ArticleNature communications2017
Prioritizing multiple therapeutic targets in parallel using automated DNA-encoded library screening.
Erratum issuedOpen access · goldAbstract read
In one paragraph
Article in Nature communications, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 25 papers.
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0cells of the map it votes in
25citing papers in PubMed
4.0field-weighted citation impact, top 5% of its field
What it found
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Who cites it
25 citing papers in PubMed, 74 citations in OpenAlex.
- Solid-phase DNA-encoded library synthesis: a master builder's instructions.Nature protocols · 2026Review
- Expansion of DNA-Encoded Library Hits Using Generative Chemistry and Ultra-Large Compound Catalogs.bioRxiv : the preprint server for biology · 2025Article
- The power of DNA-encoded chemical libraries in the battle against drug-resistant bacteria.RSC advances · 2025Review
- Targeting fusion oncoproteins in childhood cancers: challenges and future opportunities for developing therapeutics.Journal of the National Cancer Institute · 2024Article
- Building Block-Centric Approach to DNA-Encoded Library Design.Journal of chemical information and modeling · 2024Article
- Inhibitors of the Thioesterase Activity ofACS infectious diseases · 2024Article
- Exploiting the Carboxylate-Binding Pocket of β-Lactamase Enzymes Using a Focused DNA-Encoded Chemical Library.Journal of medicinal chemistry · 2024Article
- Unrealized targets in the discovery of antibiotics for Gram-negative bacterial infections.Nature reviews. Drug discovery · 2023Review
- Small-molecule discovery through DNA-encoded libraries.Nature reviews. Drug discovery · 2023Review
- Translating the Genome into Drugs.Accounts of chemical research · 2023Article
- Antibacterial Discovery via Phenotypic DNA-Encoded Library Screening.ACS chemical biology · 2021Article
- Combinatorial technology revitalized by DNA-encoding.MedComm · 2021Article
- DNA-Encoded Library Hit Confirmation: Bridging the Gap Between On-DNA and Off-DNA Chemistry.ACS medicinal chemistry letters · 2021Article
- Stereo- and regiodefined DNA-encoded chemical libraries enable efficient tumour-targeting applications.Nature chemistry · 2021Article
- Navigating the DNA encoded libraries chemical space.Communications chemistry · 2020Article
- Role of the lipid bilayer in outer membrane protein folding in Gram-negative bacteria.The Journal of biological chemistry · 2020Review
- Targets and Antibody Formats for Immunotherapy of Neuroblastoma.Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2020Review
- Beyond protein binding: recent advances in screening DNA-encoded libraries.Chemical communications (Cambridge, England) · 2019Review
- Encoded Library Technologies as Integrated Lead Finding Platforms for Drug Discovery.Molecules (Basel, Switzerland) · 2019Review
- Development of a Selection Method for Discovering Irreversible (Covalent) Binders from a DNA-Encoded Library.SLAS discovery : advancing life sciences R & D · 2019Article
Corrections and comments
- Erratum issued
Authors and funding
65 authors at 4 institutions in 3 countries.
Carl A MachuttaGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Christopher S KollmannGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Kenneth E LindGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Xiaopeng BaiGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Pan F ChanGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Jianzhong HuangGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Lluis BallellGlaxoSmithKline, Severo Ochoa 2, Tres Cantos, Madrid 28760, Spain.
Svetlana BelyanskayaGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Gurdyal S BesraUniversity of Birmingham, School of Biosciences, Edgbaston, Birmingham B15 2TT, UK.ORCID 0000-0002-5605-0395
David Barros-AguirreGlaxoSmithKline, Severo Ochoa 2, Tres Cantos, Madrid 28760, Spain.
Robert H BatesGlaxoSmithKline, Severo Ochoa 2, Tres Cantos, Madrid 28760, Spain.
Paolo A CentrellaGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Sandy S ChangGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Jing ChaiGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Anthony E ChoudhryGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Aaron CoffinGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Christopher P DavieGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Hongfeng DengGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Jianghe DengGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Yun DingGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Jason W DodsonGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
David T FosbennerGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Enoch N GaoGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Taylor L GrahamGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Todd L GraybillGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Karen IngrahamGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Walter P JohnsonGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Bryan W KingGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Christopher R KwiatkowskiGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Joël LelièvreGlaxoSmithKline, Severo Ochoa 2, Tres Cantos, Madrid 28760, Spain.
Yue LiGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Xiaorong LiuGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Quinn LuGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Ruth LehrGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Alfonso Mendoza-LosanaGlaxoSmithKline, Severo Ochoa 2, Tres Cantos, Madrid 28760, Spain.
John MartinGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Lynn McCloskeyGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Patti McCormickGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Heather P O'KeefeGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Thomas O'KeeffeGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Christina PaoGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Christopher B PhelpsGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Hongwei QiGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Keith RaffertyGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Genaro S ScavelloGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Matt S SteigingaGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Flora S SundersinghGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Sharon M SweitzerGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Lawrence M SzewczukGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Amy TaylorGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
May Fern TohGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Juan WangGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Minghui WangGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Devan J WilkinsGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Bing XiaGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Gang YaoGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Jean ZhangGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Jingye ZhouGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Christine P DonahueGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Jeffrey A MesserGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
David HolmesGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Christopher C Arico-MuendelGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
Andrew J PopeGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Jeffrey W GrossGlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Ghotas EvindarGlaxoSmithKline, 830 Winter Street, Waltham, Massachusetts 02451, USA.
South College · USGlaxoSmithKline (United States) · USGlaxoSmithKline (Spain) · ESUniversity of Birmingham · GB
Funding
No grant is acknowledged in the PubMed record.
Abstract
The identification and prioritization of chemically tractable therapeutic targets is a significant challenge in the discovery of new medicines. We have developed a novel method that rapidly screens multiple proteins in parallel using DNA-encoded library technology (ELT). Initial efforts were focused on the efficient discovery of antibacterial leads against 119 targets from Acinetobacter baumannii and Staphylococcus aureus. The success of this effort led to the hypothesis that the relative number of ELT binders alone could be used to assess the ligandability of large sets of proteins. This concept was further explored by screening 42 targets from Mycobacterium tuberculosis. Active chemical series for six targets from our initial effort as well as three chemotypes for DHFR from M. tuberculosis are reported. The findings demonstrate that parallel ELT selections can be used to assess ligandability and highlight opportunities for successful lead and tool discovery.
Indexed as
Gene LibrarySmall Molecule LibrariesAcinetobacter baumanniiAnti-Bacterial AgentsDrug DiscoveryDrug Evaluation, PreclinicalMolecular Targeted TherapyMycobacterium tuberculosisStaphylococcus aureusAnti-Bacterial AgentsSmall Molecule Libraries
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