PMID

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Article Title

Organization

Cholecystokinin antagonists. Synthesis and biological evaluation of 3-substituted benzolactams.

Merck Sharp & Dohme Research Laboratories

Synthesis and biological activity of some partially modified retro-inverso analogues of cholecystokinin.

Centre De Pharmacologie-Endocrinologie (Montpellier, France)

Cholecystokinin antagonists. Synthesis and biological evaluation of 3-substituted 1,4-benzodiazepin-2-amines.

Merck Sharp & Dohme Research Laboratories

Synthesis and biological activities of pseudopeptide analogues of the C-terminal heptapeptide of cholecystokinin. On the importance of the peptide bonds.

TBA

Cholecystokinin antagonists. Synthesis of asperlicin analogues with improved potency and water solubility.

TBA

Molecular Mechanism of Action of Triazolobenzodiazepinone Agonists of the Type 1 Cholecystokinin Receptor. Possible Cooperativity across the Receptor Homodimeric Complex.

Mayo Clinic

Spirotetronate polyketides as leads in drug discovery.

University Of California San Diego

Optimization of the in vitro and in vivo properties of a novel series of 2,4,5-trisubstituted imidazoles as potent cholecystokinin-2 (CCK2) antagonists.

James Black Foundation

5-(tryptophylamino)-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based cholecystokinin receptor antagonists: reversal of CCK1 receptor subtype selectivity toward CCK2 receptors.

Instituto De Qu£Mica M£Dica (Csic)

5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structure-activity relationship studies on the central 1,3-dioxoperhydropyrido[1,2-c]pyrimidine scaffold.

Instituto De Qu£Mica M£Dica (Csic)

5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1)receptor antagonists: structure-activity relationship studies on the substituent at N2-position.

Instituto De Qu£Mica M£Dica (Csic)

beta-Turned dipeptoids as potent and selective CCK(1) receptor antagonists.

Instituto De Qu£Mica M£Dica (Csic)

CCK peptides with combined features of hexa- and tetrapeptide CCK-A agonists.

Astrazeneca R&D Boston

5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.

Insituto De Qu�Mica M�Dica (Csic)

Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor.

University Of Paris

Synthesis and biological evaluation of potent, selective, hexapeptide CCK-A agonist anorectic agents.

Rochester

Synthesis and biological properties of new constrained CCK-B antagonists: discrimination of two affinity states of the CCK-B receptor on transfected CHO cells.

University Of Paris

Peptide-linked 1,3-dialkyl-3-acyltriazenes: gastrin receptor directed antineoplastic alkylating agents.

National Cancer Institute-Frederick

CCK-B agonist or antagonist activities of structurally hindered and peptidase-resistant Boc-CCK4 derivatives.

University Of Paris

Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives.

Rotta Research Laboratorium

Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists.

TBA

Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties.

University Of Paris

 

Pseudopeptide CCK-4 analogues incorporating the [CH(CN)NH] peptide bond surrogate

TBA

 

Identification and biological activity of novel peptidomimetic gastrin/CCK-B receptor agonists

TBA

Highly improved metabolic stability and pharmacokinetics of indium-111-DOTA-gastrin conjugates for targeting of the gastrin receptor.

University Medical Centre Ljubljana

 

CCK-4 restricted analogues containing a 3-oxoindolizidine skeleton

TBA

 

Synthesis and biological activity of 5-heteroaryl benzodiazepines: analogues of YM022

TBA

 

Synthesis and biological activity of 1-alkylcarbonylmethyl analogues of YM022

TBA

 

On the significance of the C-terminal primary amide in cholecystokinin

TBA

 

Structure-based design and pharmacological properties of potent selective and systemically active CCK-B peptidomimetics

TBA

Conformationally constrained CCK4 analogues incorporating IBTM and BTD beta-turn mimetics.

Instituto De QuíMica MéDica (Csic)

Combination of molecular modeling, site-directed mutagenesis, and SAR studies to delineate the binding site of pyridopyrimidine antagonists on the human CCK1 receptor.

Instituto De QuíMica MéDica (Csic)

Effects of the incorporation of IBTM beta-turn mimetics into the dipeptoid CCK(1) receptor agonist PD 170292.

Instituto De QuíMica MéDica (Csic)

Replacement of glycine with dicarbonyl and related moieties in analogues of the C-terminal pentapeptide of cholecystokinin: CCK(2) agonists displaying a novel binding mode.

University Of Paris

Novel constrained CCK-B dipeptoid antagonists derived from pipecolic acid.

University Of Paris

Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists.

Instituto De QuíMica MéDica (Csic)

(3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.

Ferring Research Institute

Chemistry, binding affinities, and behavioral properties of a new class of"antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.

Mayo Foundation

Cholecystokinin peptidomimetics as selective CCK-B antagonists: design, synthesis, and in vitro and in vivo biochemical properties.

University Of Paris

Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.

Solvay Duphar

Synthesis and biological evaluation of cholecystokinin analogs in which the Asp-Phe-NH2 moiety has been replaced by a 3-amino-7-phenylheptanoic acid or a 3-amino-6-(phenyloxy)hexanoic acid.

Ep Cnrs 51