199 articles for thisTarget
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Rationally designed"dipeptoid" analogues of CCK. A Free-Wilson/Fujita-Ban analysis of some alpha-methyltryptophan derivatives as CCK-B antagonists.
Parke-Davis Neuroscience Research Centre
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Jagiellonian University Medical College
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
Elimination of a cholecystokinin receptor agonist 'trigger' in an effort to develop positive allosteric modulators without intrinsic agonist activity.
Mayo Clinic
Development of a time-resolved fluorescence probe for evaluation of competitive binding to the cholecystokinin 2 receptor.
University of Arizona
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
Glaxo Wellcome Research and Development
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist"trigger".
Glaxo Wellcome
3-[2-(N-phenylacetamide)]-1,5-benzodiazepines: orally active, binding selective CCK-A agonists.
Glaxo Wellcome Research and Development
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.
Glaxo Research Institute
Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists II: tuning of receptor selectivity and in vivo efficacy.
Johnson & Johnson Pharmaceutical Research and Development
Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists I: discovery of CCKR1 selectivity in a previously CCKR2-selective lead series.
Johnson & Johnson Pharmaceutical Research and Development
Synthesis and in vitro characterization of radioiodinatable benzodiazepines selective for type 1 and type 2 cholecystokinin receptors.
Mayo Clinic
Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion.
James Black Foundation
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
3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents.
Glaxo Wellcome Research and Development
CCK-A receptor selective antagonists derived from the CCK-A receptor selective tetrapeptide agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623).
Glaxo Research Institute
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
Design and synthesis of trivalent ligands targeting opioid, cholecystokinin, and melanocortin receptors for the treatment of pain.
University of Arizona
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.
Tom'S of Maine
Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
University of Arizona
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)
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
University of Arizona
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.
Merck Research Laboratories
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)
Development of peptide 3D structure mimetics: rational design of novel peptoid cholecystokinin receptor antagonists.
James Black Foundation
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)
Second generation"peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
Warner-Lambert
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
The use of topographical constraints in receptor mapping: investigation of the topographical requirements of the tryptophan 30 residue for receptor binding of Asp-Tyr-D-Phe-Gly-Trp-(N-Me)Nle-Asp-Phe-NH2 (SNF 9007), a cholecystokinin (26-33) analogue that binds to both CCK-B and delta-opioid recepto
University of Arizona
Structure-antigastrin activity relationships of new spiroglumide amido acid derivatives.
Rotta Research Laboratorium
High-affinity and potent, water-soluble 5-amino-1,4-benzodiazepine CCKB/gastrin receptor antagonists containing a cationic solubilizing group.
Merck Sharp and Dohme Research Laboratories
Tetrapeptide CCK-A agonists: effect of backbone N-methylations on in vitro and in vivo CCK activity.
Abbott Laboratories
Peptide-linked 1,3-dialkyl-3-acyltriazenes: gastrin receptor directed antineoplastic alkylating agents.
National Cancer Institute-Frederick
Tetrapeptide CCK agonists: structure-activity studies on modifications at the N-terminus.
Abbott Laboratories
CCK-A-selective tetrapeptides containing lys(N epsilon)-amide residues: favorable in vivo and in vitro effects of N-methylation at the aspartyl residue.
Abbott Laboratories
Cholecystokinin dipeptoid antagonists: design, synthesis, and anxiolytic profile of some novel CCK-A and CCK-B selective and"mixed" CCK-A/CCK-B antagonists.
Parke-Davis Neuroscience Research Centre
Development of 1,4-benzodiazepine cholecystokinin type B antagonists.
Merck Research Laboratories
CCK-B agonist or antagonist activities of structurally hindered and peptidase-resistant Boc-CCK4 derivatives.
University of Paris
Amide bond replacements incorporated into CCK-B selective"dipeptoids".
Parke-Davis Neuroscience Research Center
Rationally designed"dipeptoid" analogues of CCK. Acid mimics of the potent and selective non-peptide CCK-B receptor antagonist CI-988.
