ArticleJournal of medicinal chemistry2016
Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1.
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Article in Journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers, 1 of them a synthesis that pooled it.
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24citing papers in PubMed, 1 pooled it
3.3field-weighted citation impact, top 8% of its field
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
24 citing papers in PubMed, 1 synthesis or guideline pooled it, 48 citations in OpenAlex.
- COVID-19 outbreak: history, mechanism, transmission, structural studies and therapeutics.Infection · 2021Pooled it
- "MIDA masking" of boronic acid therapeutics for enhanced stability and economy.RSC chemical biology · 2026Article
- Triptolide sensitizes cancer cells to nucleoside DNA methyltransferase inhibitors through inhibition of DCTPP1-mediated cell-intrinsic resistance.Nature communications · 2026Article
- A Comprehensive Understanding ofCurrent issues in molecular biology · 2026Review
- Structural and cellular insights into DCTPP1 antagonists and their synergistic action with DNMT inhibitors.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- DCTPP1 orchestrates dCTP pool dynamics and mtDNA stability in quiescent cells.Cell death & disease · 2026Article
- Bench-Stable Boryl Thianthrenium Dication Enables Aziridinyl Boronate Synthesis via Metal-Free Late-Stage Aziridination with Diverse Nitrogen Nucleophiles.Angewandte Chemie (International ed. in English) · 2026Article
- Recent Advancements in the Diversification and Applications of Boron-Containing Compounds in Medicinal Chemistry.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Recent Development of Boron-Containing Small-Molecule Anticancer Agents.ACS pharmacology & translational science · 2025Review
- Potential of Boronic Acid Derivatization and Activity in Agrochemical Discovery.Molecules (Basel, Switzerland) · 2025Review
- Article
- Identification and evaluation of small-molecule inhibitors against the dNTPase SAMHD1 via a comprehensive screening funnel.iScience · 2024Article
- Organoboronic acids/esters as effective drug and prodrug candidates in cancer treatments: challenge and hope.Journal of enzyme inhibition and medicinal chemistry · 2023Review
- Preparation of MIDA Anhydride and Reaction with Boronic Acids.Organic syntheses; an annual publication of satisfactory methods for the preparation of organic chemicals · 2022Article
- Recent developments in the medicinal chemistry of single boron atom-containing compounds.Acta pharmaceutica Sinica. B · 2021Review
- DCTPP1 prevents a mutator phenotype through the modulation of dCTP, dTTP and dUTP pools.Cellular and molecular life sciences : CMLS · 2020Article
- A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing.bioRxiv : the preprint server for biology · 2020Article
- Article
- Review
- Toward Generalization of Iterative Small Molecule Synthesis.Nature reviews. Chemistry · 2018Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
29 authors at 7 institutions in 4 countries.
Sabin Llona-Minguez *Division of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Andreas Höglund *Division of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Sylvain A JacquesDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Lars JohanssonDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
José Manuel Calderón-MontañoDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Magnus ClaessonDepartment of Biochemistry and Biophysics, Stockholm University, Svante Arrhenius väg 16C, SE-106 91 Stockholm, Sweden.
Olga LosevaDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Nicholas C K ValerieDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Thomas LundbäckDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Javier PiedrafitaTorrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, California 92121, United States.
Giovanni MagaIstituto di Genetica Molecolare, IGM-CNR, Via Abbiategrasso 207, 27100 Pavia, Italy.
Emmanuele CrespanIstituto di Genetica Molecolare, IGM-CNR, Via Abbiategrasso 207, 27100 Pavia, Italy.
Laurent MeijerManRos Therapeutics, Perharidy Research Center, 29680 Roscoff, Bretagne, France.
Estefanía Burgos MorónDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Pawel BaranczewskiDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Ann-Louise HagbjörkUppsala University Drug Optimization and Pharmaceutical Profiling Platform (UDOPP), Department of Pharmacy, Science for Life Laboratory, Uppsala University, Uppsala, Sweden.
Richard SvenssonUppsala University Drug Optimization and Pharmaceutical Profiling Platform (UDOPP), Department of Pharmacy, Science for Life Laboratory, Uppsala University, Uppsala, Sweden.
Elisee WiitaDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Ingrid AlmlöfDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Torkild VisnesDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Fredrik JeppssonDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Kristmundur SigmundssonDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Annika Jenmalm JensenDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Per ArturssonUppsala University Drug Optimization and Pharmaceutical Profiling Platform (UDOPP), Department of Pharmacy, Science for Life Laboratory, Uppsala University, Uppsala, Sweden.
Ann-Sofie JemthDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Pål StenmarkDepartment of Biochemistry and Biophysics, Stockholm University, Svante Arrhenius väg 16C, SE-106 91 Stockholm, Sweden.
Ulrika Warpman BerglundDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Martin ScobieDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Thomas HelledayDivision of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm, Sweden.
Science for Life Laboratory · SEKarolinska Institutet · SEUppsala University · SEIstituto di Genetica Molecolare · ITStockholm University · SEGeneral Atomics (United States) · USManRos Therapeutics (France) · FR
Funding
European Research Council 268815
Abstract
The dCTPase pyrophosphatase 1 (dCTPase) regulates the intracellular nucleotide pool through hydrolytic degradation of canonical and noncanonical nucleotide triphosphates (dNTPs). dCTPase is highly expressed in multiple carcinomas and is associated with cancer cell stemness. Here we report on the development of the first potent and selective dCTPase inhibitors that enhance the cytotoxic effect of cytidine analogues in leukemia cells. Boronate 30 displays a promising in vitro ADME profile, including plasma and mouse microsomal half-lives, aqueous solubility, cell permeability and CYP inhibition, deeming it a suitable compound for in vivo studies.
Indexed as
Drug DiscoveryDose-Response Relationship, DrugEnzyme InhibitorsHL-60 CellsHumansLigandsMolecular StructurePyrophosphatasesStructure-Activity RelationshipdCTP pyrophosphataseEnzyme InhibitorsLigandsPyrophosphatases
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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.