ArticleBioorganic & medicinal chemistry2018
Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2.
Article in Bioorganic & medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed.
- Discovery of Fused Isoquinolinone/Triazole as a Scaffold for Tankyrase and PARP Inhibition.Journal of medicinal chemistry · 2026Article
- Targeting MARylation and DePARylation in Cancer Therapy: New Promising Therapeutic Opportunities.Cancers · 2025Review
- Body-wide genetic deficiency of poly(ADP-ribose) polymerase 14 sensitizes mice to colitis.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2024Article
- Medicinal Chemistry Perspective on Targeting Mono-ADP-Ribosylating PARPs with Small Molecules.Journal of medicinal chemistry · 2022Review
- Research Progress on Mono-ADP-Ribosyltransferases in Human Cell Biology.Frontiers in cell and developmental biology · 2022Review
- ADP-Ribosylation as Post-Translational Modification of Proteins: Use of Inhibitors in Cancer Control.International journal of molecular sciences · 2021Review
- New Reactions of Contraction of theACS omega · 2021Article
- Identification and confirmation of 14-3-3 ζ as a novel target of ginsenosides in brain tissues.Journal of ginseng research · 2021Article
- The potential association between PARP14 and SARS-CoV-2 infection (COVID-19).Future medicinal chemistry · 2021Article
- MARTs and MARylation in the Cytosol: Biological Functions, Mechanisms of Action, and Therapeutic Potential.Cells · 2021Review
- ADP-ribose and analogues bound to the deMARylating macrodomain from the bat coronavirus HKU4.Proceedings of the National Academy of Sciences of the United States of America · 2021Article
- Mono(ADP-ribosyl)ation Enzymes and NADCells · 2021Review
- The Controversial Roles of ADP-Ribosyl Hydrolases MACROD1, MACROD2 and TARG1 in Carcinogenesis.Cancers · 2020Review
- ADP-ribosylation: from molecular mechanisms to human disease.Genetics and molecular biology · 2019Article
- Research Progress on PARP14 as a Drug Target.Frontiers in pharmacology · 2019Review
Corrections and comments
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Authors and funding
13 authors.
Funding
Abstract
The polyadenosine-diphosphate-ribose polymerase 14 (PARP14) has been implicated in DNA damage response pathways for homologous recombination. PARP14 contains three (ADP ribose binding) macrodomains (MD) whose exact contribution to overall PARP14 function in pathology remains unclear. A medium throughput screen led to the identification of N-(2(-9H-carbazol-1-yl)phenyl)acetamide (GeA-69, 1) as a novel allosteric PARP14 MD2 (second MD of PARP14) inhibitor. We herein report medicinal chemistry around this novel chemotype to afford a sub-micromolar PARP14 MD2 inhibitor. This chemical series provides a novel starting point for further development of PARP14 chemical probes.
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Registered trials
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.