ArticleRSC medicinal chemistry2022
PAC-FragmentDEL - photoactivated covalent capture of DNA-encoded fragments for hit discovery.
Open access · hybridAbstract read
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Article in RSC medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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0cells of the map it votes in
10citing papers in PubMed
2.3field-weighted citation impact, top 11% of its field
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
10 citing papers in PubMed, 29 citations in OpenAlex.
- Developments and challenges in hit progression within fragment-based drug discovery.Nature communications · 2026Review
- Target Agnostic Photoaffinity Labelling by Sulfonylhydrazones.Angewandte Chemie (International ed. in English) · 2025Article
- Short and High-Yielding Synthesis of a Minimalist Diazirine-Alkyne Photo-Cross-Linker and Photoaffinity Labeling Derivatives.ACS omega · 2025Article
- Click Chemistry Methodology: The Novel Paintbrush of Drug Design.ACS chemical biology · 2025Review
- Fragment-based drug discovery campaigns guided by native mass spectrometry.RSC medicinal chemistry · 2024Review
- Building Block-Centric Approach to DNA-Encoded Library Design.Journal of chemical information and modeling · 2024Article
- Small-molecule discovery through DNA-encoded libraries.Nature reviews. Drug discovery · 2023Review
- Two-Step Validation Approach for Tools To Study the DNA Repair Enzyme SNM1A.Chembiochem : a European journal of chemical biology · 2023Article
- Translating the Genome into Drugs.Accounts of chemical research · 2023Article
- Reactivity of Covalent Fragments and Their Role in Fragment Based Drug Discovery.Pharmaceuticals (Basel, Switzerland) · 2022Review
Corrections and comments
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Authors and funding
23 authors at 1 institution in 1 country.
Huiyong MaHitGen Inc. Building 6, No. 8 Huigu First East Road, Tianfu International Bio-Town, Shuangliu District Chengdu 610000 Sichuan P. R. China huiyong.ma@hitgen.com hd.luo@hitgen.com xm.cheng@hitgen.com qx.chen@hitgen.com chao.song@hitgen.com cong.duan@hitgen.com ping.tan@hitgen.com lf.zhang@hitgen.com jian.liu@hitgen.com barry.morgan@hitgen.com jin.li@hitgen.com jq.wan@hitgen.com gs.liu@hitgen.com.ORCID https://orcid.org/0000-0002-5220-1707
James B MurrayVernalis (R&D) Ltd Granta Park, Abington Cambridge CB21 6GB UK r.hubbard@vernalis.com j.murray@vernalis.com l.baker@vernalis.com w.finnie@vernalis.com l.guetzoyan@vernalis.com r.harris@vernalis.com n.hendrickson@vernalis.com natalia_matassova@hotmail.com h.simmonite@vernalis.com j.smith@vernalis.com r.hubbard@vernalis.com.
Huadong LuoHitGen Inc. Building 6, No. 8 Huigu First East Road, Tianfu International Bio-Town, Shuangliu District Chengdu 610000 Sichuan P. R. China huiyong.ma@hitgen.com hd.luo@hitgen.com xm.cheng@hitgen.com qx.chen@hitgen.com chao.song@hitgen.com cong.duan@hitgen.com ping.tan@hitgen.com lf.zhang@hitgen.com jian.liu@hitgen.com barry.morgan@hitgen.com jin.li@hitgen.com jq.wan@hitgen.com gs.liu@hitgen.com.
Xuemin ChengHitGen Inc. Building 6, No. 8 Huigu First East Road, Tianfu International Bio-Town, Shuangliu District Chengdu 610000 Sichuan P. R. China huiyong.ma@hitgen.com hd.luo@hitgen.com xm.cheng@hitgen.com qx.chen@hitgen.com chao.song@hitgen.com cong.duan@hitgen.com ping.tan@hitgen.com lf.zhang@hitgen.com jian.liu@hitgen.com barry.morgan@hitgen.com jin.li@hitgen.com jq.wan@hitgen.com gs.liu@hitgen.com.
Qiuxia ChenHitGen Inc. Building 6, No. 8 Huigu First East Road, Tianfu International Bio-Town, Shuangliu District Chengdu 610000 Sichuan P. R. China huiyong.ma@hitgen.com hd.luo@hitgen.com xm.cheng@hitgen.com qx.chen@hitgen.com chao.song@hitgen.com cong.duan@hitgen.com ping.tan@hitgen.com lf.zhang@hitgen.com jian.liu@hitgen.com barry.morgan@hitgen.com jin.li@hitgen.com jq.wan@hitgen.com gs.liu@hitgen.com.ORCID https://orcid.org/0000-0001-5074-5324
Chao SongHitGen Inc. Building 6, No. 8 Huigu First East Road, Tianfu International Bio-Town, Shuangliu District Chengdu 610000 Sichuan P. R. China huiyong.ma@hitgen.com hd.luo@hitgen.com xm.cheng@hitgen.com qx.chen@hitgen.com chao.song@hitgen.com cong.duan@hitgen.com ping.tan@hitgen.com lf.zhang@hitgen.com jian.liu@hitgen.com barry.morgan@hitgen.com jin.li@hitgen.com jq.wan@hitgen.com gs.liu@hitgen.com.
