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Roscovitine Targets, Protein Kinases and Pyridoxal Kinase*[boxs]
(R)-Roscovitine (CYC202) is often referred to as a “selective inhibitor of cyclin-dependent kinases.” Besides its use as a biological tool in cell cycle, neuronal functions, and apoptosis studies, itExpand
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Isolation of drugs active against mammalian prions using a yeast-based screening assay
We have developed a rapid, yeast-based, two-step assay to screen for antiprion drugs. The method allowed us to identify several compounds effective against budding yeast prions responsible for theExpand
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CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases
Among the ten pharmacological inhibitors of cyclin-dependent kinases (CDKs) currently in clinical trials, the purine roscovitine (CYC202, Seliciclib) is undergoing phase 2 trials againstExpand
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FAF-Drugs2: Free ADME/tox filtering tool to assist drug discovery and chemical biology projects
TLDR
This paper presents FAF-Drugs2, a free adaptable tool for ADMET filtering of electronic compound collections. Expand
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Antihypertensive Drug Guanabenz Is Active In Vivo against both Yeast and Mammalian Prions
Background Prion-based diseases are incurable transmissible neurodegenerative disorders affecting animals and humans. Methodology/Principal Findings Here we report the discovery of the in vivoExpand
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Protein Folding Activity of Ribosomal RNA Is a Selective Target of Two Unrelated Antiprion Drugs
Background 6-Aminophenanthridine (6AP) and Guanabenz (GA, a drug currently in use for the treatment of hypertension) were isolated as antiprion drugs using a yeast-based assay. These structurallyExpand
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CDK inhibitors R-roscovitine and S-CR8 effectively block renal and hepatic cystogenesis in an orthologous model of ADPKD
Autosomal dominant polycystic kidney disease (ADPKD) and other forms of PKD are associated with dysregulated cell cycle and proliferation. Although no effective therapy for the treatment of PKD isExpand
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Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1.
Cyclin-dependent kinases (CDKs) and casein kinases 1 (CK1) are involved in the two key molecular features of Alzheimer's disease, production of amyloid-beta peptides (extracellular plaques) andExpand
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The FAF-Drugs2 server: a multistep engine to prepare electronic chemical compound collections
TLDR
SUMMARY The FAF-Drugs2 server is a web application that prepares chemical compound libraries prior to virtual screening or that assists hit selection/lead optimization before chemical synthesis or ordering. Expand
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CDK Inhibitors Roscovitine and CR8 Trigger Mcl-1 Down-Regulation and Apoptotic Cell Death in Neuroblastoma Cells.
Neuroblastoma (NB), the most frequent extracranial solid tumor of children accounting for nearly 15% of all childhood cancer mortality, displays overexpression of antiapoptotic Bcl-2 and Mcl-1 inExpand
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