Literature DB >> 2994227

A potent nonpeptide cholecystokinin antagonist selective for peripheral tissues isolated from Aspergillus alliaceus.

R S Chang, V J Lotti, R L Monaghan, J Birnbaum, E O Stapley, M A Goetz, G Albers-Schönberg, A A Patchett, J M Liesch, O D Hensens.   

Abstract

A new, competitive, nonpeptide cholecystokinin (CCK) antagonist, asperlicin, was isolated from the fungus Aspergillus alliaceus. The compound has 300 to 400 times the affinity for pancreatic, ileal, and gallbladder CCK receptors than proglumide, a standard agent of this class. Moreover, asperlicin is highly selective for peripheral CCK receptors relative to brain CCK and gastrin receptors. Since asperlicin also exhibits long-lasting CCK antagonist activity in vivo, it should provide a valuable tool for investigating the physiological and pharmacological actions of CCK.

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Year:  1985        PMID: 2994227     DOI: 10.1126/science.2994227

Source DB:  PubMed          Journal:  Science        ISSN: 0036-8075            Impact factor:   47.728


  38 in total

1.  Synthesis and diversification of 1,2,3-triazole-fused 1,4-benzodiazepine scaffolds.

Authors:  James R Donald; Stephen F Martin
Journal:  Org Lett       Date:  2011-01-28       Impact factor: 6.005

Review 2.  Mass receptor screening for new drugs.

Authors:  R M Burch; D J Kyle
Journal:  Pharm Res       Date:  1991-02       Impact factor: 4.200

3.  Comparative molecular field analysis of CCK-A antagonists using field-fit as an alignment technique. A convenient guide to design new CCK-A ligands.

Authors:  S Rault; R Bureau; J C Pilo; M Robba
Journal:  J Comput Aided Mol Des       Date:  1992-12       Impact factor: 3.686

4.  Effect of loxiglumide (CR-1505) on bombesin- and meal-stimulated plasma cholecystokinin in man.

Authors:  J B Jansen; M C Jebbink; B R Douglas; C B Lamers
Journal:  Eur J Clin Pharmacol       Date:  1990       Impact factor: 2.953

5.  The cholecystokinin receptor antagonist L-364,718 reduces taurocholate-induced pancreatitis in rats.

Authors:  K H Kim; M G Lee; D G Kim
Journal:  Int J Pancreatol       Date:  1996-12

Review 6.  General lack of structural characterization of chemically synthesized long peptides.

Authors:  Jean A Boutin; André L Tartar; Alain van Dorsselaer; Hubert Vaudry
Journal:  Protein Sci       Date:  2019-03-25       Impact factor: 6.725

7.  Differential effects of proglumide on mesolimbic and nigrostriatal dopamine function.

Authors:  J G Csernansky; S Glick; J Mellentin
Journal:  Psychopharmacology (Berl)       Date:  1987       Impact factor: 4.530

Review 8.  Drug discovery--today and tomorrow: the role of medicinal chemistry.

Authors:  K R Freter
Journal:  Pharm Res       Date:  1988-07       Impact factor: 4.200

9.  Design of potent, orally effective, nonpeptidal antagonists of the peptide hormone cholecystokinin.

Authors:  B E Evans; M G Bock; K E Rittle; R M DiPardo; W L Whitter; D F Veber; P S Anderson; R M Freidinger
Journal:  Proc Natl Acad Sci U S A       Date:  1986-07       Impact factor: 11.205

10.  Assembly of asperlicin peptidyl alkaloids from anthranilate and tryptophan: a two-enzyme pathway generates heptacyclic scaffold complexity in asperlicin E.

Authors:  Stuart W Haynes; Xue Gao; Yi Tang; Christopher T Walsh
Journal:  J Am Chem Soc       Date:  2012-10-09       Impact factor: 15.419

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