Cong DuanHitGen Inc. Building 6, No. 8 Huigu First East Road, Tianfu International Bio-Town, Shuangliu District Chengdu 610000 Sichuan P. R. China huiyong.ma@hitgen.com hd.luo@hitgen.com xm.cheng@hitgen.com qx.chen@hitgen.com chao.song@hitgen.com cong.duan@hitgen.com ping.tan@hitgen.com lf.zhang@hitgen.com jian.liu@hitgen.com barry.morgan@hitgen.com jin.li@hitgen.com jq.wan@hitgen.com gs.liu@hitgen.com.
Ping TanHitGen Inc. Building 6, No. 8 Huigu First East Road, Tianfu International Bio-Town, Shuangliu District Chengdu 610000 Sichuan P. R. China huiyong.ma@hitgen.com hd.luo@hitgen.com xm.cheng@hitgen.com qx.chen@hitgen.com chao.song@hitgen.com cong.duan@hitgen.com ping.tan@hitgen.com lf.zhang@hitgen.com jian.liu@hitgen.com barry.morgan@hitgen.com jin.li@hitgen.com jq.wan@hitgen.com gs.liu@hitgen.com.
Lifang ZhangHitGen Inc. Building 6, No. 8 Huigu First East Road, Tianfu International Bio-Town, Shuangliu District Chengdu 610000 Sichuan P. R. China huiyong.ma@hitgen.com hd.luo@hitgen.com xm.cheng@hitgen.com qx.chen@hitgen.com chao.song@hitgen.com cong.duan@hitgen.com ping.tan@hitgen.com lf.zhang@hitgen.com jian.liu@hitgen.com barry.morgan@hitgen.com jin.li@hitgen.com jq.wan@hitgen.com gs.liu@hitgen.com.
Jian LiuHitGen Inc. Building 6, No. 8 Huigu First East Road, Tianfu International Bio-Town, Shuangliu District Chengdu 610000 Sichuan P. R. China huiyong.ma@hitgen.com hd.luo@hitgen.com xm.cheng@hitgen.com qx.chen@hitgen.com chao.song@hitgen.com cong.duan@hitgen.com ping.tan@hitgen.com lf.zhang@hitgen.com jian.liu@hitgen.com barry.morgan@hitgen.com jin.li@hitgen.com jq.wan@hitgen.com gs.liu@hitgen.com.
Barry A MorganHitGen Inc. Building 6, No. 8 Huigu First East Road, Tianfu International Bio-Town, Shuangliu District Chengdu 610000 Sichuan P. R. China huiyong.ma@hitgen.com hd.luo@hitgen.com xm.cheng@hitgen.com qx.chen@hitgen.com chao.song@hitgen.com cong.duan@hitgen.com ping.tan@hitgen.com lf.zhang@hitgen.com jian.liu@hitgen.com barry.morgan@hitgen.com jin.li@hitgen.com jq.wan@hitgen.com gs.liu@hitgen.com.
Jin LiHitGen Inc. Building 6, No. 8 Huigu First East Road, Tianfu International Bio-Town, Shuangliu District Chengdu 610000 Sichuan P. R. China huiyong.ma@hitgen.com hd.luo@hitgen.com xm.cheng@hitgen.com qx.chen@hitgen.com chao.song@hitgen.com cong.duan@hitgen.com ping.tan@hitgen.com lf.zhang@hitgen.com jian.liu@hitgen.com barry.morgan@hitgen.com jin.li@hitgen.com jq.wan@hitgen.com gs.liu@hitgen.com.
Jinqiao WanHitGen Inc. Building 6, No. 8 Huigu First East Road, Tianfu International Bio-Town, Shuangliu District Chengdu 610000 Sichuan P. R. China huiyong.ma@hitgen.com hd.luo@hitgen.com xm.cheng@hitgen.com qx.chen@hitgen.com chao.song@hitgen.com cong.duan@hitgen.com ping.tan@hitgen.com lf.zhang@hitgen.com jian.liu@hitgen.com barry.morgan@hitgen.com jin.li@hitgen.com jq.wan@hitgen.com gs.liu@hitgen.com.ORCID https://orcid.org/0000-0003-3597-2398
Lisa M BakerVernalis (R&D) Ltd Granta Park, Abington Cambridge CB21 6GB UK r.hubbard@vernalis.com j.murray@vernalis.com l.baker@vernalis.com w.finnie@vernalis.com l.guetzoyan@vernalis.com r.harris@vernalis.com n.hendrickson@vernalis.com natalia_matassova@hotmail.com h.simmonite@vernalis.com j.smith@vernalis.com r.hubbard@vernalis.com.ORCID https://orcid.org/0000-0003-2002-0941
William FinnieVernalis (R&D) Ltd Granta Park, Abington Cambridge CB21 6GB UK r.hubbard@vernalis.com j.murray@vernalis.com l.baker@vernalis.com w.finnie@vernalis.com l.guetzoyan@vernalis.com r.harris@vernalis.com n.hendrickson@vernalis.com natalia_matassova@hotmail.com h.simmonite@vernalis.com j.smith@vernalis.com r.hubbard@vernalis.com.
