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Cholecystokinin antagonists: Pharmacological and therapeutic potential
  • R. Herranz
  • Biology, Medicine
    Medicinal research reviews
  • 1 September 2003
TLDR
A broad assortment of potent and selective CCK1 and CCK2 antagonists of diverse chemical structure are provided through optimization programs of lead compounds designed based on the structures of the C‐terminal tetrapeptide, CCK‐4, or the non‐peptide natural compound, asperlicin, or derived from random screening programs.
Cholecystokinin antagonists: Pharmacological and therapeutic potential
  • R. Herranz
  • Biology, Medicine
    Medicinal research reviews
  • 1 September 2003
TLDR
A broad assortment of potent and selective CCK1 and CCK2 antagonists of diverse chemical structure are provided through optimization programs of lead compounds designed based on the structures of the C‐terminal tetrapeptide, CCK‐4, or the non‐peptide natural compound, asperlicin, or derived from random screening programs.
Thrombin-activated receptors: promising targets for cancer therapy?
TLDR
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.
Pharmacological evaluation of IQM‐95,333, a highly selective CCKA receptor antagonist with anxiolytic‐like activity in animal models
TLDR
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
The N‐terminal tripeptide of insulin‐like growth factor‐I protects against β‐amyloid‐induced somatostatin depletion by calcium and glycogen synthase kinase 3β modulation
TLDR
The findings suggest that GPE, but not its metabolite, mimics insulin‐like growth factor I effects on the SRIF system through a mechanism independent of Aβ clearance that involves modulation of calcium and glycogen synthase kinase 3β signaling.
From Multiple PAR1 Receptor/Protein Interactions to their Multiple Therapeutic Implications.
TLDR
An overview on the complex PAR1 interactome is given, its therapeutic impact upon the cardiovascular, immune and nervous systems, inflammation and cancer, as well as, on its modulation with agonists and antagonists.
beta-Turned dipeptoids as potent and selective CCK(1) receptor antagonists.
TLDR
It is proposed that the presence of a beta-turn-like conformation within the peptide backbone of dipeptoids could contribute to their bioactive conformation at the CCK(1) receptor subtype.
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