.   Pharmaceutics

RNA‐PROTACs: Degraders of RNA‐Binding Proteins

(2020) Alice Ghidini et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Milestones in Personalized Medicine: From the Ancient Time to Nowadays—the Provocation of COVID-19

(2020) Sophie Visvikis-Siest et al.   Frontiers in Genetics

Chemical modification of PS-ASO therapeutics reduces cellular protein-binding and improves the therapeutic index

(2019) Wen Shen et al.   NATURE BIOTECHNOLOGY

Proteolysis targeting chimeras (PROTACs) in ‘beyond rule-of-five’ chemical space: Recent progress and future challenges

(2019) Scott D. Edmondson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-mediated Targeted Protein Degradation

(2019) George M Burslem et al.   CANCER RESEARCH

Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16

(2019) Xiaoyu Zhang et al.   Nature Chemical Biology

A programmable DNA-origami platform for studying lipid transfer between bilayers

(2019) Xin Bian et al.   Nature Chemical Biology

DHX36 prevents the accumulation of translationally inactive mRNAs with G4-structures in untranslated regions

(2019) Markus Sauer et al.   Nature Communications

Metabolite profiling of the antisense oligonucleotide eluforsen using liquid chromatography-mass spectrometry

(2019) Jaeah Kim et al.   Molecular Therapy-Nucleic Acids

The Membrane-Associated MARCH E3 Ligase Family: Emerging Roles in Immune Regulation

(2019) Heng Lin et al.   Frontiers in Immunology

Mechanisms of DNA Replication and Repair: Insights from the Study of G-Quadruplexes

(2019) Tracy M. Bryan   MOLECULES

LIN 28A loss of function is associated with Parkinson's disease pathogenesis

(2019) Mi‐Yoon Chang et al.   EMBO JOURNAL

Interplay of Guanine Oxidation and G-Quadruplex Folding in Gene Promoters

(2019) Aaron M. Fleming et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation

(2018) Nobumichi Ohoka et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A brave new world of RNA-binding proteins

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

DNA-Based Dynamic Reaction Networks

(2018) Ting Fu et al.   TRENDS IN BIOCHEMICAL SCIENCES

High throughput protease profiling comprehensively defines active site specificity for thrombin and ADAMTS13

(2018) Colin A. Kretz et al.   Scientific Reports

Comprehensive Genomic Characterization of RNA-Binding Proteins across Human Cancers

(2018) Ze-Lin Wang et al.   Cell Reports

A Sensitive In Vitro Approach to Assess the Hybridization-Dependent Toxic Potential of High Affinity Gapmer Oligonucleotides

(2018) Andreas Dieckmann et al.   Molecular Therapy-Nucleic Acids

Structural basis of G-quadruplex unfolding by the DEAH/RHA helicase DHX36

(2018) Michael C. Chen et al.   NATURE

Pharmacological difference between degrader and inhibitor against oncogenic BCR-ABL kinase

(2018) Norihito Shibata et al.   Scientific Reports

Targeted therapy for gynecologic cancers: Toward the era of precision medicine

(2018) Partha Basu et al.   INTERNATIONAL JOURNAL OF GYNECOLOGY & OBSTETRICS

Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion

(2018) George M. Burslem et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Targeted Intracellular Delivery of Antibodies: The State of the Art

(2018) Tatiana A. Slastnikova et al.   Frontiers in Pharmacology

In VivoKnockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs)

(2017) Nobumichi Ohoka et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Aptamers as targeted therapeutics: current potential and challenges

(2017) Jiehua Zhou et al.   NATURE REVIEWS DRUG DISCOVERY

DNA nanotechnology

(2017) Nadrian C. Seeman et al.   Nature Reviews Materials

A Small-Molecule Inhibitor of Lin28

(2016) Martina Roos et al.   ACS Chemical Biology

AS1411-Induced Growth Inhibition of Glioma Cells by Up-Regulation of p53 and Down-Regulation of Bcl-2 and Akt1 via Nucleolin

(2016) Ye Cheng et al.   PLoS One

Progress and Challenges in Developing Aptamer-Functionalized Targeted Drug Delivery Systems