Parke-Davis Neuroscience Research Centre
Development of potent and selective CCK-A receptor agonists from Boc-CCK-4: tetrapeptides containing Lys(N epsilon)-amide residues.
Abbott Laboratories
Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives.
Rotta Research Laboratorium
Rationally designed"dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
Parke-Davis Research Unit
Novel glutamic acid derived cholecystokinin receptor ligands.
Merck Sharp & Dohme Research Laboratories
Development of CCK-tetrapeptide analogues as potent and selective CCK-A receptor agonists.
Abbott Laboratories
Benzodiazepine gastrin and brain cholecystokinin receptor ligands: L-365,260.
Merck Sharp & Dohme Research Laboratories
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.
Merck Sharp & Dohme Research Laboratories
Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties.
University of Paris
Design of non-peptide CCK2 and NK1 peptidomimetics using 1-(2-nitrophenyl)thiosemicarbazide as a novel common scaffold.
Novartis Institute For Medical Sciences
The design and synthesis of the high efficacy, non-peptide CCK1 receptor agonist PD170292.
Ccipe-Faculte De Pharmacie
Conversion of acyclic nonpeptide CCK antagonists into CCK agonists
Glaxo Wellcome Research and Development
Design and synthesis of a targeted set of aromatic amino acid derivatives for identification of new lead compounds
TBA
Identification and biological activity of novel peptidomimetic gastrin/CCK-B receptor agonists
TBA
Synthesis of novel iodinated radioligands with high affinity and selectivity for CCK-B/gastrin receptors
TBA
The rational design and synthesis of non-peptide rhegnylogues of CCK-26-33 - a novel series of CCK-A selective ligands
TBA
Synthesis of a potent and selective non-peptide CCK-B/gastrin receptor antagonist tritiated ligand.
TBA
Cholecystokinin analogues: The ergopeptine alkaloids as models of the active conformation of CCK
TBA
New anthranilic acid based antagonists with high affinity and selectivity for the human cholecystokinin receptor 1 (hCCK1-R).
University of Trieste
A sucrose-derived scaffold for multimerization of bioactive peptides.
The University of Arizona
Highly improved metabolic stability and pharmacokinetics of indium-111-DOTA-gastrin conjugates for targeting of the gastrin receptor.
University Medical Centre Ljubljana
Discovery of pyrimidine carboxamides as potent and selective CCK1 receptor agonists.
Merck
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
Synthesis and pharmacological evaluation of highly potent dual histamine H2 and gastrin receptor antagonists
TBA
Design, synthesis, and pharmacological evaluation of dual histamine H2 and gastrin receptor antagonists
TBA
C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCKB/gastrin receptor antagonists
TBA
Potent, selective, water-soluble benzodiazepine-based CCKB receptor antagonists that contain lipophilic carboxylate surrogates
TBA
Alternative strategies towards the identification of chemical lead compounds by rational design
TBA
α-β-didehydrotryptophan as a surrogate for α-methyltryptophan in CCK ‘peptoids’ related to CI-988.
TBA
Selective ligands for cholecystokinin receptor subtypes CCK-A and CCK-B within a single structural class
TBA
Diphenylpyrazolidinone and benzodiazepine cholecystokinin antagonists: A case of convergent evolution in medicinal chemistry
TBA
Toward developing peptidomimetics: Successful replacement of backbone amide bonds in tetrapeptide-based CCK-A receptor agonists
TBA
Structure-based design and pharmacological properties of potent selective and systemically active CCK-B peptidomimetics
TBA
Diastereoselective synthesis of cyclopropyl phenylalanines and their incorporation into dipeptides
TBA
Tryptophan-norleucine 1,5-disubstituted tetrazoles as cis peptide bond mimics: Investigation of the bioactive conformation of a potent and selective peptide for the cholecystokinin-B receptor
TBA
L-708,474: The C5-cyclohexyl analogue of L-365,260, a selective high affinity ligand for the CCKB/gastrin receptor
TBA
1,3,4-trisubstituted pyrrolidinones as scaffolds for construction of peptidomimetic cholecystokinin antagonists
TBA
The synthesis and CCK receptor affinities of selected carboyxlic acid mimics of CI-988 - a potent and selective CCK-B antagonist
TBA
Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands.
