DNA-encoded libraries – an efficient small molecule discovery technology for the biomedical sciences

Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases

(2017) Philip A. Harris et al.   JOURNAL OF MEDICINAL CHEMISTRY

Comparative Analysis of Single-Cell RNA Sequencing Methods

(2017) Christoph Ziegenhain et al.   MOLECULAR CELL

Structural insight into allosteric modulation of protease-activated receptor 2

(2017) Robert K. Y. Cheng et al.   NATURE

Directing evolution: the next revolution in drug discovery?

(2017) Andrew M. Davis et al.   NATURE REVIEWS DRUG DISCOVERY

Targeted protein degradation by PROTACs

(2017) Taavi K. Neklesa et al.   PHARMACOLOGY & THERAPEUTICS

Allosteric “beta-blocker” isolated from a DNA-encoded small molecule library

(2017) Seungkirl Ahn et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A carbohydrate-derived trifunctional scaffold for DNA-encoded libraries

(2017) Amalia M. Estévez et al.   TETRAHEDRON-ASYMMETRY

Acid- and Au(i)-mediated synthesis of hexathymidine-DNA-heterocycle chimeras, an efficient entry to DNA-encoded libraries inspired by drug structures

(2017) Mateja Klika Škopić et al.   Chemical Science

Prioritizing multiple therapeutic targets in parallel using automated DNA-encoded library screening

(2017) Carl A. Machutta et al.   Nature Communications

Analysis of Current DNA Encoded Library Screening Data Indicates Higher False Negative Rates for Numerically Larger Libraries

(2017) Alexander L. Satz et al.   ACS Combinatorial Science

Advancements in Aptamer Discovery Technologies

(2016) Michael R. Gotrik et al.   ACCOUNTS OF CHEMICAL RESEARCH

Chemical Biology Probes from Advanced DNA-encoded Libraries

(2016) Hazem Salamon et al.   ACS Chemical Biology

Chemical Space of DNA-Encoded Libraries

(2016) Raphael M. Franzini et al.   JOURNAL OF MEDICINAL CHEMISTRY

Advances in Computational Medicinal Chemistry: A Reflection on the Evolution of the Field and Perspective Going Forward

(2016) Brian K. Shoichet et al.   JOURNAL OF MEDICINAL CHEMISTRY

Automated screening for small organic ligands using DNA-encoded chemical libraries

(2016) Willy Decurtins et al.   Nature Protocols

DNA-encoded chemistry: enabling the deeper sampling of chemical space

(2016) Robert A. Goodnow et al.   NATURE REVIEWS DRUG DISCOVERY

Twenty years on: the impact of fragments on drug discovery

(2016) Daniel A. Erlanson et al.   NATURE REVIEWS DRUG DISCOVERY

A comprehensive map of molecular drug targets

(2016) Rita Santos et al.   NATURE REVIEWS DRUG DISCOVERY

From haystack to needle: finding value with DNA encoded library technology at GSK

(2016) Christopher C. Arico-Muendel   MedChemComm

Analysis of the productivity of DNA encoded libraries

(2016) Oliv Eidam et al.   MedChemComm

Development and design of the tertiary amino effect reaction for DNA-encoded library synthesis

(2016) Xia Tian et al.   MedChemComm

Novel p38α MAP kinase inhibitors identified from yoctoReactor DNA-encoded small molecule library

(2016) L. K. Petersen et al.   MedChemComm

Crosslinking of DNA-linked ligands to target proteins for enrichment from DNA-encoded libraries

(2016) Kyle E. Denton et al.   MedChemComm

Screening for covalent inhibitors using DNA-display of small molecule libraries functionalized with cysteine reactive moieties

(2016) C. Zambaldo et al.   MedChemComm

Design and synthesis of DNA-encoded libraries based on a benzodiazepine and a pyrazolopyrimidine scaffold

(2016) M. Klika Škopić et al.   MedChemComm

What is a “DNA-Compatible” Reaction?