(2015) Feng Jiang et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Hepatotoxicity of high affinity gapmer antisense oligonucleotides is mediated by RNase H1 dependent promiscuous reduction of very long pre-mRNA transcripts

(2015) Sebastien A. Burel et al.   NUCLEIC ACIDS RESEARCH

Insights into G-quadruplex specific recognition by the DEAH-box helicase RHAU: Solution structure of a peptide–quadruplex complex

(2015) Brahim Heddi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Conservation of transcription factor binding specificities across 600 million years of bilateria evolution

(2015) Kazuhiro R Nitta et al.   eLife

Determination and Inference of Eukaryotic Transcription Factor Sequence Specificity

(2014) Matthew T. Weirauch et al.   CELL

Synthesis and Biological Evaluation of a Novel Series of Heterobivalent Muscarinic Ligands Based on Xanomeline and 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1)

(2014) Alessandro Bonifazi et al.   JOURNAL OF MEDICINAL CHEMISTRY

A census of human RNA-binding proteins

(2014) Stefanie Gerstberger et al.   NATURE REVIEWS GENETICS

UniPROBE, update 2015: new tools and content for the online database of protein-binding microarray data on protein–DNA interactions

(2014) Maxwell A. Hume et al.   NUCLEIC ACIDS RESEARCH

DNA-Binding Specificities of Human Transcription Factors

(2013) Arttu Jolma et al.   CELL

Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease

(2013) Bruce J. Melancon et al.   DRUG DISCOVERY TODAY

A phase II trial of AS1411 (a novel nucleolin-targeted DNA aptamer) in metastatic renal cell carcinoma

(2013) Jonathan E. Rosenberg et al.   INVESTIGATIONAL NEW DRUGS

Monomer-Dimer Equilibrium for the 5′-5′ Stacking of Propeller-Type Parallel-Stranded G-Quadruplexes: NMR Structural Study

(2012) Ngoc Quang Do et al.   CHEMISTRY-A EUROPEAN JOURNAL

Generating Aptamers by Cell-SELEX for Applications in Molecular Medicine

(2012) Mao Ye et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

The Extended Cleavage Specificity of Human Thrombin

(2012) Maike Gallwitz et al.   PLoS One

G4 Resolvase 1 tightly binds and unwinds unimolecular G4-DNA

(2011) Banabihari Giri et al.   NUCLEIC ACIDS RESEARCH

A New Paradigm for Aptamer Therapeutic AS1411 Action: Uptake by Macropinocytosis and Its Stimulation by a Nucleolin-Dependent Mechanism

(2010) E. M. Reyes-Reyes et al.   CANCER RESEARCH

Hybrid Molecules from Xanomeline and Tacrine: Enhanced Tacrine Actions on Cholinesterases and Muscarinic M1Receptors

(2010) Lei Fang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Protein Knockdown Using Methyl Bestatin−Ligand Hybrid Molecules: Design and Synthesis of Inducers of Ubiquitination-Mediated Degradation of Cellular Retinoic Acid-Binding Proteins

(2010) Yukihiro Itoh et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Aptamers as therapeutics

(2010) Anthony D. Keefe et al.   NATURE REVIEWS DRUG DISCOVERY

Long Range Communication between Exosites 1 and 2 Modulates Thrombin Function

(2009) Nicolas S. Petrera et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Modifications Incorporated in CpG Motifs of Oligodeoxynucleotides Lead to Antagonist Activity of Toll-like Receptors 7 and 9

(2009) Dong Yu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Plasma Membrane Nucleolin Is a Receptor for the Anticancer Aptamer AS1411 in MV4-11 Leukemia Cells

(2009) S. Soundararajan et al.   MOLECULAR PHARMACOLOGY

The Nucleolin Targeting Aptamer AS1411 Destabilizes Bcl-2 Messenger RNA in Human Breast Cancer Cells

(2008) S. Soundararajan et al.   CANCER RESEARCH

Inhibition of transcription factors with small organic molecules

(2008) Thorsten Berg   CURRENT OPINION IN CHEMICAL BIOLOGY