ArticleACS medicinal chemistry letters2019
Rational Design of Cell-Active Inhibitors of PARP10.
Article in ACS medicinal chemistry letters, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
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The trial behind it
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Who cites it
16 citing papers in PubMed, 31 citations in OpenAlex.
- Targeting MARylation and DePARylation in Cancer Therapy: New Promising Therapeutic Opportunities.Cancers · 2025Review
- [1,2,4]Triazolo[3,4-Journal of medicinal chemistry · 2023Article
- Structurally distinct PARP7 inhibitors provide new insights into the function of PARP7 in regulating nucleic acid-sensing and IFN-β signaling.Cell chemical biology · 2023Article
- Structure-guided design and characterization of a clickable, covalent PARP16 inhibitor.Chemical science · 2022Article
- Medicinal Chemistry Perspective on Targeting Mono-ADP-Ribosylating PARPs with Small Molecules.Journal of medicinal chemistry · 2022Review
- Synthesis, molecular docking, and cytotoxicity of quinazolinone and dihydroquinazolinone derivatives as cytotoxic agents.BMC chemistry · 2022Article
- Article
- Depletion of PARP10 inhibits the growth and metastatic potential of oral squamous cell carcinoma.Frontiers in genetics · 2022Article
- Rational design of selective inhibitors of PARP4.RSC medicinal chemistry · 2021Article
- ADP-Ribosylation as Post-Translational Modification of Proteins: Use of Inhibitors in Cancer Control.International journal of molecular sciences · 2021Review
- Evaluation of 3- and 4-Phenoxybenzamides as Selective Inhibitors of the Mono-ADP-Ribosyltransferase PARP10.ChemistryOpen · 2021Article
- PASTA: PARP activity screening and inhibitor testing assay.STAR protocols · 2021Article
- MARTs and MARylation in the Cytosol: Biological Functions, Mechanisms of Action, and Therapeutic Potential.Cells · 2021Review
- Mono(ADP-ribosyl)ation Enzymes and NADCells · 2021Review
- Integrating DNA-encoded chemical libraries with virtual combinatorial library screening: Optimizing a PARP10 inhibitor.Bioorganic & medicinal chemistry letters · 2020Article
- Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes.SLAS discovery : advancing life sciences R & D · 2020Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Poly-ADP-ribose polymerases (PARPs 1-16) have emerged as major regulators of diverse cellular processes. PARPs can be subclassified based on their ability to catalyze poly-ADP-ribosylation (PARylation) or mono-ADP-ribosylation (MARylation). While much is known about the cellular roles of PARPs that catalyze PARylation (e.g., PARP1), the function of PARPs that catalyze MARylation (e.g., PARP10) is substantially less understood. This is due in large part to the lack of small-molecule inhibitors that are selective for individual PARP family members that catalyze MARylation. Herein, we describe the rational design and synthesis of selective inhibitors of PARP10. Using structure-based design, we targeted a hydrophobic subpocket within the nicotinamide-binding site of PARP10. We synthesized a series of small molecules based on a 3,4-dihydroisoquinolin-1(2
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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.