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Antibacterial agents based on the cyclic d,l-α-peptide architecture
It is reported that six- and eight-residue cyclic d,l-α-peptides act preferentially on Gram-positive and/or Gram-negative bacterial membranes compared to mammalian cells, increase membrane permeability, collapse transmembrane ion potentials, and cause rapid cell death.
Antibacterial agents based on the cyclic D,L-alpha-peptide architecture.
It is reported that six- and eight-residue cyclic d,l-alpha-peptides act preferentially on Gram-positive and/or Gram-negative bacterial membranes compared to mammalian cells, increase membrane permeability, collapse transmembrane ion potentials, and cause rapid cell death.
Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor.
A Novel Triazolopyridine-Based Spleen Tyrosine Kinase Inhibitor That Arrests Joint Inflammation
CC-509 is a potent, moderately selective, and efficacious inhibitor of Syk that has a differentiated profile when compared to other Syk compounds that have progressed into the clinic for RA.
Aminopurine based JNK inhibitors for the prevention of ischemia reperfusion injury.
Spleen tyrosine kinase promotes acute neutrophil-mediated glomerular injury via activation of JNK and p38 MAPK in rat nephrotoxic serum nephritis
- J. Ryan, F. Ma, J. Kanellis, M. Delgado, K. Blease, D. Nikolic-Paterson
- Biology, MedicineLaboratory Investigation
- 5 September 2011
It is demonstrated that Syk signalling is required for JNK and p38 MAPK signalling and acute neutrophil-dependent glomerular injury in rat NTN, which identifies Syk as a potential therapeutic target in antibody-dependent kidney disease.
correction: Antibacterial agents based on the cyclic d,l-α-peptide architecture
This corrects the article DOI: 35086601
Discovery of the c-Jun N-Terminal Kinase Inhibitor CC-90001.
The synthesis and structure-activity relationship (SAR) studies for a novel series of JNK inhibitors demonstrating an increased JNK1 bias resulted in compounds that demonstrated excellent systemic exposure following oral dosing, enabling in vivo efficacy studies and the selection of a candidate for clinical development.
A Novel mTOR Kinase Inhibitor Causes Growth Inhibition, Cell Cycle Arrest, Apoptosis and Autophagic Cell Death in Mantle Cell Lymphoma Cell Lines: A Distinct Profile from Rapamycin.
It is demonstrated that a selective mTOR kinase inhibitor displays potent anti-proliferative activity in JeKo-1 and Mino cells associated with decreased phosphorylation of S6, p70S6K, AKT S473, 4E-BP1 as well as decreased cyclin D1 levels leading to G1 arrest.