University of Minnesota
Discovery of imidazole carboxamides as potent and selective CCK1R agonists.
Merck Research Laboratories
Recent natural products based drug development: a pharmaceutical industry perspective.
Bristol-Myers Squibb Pharmaceutical Research Institute
Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
University of Arizona
Emerging trends of receptor-mediated tumor targeting peptides: A review with perspective from molecular imaging modalities.
Lanzhou University
Identification and optimization of anthranilic sulfonamides as novel, selective cholecystokinin-2 receptor antagonists.
Johnson and Johnson Pharmaceutical Research and Development
Peptide-based long-acting co-agonists of GLP-1 and cholecystokinin 1 receptors as novel anti-diabesity agents.
Jiangsu Normal University
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)
Synthesis and medicinal chemistry of tetronamides: Promising agrochemicals and antitumoral compounds.
Universidade Federal De Minas Gerais
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
University of Nebraska Medical Center
Opportunities for Tapping into Three-Dimensional Chemical Space through a Quaternary Carbon.
St. John'S University
Stabilization Strategies for Linear Minigastrin Analogues: Further Improvements
Medical University of Innsbruck
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
Highly constrained dipeptoid analogues containing a type II' beta-turn mimic as novel and selective CCK-A receptor ligands.
Instituto De QuíMica MéDica (Csic)
Structure-Activity Relationships and Characterization of Highly Selective, Long-Acting, Peptide-Based Cholecystokinin 1 Receptor Agonists.
TBA
Relationship between dihedral angles of N1 and C9 substituents in 1,4-benzodiazepines and dual cholecystokinin-A and -B antagonistic activities.
Fujisawa Pharmaceutical
Novel constrained CCK-B dipeptoid antagonists derived from pipecolic acid.
University of Paris
Triazolo-Peptidomimetics: Novel Radiolabeled Minigastrin Analogs for Improved Tumor Targeting.
Eth Zurich
Novel nonpeptide CCK-B antagonists: design and development of quinazolinone derivatives as potent, selective, and orally active CCK-B antagonists.
Parke-Davis Pharmaceutical Research
Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]acetamide.
Merck Research Laboratories
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)
5-(Piperidin-2-yl)- and 5-(homopiperidin-2-yl)-1,4-benzodiazepines: high-affinity, basic ligands for the cholecystokinin-B receptor.
Merck Sharp & Dohme Research Laboratories
Minor structural differences in Boc-CCK-4 derivatives dictate affinity and selectivity for CCK-A and CCK-B receptors.
Abbott Laboratories
(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
Synthesis, biological evaluation, and quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for kappa-opioid receptors.
Universitá
Controlled modification of acidity in cholecystokinin B receptor antagonists: N-(1,4-benzodiazepin-3-yl)-N'-[3-(tetrazol-5-ylamino) phenyl]ureas.
Neuroscience Research Centre
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
Second-generation benzodiazepine CCK-B antagonists. Development of subnanomolar analogs with selectivity and water solubility.
Merck Research Laboratories
Synthesis and evaluation of cholecystokinin trimers: a multivalent approach to pancreatic cancer detection and treatment.
Pierre and Marie Curie University
Ac-[3- and 4-alkylthioproline31]-CCK4 analogs: synthesis and implications for the CCK-B receptor-bound conformation.
Washington University
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
Discovery of potent cholecystokinin-2 receptor antagonists: elucidation of key pharmacophore elements by X-ray crystallographic and NMR conformational analysis.
Johnson & Johnson Pharmaceutical Research and Development
Synthesis and solid-phase purification of anthranilic sulfonamides as CCK-2 ligands.
Johnson & Johnson Pharmaceutical Research and Development
Scaffold hopping with molecular field points: identification of a cholecystokinin-2 (CCK2) receptor pharmacophore and its use in the design of a prototypical series of pyrrole- and imidazole-based CCK2 antagonists.
James Black Foundation
Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.
