ArticleJournal of medicinal chemistry2022
Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
Article in Journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 30 citations in OpenAlex.
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- Phosphoinositide-dependent kinase 1 (PDK1) in cancer: molecular insights and therapeutic strategies.Frontiers in chemistry · 2026Review
- Synthetic pancreatic lipase inhibitors in obesity treatment: current updates onRSC medicinal chemistry · 2025Review
- Development of Purine and Pyrrolopyrimidine Scaffolds as Potent, Selective, and Brain Penetrant NUAK1 Inhibitors.ACS medicinal chemistry letters · 2025Article
- Development of Next Generation Cell-Permeable Peptide Inhibitors for the Oncological Target MAGE-A4.Journal of medicinal chemistry · 2025Article
- System biology-based assessment of the molecular mechanism of IMPHY000797 in Parkinson's disease: a network pharmacology and in-silico evaluation.Scientific reports · 2024Article
- Role of CSF1R 550th-tryptophan in kusunokinin and CSF1R inhibitor binding and ligand-induced structural effect.Scientific reports · 2024Article
- Illuminating the druggable genome: Pathways to progress.Drug discovery today · 2024Review
- Extract2Chip-Bypassing Protein Purification in Drug Discovery Using Surface Plasmon Resonance.Biosensors · 2023Article
- Article
- Modulation of tau tubulin kinases (TTBK1 and TTBK2) impacts ciliogenesis.Scientific reports · 2023Article
- Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2.ACS medicinal chemistry letters · 2023Article
- Iron-Catalysed Carbene Transfer to Isocyanides as a Platform for Heterocycle Synthesis.Chemistry (Weinheim an der Bergstrasse, Germany) · 2023Article
- Identification of a chemical probe for lipid kinase phosphatidylinositol-5-phosphate 4-kinase gamma (PI5P4Kγ).Current research in chemical biology · 2023Article
- Unified Access to Pyrimidines and Quinazolines Enabled by N-N Cleaving Carbon Atom Insertion.Journal of the American Chemical Society · 2022Article
- Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of β-Coronaviruses.Journal of medicinal chemistry · 2022Article
- Multitargeting the Action of 5-HTInternational journal of molecular sciences · 2022Review
- AD Informer Set: Chemical tools to facilitate Alzheimer's disease drug discovery.Alzheimer's & dementia (New York, N. Y.) · 2022Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
Abstract
The pyrimidine core has been utilized extensively to construct kinase inhibitors, including eight FDA-approved drugs. Because the pyrimidine hinge-binding motif is accommodated by many human kinases, kinome-wide selectivity of resultant molecules can be poor. This liability was seen as an advantage since it is well tolerated by many understudied kinases. We hypothesized that nonexemplified aminopyrimidines bearing side chains from well-annotated pyrimidine-based inhibitors with off-target activity on understudied kinases would provide us with useful inhibitors of these lesser studied kinases. Our strategy paired mixing and matching the side chains from the 2- and 4-positions of the parent compounds with modifications at the 5-position of the pyrimidine core, which is situated near the gatekeeper residue of the binding pocket. Utilizing this approach, we imparted improved kinome-wide selectivity to most members of the resultant library. Importantly, we also identified potent biochemical and cell-active lead compounds for understudied kinases like DRAK1, BMP2K, and MARK3/4.
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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.