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CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases
TLDR
Results show that second-generation analogues of (R)-roscovitine can be designed with improved antitumor potential and are likely to be effective against non-small-cell lung and nasopharyngeal cancers.
TRPC6 channel translocation into phagosomal membrane augments phagosomal function
TLDR
These data show that enhancing vesicular insertion of the TRPC6 channel to the plasma membrane may represent a general mechanism for restoring phagosome activity in conditions, where it is lost or impaired.
Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1.
TLDR
Modeling of these molecules into the ATP-binding pocket of CK1delta provided a rationale for the increased selectivity toward this kinase, and derivative 13a was able to prevent the CK1-dependent production of amyloid-beta in a cell model.
CDK inhibitors R-roscovitine and S-CR8 effectively block renal and hepatic cystogenesis in an orthologous model of ADPKD
TLDR
Mechanism of action studies demonstrated effective blockade of cell cycle and proliferation and reduction of apoptosis and validate CDK inhibition as a novel and effective approach for the treatment of ADPKD.
CDK Inhibitors Roscovitine and CR8 Trigger Mcl-1 Down-Regulation and Apoptotic Cell Death in Neuroblastoma Cells.
TLDR
Results suggest that the clinical drug roscovitine and its novel analog CR8 induce apoptotic tumor cell death by down-regulating Mcl-1, a key survival factor expressed in all NB cell lines, and may constitute a new approach to treat refractory high-risk NB.
Cyclin-dependent kinase inhibitors closer to market launch?
TLDR
This review coversCDK inhibitor patents published between 2009 and September 2012 and presents compounds currently undergoing clinical development, along with an update of all chemical structures of current interest in the CDK inhibitor field.
Aftins increase amyloid-β42, lower amyloid-β38, and do not alter amyloid-β40 extracellular production in vitro: toward a chemical model of Alzheimer's disease?
TLDR
A family of low molecular weight molecules, the Aftins (Amyloid-β Forty-Two Inducers), which, in cultured cells, dramatically affect the production of extracellular/secreted amyloid peptides and alter the Aβ levels in a fashion similar to that described in the brain of AD patients.
Evaluation of the antiprion activity of 6-aminophenanthridines and related heterocycles.
Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor.
Cyclin-dependent kinase inhibitors: a survey of recent patent literature
TLDR
In most cases, applications have been claimed in the field of cancer; however, potential applications of CDK inhibitors in other therapeutic areas are regularly reported and could herald therapeutic introduction over the next few years.
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