Glaxo Wellcome Medicines Research Centre
2,7-Dioxo-2,3,4,5,6,7-hexahydro-1H-benzo[h][1,4]diazonine as a new template for the design of CCK(2) receptor antagonists.
James Black Foundation
Non-peptide cholecystokinin-B/gastrin receptor antagonists based on bicyclic, heteroaromatic skeletons.
James Black Foundation
Improving the affinity and selectivity of a nonpeptide series of cholecystokinin-B/gastrin receptor antagonists based on the dibenzobicyclo[2.2.2]octane skeleton.
James Black Foundation
A new class of non-peptidic cholecystokinin-B/gastrin receptor antagonists based on dibenzobicyclo[2.2.2]octane.
James Black Foundation
Receptor-Ligand Interaction Measured by Inductively Coupled Plasma Mass Spectrometry and Selenium Labeling.
University of Montpellier
Synthesis and biological activity of partially modified retro-inverso pseudopeptide derivatives of the C-terminal tetrapeptide of gastrin.
TBA
Cholecystokinin antagonists. Synthesis and biological evaluation of 4-substituted 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines.
Merck Sharp & Dohme Research Laboratories
Synthesis of gastrin antagonists, analogues of the C-terminal tetrapeptide of gastrin, by introduction of a beta-homo residue.
Centre De Pharmacologie-Endocrinologie (Montpellier, France)
Synthesis and binding affinities of cyclic and related linear analogues of CCK8 selective for central receptors.
University of Paris
Cholecystokinin-A receptor ligands based on the kappa-opioid agonist tifluadom.
Merck Sharp & Dohme Research Laboratories
Carboxylic acids and tetrazoles as isosteric replacements for sulfate in cholecystokinin analogues.
Roche Research Center
trans-3-n-propyl-L-proline is a highly favorable, conformationally restricted replacement for methionine in the C-terminal tetrapeptide of cholecystokinin. Stereoselective synthesis of 3-allyl- and 3-n-propyl-L-proline derivatives from 4-hydroxy-L-proline.
Abbott Laboratories
Cholecystokinin antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors.
Abbott Laboratories
Boc-CCK-4 derivatives containing side-chain ureas as potent and selective CCK-a receptor agonists.
Abbott Laboratories
Boc-Trp-Orn(Z)-Asp-NH2 and derivatives: a new family of CCK antagonists.
University of Paris
Synthesis and X-ray crystallographic analysis of quinazolinone cholecystokinin/gastrin receptor ligands.
Eli Lilly
Synthesis and biological activity of CCK heptapeptide analogues. Effects of conformational constraints and standard modifications on receptor subtype selectivity, functional activity in vitro, and appetite suppression in vivo.
Abbott Laboratories
N-methylated analogs of Ac[Nle28,31]CCK(26-33): synthesis, activity, and receptor selectivity.
Hadassah-University Hospital
Analogs of CCK incorporating conformationally constrained replacements for Asp32.
Roche Research Center
Analogs of Ac-CCK-7 incorporating dipeptide mimics in place of Met28-Gly29.
Roche Research Center
Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors
Ctxt
8-(piperazin-1-yl)-1,2,3,4-tetrahydro-isoquinoline derivatives
Idorsia Pharmaceuticals
Substituted amino triazoles useful as human chitinase inhibitors
Oncoarendi Therapeutics
Use of pyrazolopyrimidine derivatives for the treatment of PI3K-delta related disorders
Incyte
Glycogen phosphorylase inhibitory effects of 2-oxo-1,2-dihydropyridin-3-yl amide derivatives.
Griffith University
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.
Duquesne University
N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.
Bristol-Myers Squibb
Discovery of potent inhibitors of interleukin-2 inducible T-cell kinase (ITK) through structure-based drug design.
Boehringer Ingelheim Pharmaceuticals
Novel thiol-based TACE inhibitors: rational design, synthesis, and SAR of thiol-containing aryl sulfonamides.
Vertex Pharmaceuticals
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors.
Sunesis Pharmaceuticals
Discovery of novel nitrobenzothiazole inhibitors for Mycobacterium tuberculosis ATP phosphoribosyl transferase (HisG) through virtual screening.
Yale University