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Thrombin-activated receptors: promising targets for cancer therapy?
A central aspect of this review is that directed to summarize the approaches that have been followed to the search of PAR-1 antagonists, illustrating with some significant examples the scarce data concerning the effects of these antagonists on anticancer assay models.
Conformationally restricted PACAP27 analogues incorporating type II/II' IBTM beta-turn mimetics. Synthesis, NMR structure determination, and binding affinity.
Compounds 1 and 2, two conformationally restricted analogues of PACAP27 incorporating respectively (S)- or (R)-IBTM as type II or II' beta-turn dipeptide mimetic at the Y10-S11 position, were synthesized and the data seem more compatible with a segment of the alpha-helix than with the Beta-turn previously proposed for this fragment.
Pharmacological evaluation of IQM‐95,333, a highly selective CCKA receptor antagonist with anxiolytic‐like activity in animal models
In conclusion, IQM‐95,333 is a potent and selective CCKA receptor antagonist both in vitro and in vivo with an anxiolytic‐like activity in two different animal models, which can only be attributed to blockade of this CCK receptor subtype.
Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists.
The synthesis and stereochemical structure--activity relationships of a new class of potent and selective non-peptide cholecystokinin-A (CCK-A) receptor antagonists based on the
A facile synthesis of ascamycin and related analogues
Abstract The nucleoside antibiotic ascamycin [2-chloro-5'- O -[ N -( L-alanyl )sulfamoyl] adenosine 1 ] has been synthesized by an improved procedure involving the direct condensation of
Gly-Pro-Glu protects &bgr;-amyloid-induced somatostatin depletion in the rat cortex
Results indicate that GPE may have an in vivo effect protecting the temporal cortical somatostatinergic system from A&bgr; insult.
Quaternary α,α-2-oxoazepane α-amino acids: synthesis from ornithine-derived β-lactams and incorporation into model dipeptides.
Molecular modeling and NMR experiments indicate that these quaternary amino acids are able to drive the adoption of β-turn secondary structures when incorporated in model dipeptide derivatives.
Alkylating nucleosides. 4. Synthesis and cytostatic activity of chloro- and iodomethylpyrazole nucleosides.
Chloromethyl-substituted nucleotides showed moderate activities against HeLa cells, while all the corresponding iodometHyl derivatives exhibited high activities.