• Publications
  • Influence
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
  • 132
  • 8
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
  • 48
  • 3
  • PDF
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
  • 105
  • 2
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
  • 62
  • 2
Cyclin-dependent kinase inhibitors closer to market launch?
Introduction: Interest in cyclin-dependent kinase (CDK) inhibitors was stimulated by the demonstration that their pharmacological activities could lead to therapies for numerous diseases. Until now,Expand
  • 30
  • 2
TRPC6 channel translocation into phagosomal membrane augments phagosomal function
Significance Historically, pulmonary infections treated with antibiotics killed bacteria while selecting for the unintended development of pathogenic resistance. One strategy to circumvent antibioticExpand
  • 34
  • 2
  • PDF
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?
Increased production of amyloid-β (Aβ)42 peptide, derived from the amyloid-β protein precursor, and its subsequent aggregation into oligomers and plaques constitutes a hallmark of Alzheimer's diseaseExpand
  • 14
  • 2
  • PDF
Cyclin-dependent kinase inhibitors: a survey of recent patent literature
Importance of the field: Abnormalities in protein phosphorylation by cyclin-dependent kinases (CDKs) have been observed in numerous major human diseases, which has strongly encouraged the search forExpand
  • 53
  • 1
Identification of Soluble Candidate Biomarkers of Therapeutic Response to Sunitinib in Medullary Thyroid Carcinoma in Preclinical Models
Purpose: Medullary thyroid carcinoma (MTC), an aggressive rare tumor due to activating mutations in the proto-oncogene RET, requires new therapeutic strategies. Sunitinib, a potent inhibitor of RET,Expand
  • 36
  • 1
  • PDF
Targeting low molecular weight cyclin E (LMW-E) in breast cancer
Low molecular weight cyclin E (LMW-E) plays an important oncogenic role in breast cancer. LMW-E, which is not found in normal tissue, can promote the formation of aggressive tumors and can lead toExpand
  • 31
  • 1