(2016) Marie L. Malone et al.   ACS Combinatorial Science

DNA Encoded Library Selections and Insights Provided by Computational Simulations

(2015) Alexander L. Satz   ACS Chemical Biology

Identification of Structure-Activity Relationships from Screening a Structurally Compact DNA-Encoded Chemical Library

(2015) Raphael M. Franzini et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A Versatile Approach Towards Nucleobase-Modified Aptamers

(2015) Fabian Tolle et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

DNA Compatible Multistep Synthesis and Applications to DNA Encoded Libraries

(2015) Alexander Lee Satz et al.   BIOCONJUGATE CHEMISTRY

Dynamic combinatorial chemistry: a tool to facilitate the identification of inhibitors for protein targets

(2015) Milon Mondal et al.   CHEMICAL SOCIETY REVIEWS

Overcoming Chemical, Biological, and Computational Challenges in the Development of Inhibitors Targeting Protein-Protein Interactions

(2015) Luca Laraia et al.   CHEMISTRY & BIOLOGY

Novel selection methods for DNA-encoded chemical libraries

(2015) Alix I Chan et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Fidelity by design: Yoctoreactor and binder trap enrichment for small-molecule DNA-encoded libraries and drug discovery

(2015) Peter Blakskjaer et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

PNA-encoded chemical libraries

(2015) Claudio Zambaldo et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Construction and screening of vast libraries of natural product-like macrocyclic peptides using in vitro display technologies

(2015) Nasir K Bashiruddin et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Chemical ligation methods for the tagging of DNA-encoded chemical libraries

(2015) Anthony D Keefe et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

The Role of Phosphodiesterase 12 (PDE12) as a Negative Regulator of the Innate Immune Response and the Discovery of Antiviral Inhibitors

(2015) Edgar R. Wood et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Silent Encoding of Chemical Post-Translational Modifications in Phage-Displayed Libraries

(2015) Katrina F. Tjhung et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation

(2015) Huw D Lewis et al.   Nature Chemical Biology

The promise and peril of chemical probes

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

Dual-display of small molecules enables the discovery of ligand pairs and facilitates affinity maturation

(2015) Moreno Wichert et al.   Nature Chemistry

Design, preparation, and selection of DNA-encoded dynamic libraries

(2015) Gang Li et al.   Chemical Science

Discovery of a Potent Class of PI3Kα Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT)

(2015) Hongfang Yang et al.   ACS Medicinal Chemistry Letters

Discovery, SAR, and X-ray Binding Mode Study of BCATm Inhibitors from a Novel DNA-Encoded Library

(2015) Hongfeng Deng et al.   ACS Medicinal Chemistry Letters

A comprehensive assessment of somatic mutation detection in cancer using whole-genome sequencing

(2015) Tyler S. Alioto et al.   Nature Communications

Cell-Based Selection Expands the Utility of DNA-Encoded Small-Molecule Library Technology to Cell Surface Drug Targets: Identification of Novel Antagonists of the NK3 Tachykinin Receptor

(2015) Zining Wu et al.   ACS Combinatorial Science

“Cap-and-Catch” Purification for Enhancing the Quality of Libraries of DNA Conjugates

(2015) Raphael M. Franzini et al.   ACS Combinatorial Science

DNA-Encoded Solid-Phase Synthesis: Encoding Language Design and Complex Oligomer Library Synthesis

(2015) Andrew B. MacConnell et al.   ACS Combinatorial Science

Encoded Library Synthesis Using Chemical Ligation and the Discovery of sEH Inhibitors from a 334-Million Member Library

(2015) Alexander Litovchick et al.   Scientific Reports

DNA-Encoded Chemical Libraries: Advancing beyond Conventional Small-Molecule Libraries

(2014) Raphael M. Franzini et al.   ACCOUNTS OF CHEMICAL RESEARCH

Characterization of DNA-Conjugated Compounds Using a Regenerable Chip

(2014) Weilin Lin et al.   ANALYTICAL CHEMISTRY

Selection of DNA-Encoded Small Molecule Libraries Against Unmodified and Non-Immobilized Protein Targets

(2014) Peng Zhao et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Systematic Evaluation and Optimization of Modification Reactions of Oligonucleotides with Amines and Carboxylic Acids for the Synthesis of DNA-Encoded Chemical Libraries

(2014) Raphael M. Franzini et al.   BIOCONJUGATE CHEMISTRY

Application of encoded library technology (ELT) to a protein–protein interaction target: Discovery of a potent class of integrin lymphocyte function-associated antigen 1 (LFA-1) antagonists

(2014) Christopher S. Kollmann et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A DNA-templated synthesis of encoded small molecules by DNA self-assembly

