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Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.
Pyrazole-based inhibitors of the transforming growth factor-beta type I receptor kinase domain (TbetaR-I) are described and a common binding mode at the active site has been established by successful cocrystallization and X-ray analysis of potent inhibitors with the TbetaR -I receptor Kinase domain.
Kinetic characterization of novel pyrazole TGF-beta receptor I kinase inhibitors and their blockade of the epithelial-mesenchymal transition.
Novel pyrazole compounds are shown to inhibit TGF-beta-induced Smad2 phosphorylation in vivo in NMuMg mammary epithelial cells with potency equivalent to the inhibitory activity in the in vitro kinase assay and provide a foundation for future development of potent and selective TbetaRI kinase inhibitors to treat human disease.
High-affinity aptamers selectively inhibit human nonpancreatic secretory phospholipase A2 (hnps-PLA2).
The affinity and activity of the aptamers demonstrate the ability of the SELEX process to isolate antagonists of nonnucleic-acid-binding proteins from vast oligonucleotide combinatorial libraries.
Leukotriene B4 receptor antagonists: the LY255283 series of hydroxyacetophenones.
A series of hydroxyacetophenones was prepared for evaluation as leukotriene B4 (LTB4) receptor antagonists, culminating in 1-[5-ethyl-2-hydroxy-4-[[6-methyl-6-(1H-tetrazol-5-
Anthranilamide inhibitors of factor Xa.
OVID and SUPER: Two overlap programs for drug design
SUP appears to be a practical brainstorming tool for the medicinal chemist trying to understand how molecules whose structures may not resemble one another in an obvious way can bind to the same site.
Development of a series of phenyltetrazole leukotriene D4 (LTD4) receptor antagonists.
A new structural series of LTD4 receptor antagonists exemplified by 5-[4-phenylbutoxy)phenyl]-2-[4-(tetrazol-5-yl)butyl]2H-t etrazole was designed in which a phenyltetrazole moiety was incorporated as a receptor binding equivalent of the triene unit of LTD 4.
Effects of leukotriene B4 inhalation. Airway sensitization and lung granulocyte infiltration in the guinea pig.
It is concluded that inhaled LTB4 produces airway granulocyte infiltration in the guinea pig and alterations in airway responsiveness that vary with the challenge stimulus and time after exposure.