Lucie GuetzoyanVernalis (R&D) Ltd Granta Park, Abington Cambridge CB21 6GB UK r.hubbard@vernalis.com j.murray@vernalis.com l.baker@vernalis.com w.finnie@vernalis.com l.guetzoyan@vernalis.com r.harris@vernalis.com n.hendrickson@vernalis.com natalia_matassova@hotmail.com h.simmonite@vernalis.com j.smith@vernalis.com r.hubbard@vernalis.com.
Richard HarrisVernalis (R&D) Ltd Granta Park, Abington Cambridge CB21 6GB UK r.hubbard@vernalis.com j.murray@vernalis.com l.baker@vernalis.com w.finnie@vernalis.com l.guetzoyan@vernalis.com r.harris@vernalis.com n.hendrickson@vernalis.com natalia_matassova@hotmail.com h.simmonite@vernalis.com j.smith@vernalis.com r.hubbard@vernalis.com.ORCID https://orcid.org/0000-0001-7459-1745
Nicole HendricksonVernalis (R&D) Ltd Granta Park, Abington Cambridge CB21 6GB UK r.hubbard@vernalis.com j.murray@vernalis.com l.baker@vernalis.com w.finnie@vernalis.com l.guetzoyan@vernalis.com r.harris@vernalis.com n.hendrickson@vernalis.com natalia_matassova@hotmail.com h.simmonite@vernalis.com j.smith@vernalis.com r.hubbard@vernalis.com.
Natalia MatassovaVernalis (R&D) Ltd Granta Park, Abington Cambridge CB21 6GB UK r.hubbard@vernalis.com j.murray@vernalis.com l.baker@vernalis.com w.finnie@vernalis.com l.guetzoyan@vernalis.com r.harris@vernalis.com n.hendrickson@vernalis.com natalia_matassova@hotmail.com h.simmonite@vernalis.com j.smith@vernalis.com r.hubbard@vernalis.com.
Heather SimmoniteVernalis (R&D) Ltd Granta Park, Abington Cambridge CB21 6GB UK r.hubbard@vernalis.com j.murray@vernalis.com l.baker@vernalis.com w.finnie@vernalis.com l.guetzoyan@vernalis.com r.harris@vernalis.com n.hendrickson@vernalis.com natalia_matassova@hotmail.com h.simmonite@vernalis.com j.smith@vernalis.com r.hubbard@vernalis.com.
Julia SmithVernalis (R&D) Ltd Granta Park, Abington Cambridge CB21 6GB UK r.hubbard@vernalis.com j.murray@vernalis.com l.baker@vernalis.com w.finnie@vernalis.com l.guetzoyan@vernalis.com r.harris@vernalis.com n.hendrickson@vernalis.com natalia_matassova@hotmail.com h.simmonite@vernalis.com j.smith@vernalis.com r.hubbard@vernalis.com.
Roderick E HubbardVernalis (R&D) Ltd Granta Park, Abington Cambridge CB21 6GB UK r.hubbard@vernalis.com j.murray@vernalis.com l.baker@vernalis.com w.finnie@vernalis.com l.guetzoyan@vernalis.com r.harris@vernalis.com n.hendrickson@vernalis.com natalia_matassova@hotmail.com h.simmonite@vernalis.com j.smith@vernalis.com r.hubbard@vernalis.com.ORCID https://orcid.org/0000-0002-8233-7461
Guansai LiuHitGen Inc. Building 6, No. 8 Huigu First East Road, Tianfu International Bio-Town, Shuangliu District Chengdu 610000 Sichuan P. R. China huiyong.ma@hitgen.com hd.luo@hitgen.com xm.cheng@hitgen.com qx.chen@hitgen.com chao.song@hitgen.com cong.duan@hitgen.com ping.tan@hitgen.com lf.zhang@hitgen.com jian.liu@hitgen.com barry.morgan@hitgen.com jin.li@hitgen.com jq.wan@hitgen.com gs.liu@hitgen.com.ORCID https://orcid.org/0000-0001-8925-6093
Granta Design (United Kingdom) · GB
Funding
No grant is acknowledged in the PubMed record.
Abstract
We describe a novel approach for screening fragments against a protein that combines the sensitivity of DNA-encoded library technology with the ability of fragments to explore what will bind. Each of the members of the library consists of a fragment which is linked to a photoactivatable diazirine moiety. Split and pool synthesis combines each fragment with a set of linkers with the version of the library reported here containing some 70k different compounds, each with an individual DNA code. Incubation of the library with a protein sample is followed by photoactivation, washing and subsequent PCR and sequencing which allows the individual fragment hits to be identified. We illustrate how the approach allows successful hit fragment identification using only microgram quantities of material for two targets. PAK4 is a kinase for which conventional fragment screening has generated many advance leads. The as yet undrugged target, 2-epimerase, presents a more challenging active site for identification of hit compounds. In both cases, PAC-FragmentDEL identified fragments validated as hits by ligand-observed NMR measurements and crystal structure determination of off-DNA sample binding to the proteins.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.