(2014) Cheng Cao et al.   CHEMICAL COMMUNICATIONS

Modulators of Protein–Protein Interactions

(2014) Lech-Gustav Milroy et al.   CHEMICAL REVIEWS

Aptamers and SELEX in Chemistry & Biology

(2014) Michael Famulok et al.   CHEMISTRY & BIOLOGY

Encoded Library Technology as a Source of Hits for the Discovery and Lead Optimization of a Potent and Selective Class of Bactericidal Direct Inhibitors of Mycobacterium tuberculosis InhA

(2014) Lourdes Encinas et al.   JOURNAL OF MEDICINAL CHEMISTRY

Anti-diabetic activity of insulin-degrading enzyme inhibitors mediated by multiple hormones

(2014) Juan Pablo Maianti et al.   NATURE

Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction

(2014) Aidan G Gilmartin et al.   Nature Chemical Biology

Small Targeted Cytotoxics: Current State and Promises from DNA-Encoded Chemical Libraries

(2013) Nikolaus Krall et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Expanding the Scope of PNA-Encoded Synthesis (PES): Mtt-Protected PNA Fully Orthogonal to Fmoc Chemistry and a Broad Array of Robust Diversity-Generating Reactions

(2012) Dalila Chouikhi et al.   CHEMISTRY-A EUROPEAN JOURNAL

Discovery of Small-Molecule Interleukin-2 Inhibitors from a DNA-Encoded Chemical Library

(2012) Markus Leimbacher et al.   CHEMISTRY-A EUROPEAN JOURNAL

Discovery of Highly Potent and Selective Small Molecule ADAMTS-5 Inhibitors That Inhibit Human Cartilage Degradation via Encoded Library Technology (ELT)

(2012) Hongfeng Deng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Highly specific, bisubstrate-competitive Src inhibitors from DNA-templated macrocycles

(2012) George Georghiou et al.   Nature Chemical Biology

Routine Use of Microbial Whole Genome Sequencing in Diagnostic and Public Health Microbiology

(2012) Claudio U. Köser et al.   PLoS Pathogens

Small-molecule discovery from DNA-encoded chemical libraries

(2011) Ralph E. Kleiner et al.   CHEMICAL SOCIETY REVIEWS

A Decade of the Human Genome Sequence-How Does the Medicinal Chemist Benefit?

(2011) Andreas Brunschweiger et al.   ChemMedChem

Beyond natural antibodies: the power of in vitro display technologies

(2011) Andrew R M Bradbury et al.   NATURE BIOTECHNOLOGY

Impact of high-throughput screening in biomedical research

(2011) Ricardo Macarron et al.   NATURE REVIEWS DRUG DISCOVERY

Selection of Carbonic Anhydrase IX Inhibitors from One Million DNA-Encoded Compounds

(2010) Fabian Buller et al.   ACS Chemical Biology

Drug Discovery with DNA-Encoded Chemical Libraries

(2010) Fabian Buller et al.   BIOCONJUGATE CHEMISTRY

Isolation of a Small-Molecule Inhibitor of the Antiapoptotic Protein Bcl-xL from a DNA-Encoded Chemical Library

(2010) Samu Melkko et al.   ChemMedChem

Selecting chemicals: the emerging utility of DNA-encoded libraries

(2010) Matthew A. Clark   CURRENT OPINION IN CHEMICAL BIOLOGY

In VitroSelection of a DNA-Templated Small-Molecule Library Reveals a Class of Macrocyclic Kinase Inhibitors

(2010) Ralph E. Kleiner et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Interaction-Dependent PCR: Identification of Ligand−Target Pairs from Libraries of Ligands and Libraries of Targets in a Single Solution-Phase Experiment

(2010) Lynn M. McGregor et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The road less traveled: modulating signal transduction enzymes by inhibiting their protein–protein interactions

(2009) Michelle R Arkin et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

A Yoctoliter-Scale DNA Reactor for Small-Molecule Evolution

(2009) Margit Haahr Hansen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Design, synthesis and selection of DNA-encoded small-molecule libraries

(2009) Matthew A Clark et al.   Nature Chemical Biology

Phage-encoded combinatorial chemical libraries based on bicyclic peptides

(2009) Christian Heinis et al.   Nature Chemical Biology

Design and synthesis of a novel DNA-encoded chemical library using Diels-Alder cycloadditions

(2008) Fabian Buller et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

High-throughput sequencing allows the identification of binding molecules isolated from DNA-encoded chemical libraries

(2008) L. Mannocci et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA