182 articles for KA Jacobson
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT
National Institute of Diabetes and Digestive and Kidney Diseases
Purine (N)-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A3 Adenosine Receptor Agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
Rigidified A3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy.
National Institute of Diabetes and Digestive and Kidney Diseases
Molecular modeling of the human P2Y14 receptor: A template for structure-based design of selective agonist ligands.
National Institute of Diabetes and Digestive and Kidney Diseases
In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
Extended N(6) substitution of rigid C2-arylethynyl nucleosides for exploring the role of extracellular loops in ligand recognition at the A3 adenosine receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and evaluation of N6-substituted apioadenosines as potential adenosine A3 receptor modulators.
Ghent University
Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
4-Alkyloxyimino derivatives of uridine-5'-triphosphate: distal modification of potent agonists as a strategy for molecular probes of P2Y2, P2Y4, and P2Y6 receptors.
National Institute of Diabetes and Digestive and Kidney Diseases
Flavonoid derivatives as adenosine receptor antagonists: a comparison of the hypothetical receptor binding site based on a comparative molecular field analysis model.
National Institute of Diabetes
Fluorescent ligands for adenosine receptors.
National Institute of Diabetes and Digestive and Kidney Diseases
Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-based approaches to ligands for G-protein-coupled adenosine and P2Y receptors, from small molecules to nanoconjugates.
National Institute of Diabetes and Digestive and Kidney Diseases
Truncated Nucleosides as A(3) Adenosine Receptor Ligands: Combined 2-Arylethynyl and Bicyclohexane Substitutions.
TBA
Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-activity relationships and molecular modeling of 1,2,4-triazoles as adenosine receptor antagonists.
TBA
Virtual screening leads to the discovery of novel non-nucleotide P2Y1 receptor antagonists.
National Institutes of Health
Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions.
National Institute of Diabetes and Digestive and Kidney Diseases
Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element.
TBA
Discovery of New Human A(2A) Adenosine Receptor Agonists: Design, Synthesis, and Binding Mode of Truncated 2-Hexynyl-4'-thioadenosine.
Ewha Womans University
Human P2Y(14) receptor agonists: truncation of the hexose moiety of uridine-5'-diphosphoglucose and its replacement with alkyl and aryl groups.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists.
Niddk
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
Probing distal regions of the A2B adenosine receptor by quantitative structure-activity relationship modeling of known and novel agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists.
Ewha Womans University
Molecular dynamics simulation of the P2Y14 receptor. Ligand docking and identification of a putative binding site of the distal hexose moiety.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
Molecular modeling of the human P2Y2 receptor and design of a selective agonist, 2'-amino-2'-deoxy-2-thiouridine 5'-triphosphate.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-activity relationships of uridine 5'-diphosphate analogues at the human P2Y6 receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
National Institute of Diabetes and Digestive and Kidney Diseases
Design and synthesis of 3'-ureidoadenosine-5'-uronamides: effects of the 3'-ureido group on binding to the A3 adenosine receptor.
Ewha Womans University
Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists.
Niddk
N6-substituted D-4'-thioadenosine-5'-methyluronamides: potent and selective agonists at the human A3 adenosine receptor.
Ewha Womans University
A conformationally locked analogue of the anti-HIV agent stavudine. An important correlation between pseudorotation and maximum amplitude.
National Cancer Institute-Frederick
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.
National Institute of Diabetes and Digestive and Kidney Diseases
Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.
University of Bonn
Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists.
National Institute of Diabetes
Methanocarba modification of uracil and adenine nucleotides: high potency of Northern ring conformation at P2Y1, P2Y2, P2Y4, and P2Y11 but not P2Y6 receptors.
National Institute of Diabetes
Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y(1) receptor ligands.
National Institute of Diabetes
Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.
National Institute of Diabetes
Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y1 receptor antagonists and partial agonists.
National Institute of Diabetes
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.
National Institute of Diabetes
Deoxyadenosine bisphosphate derivatives as potent antagonists at P2Y1 receptors.
National Institute of Diabetes
Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
National Institute of Diabetes
Synthesis and biological activity of a new series of N6-arylcarbamoyl, 2-(Ar)alkynyl-N6-arylcarbamoyl, and N6-carboxamido derivatives of adenosine-5'-N-ethyluronamide as A1 and A3 adenosine receptor agonists.
University of Ferrara
Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.
Niddk
Novel N6-(substituted-phenylcarbamoyl)adenosine-5'-uronamides as potent agonists for A3 adenosine receptors.
University of Ferrara
6-phenyl-1,4-dihydropyridine derivatives as potent and selective A3 adenosine receptor antagonists.
National Institute of Diabetes
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
National Institute of Diabetes
Search for new purine- and ribose-modified adenosine analogues as selective agonists and antagonists at adenosine receptors.
National Institute of Diabetes
Structure-activity relationships of 9-alkyladenine and ribose-modified adenosine derivatives at rat A3 adenosine receptors.
National Institute of Diabetes
Selective ligands for rat A3 adenosine receptors: structure-activity relationships of 1,3-dialkylxanthine 7-riboside derivatives.
National Institute of Diabetes
2-Substitution of N6-benzyladenosine-5'-uronamides enhances selectivity for A3 adenosine receptors.
National Institute of Diabetes
Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.
Niddk
Synthesis and biological activity of N6-(p-sulfophenyl)alkyl and N6-sulfoalkyl derivatives of adenosine: water-soluble and peripherally selective adenosine agonists.
National Institute of Diabetes
Functionalized congener approach for the design of novel muscarinic agents. Synthesis and pharmacological evaluation of N-methyl-N-[4-(1-pyrrolidinyl)-2-butynyl] amides.
Niddk
Sulfur-containing 1,3-dialkylxanthine derivatives as selective antagonists at A1-adenosine receptors.
Niddk
Electrophilic derivatives of purines as irreversible inhibitors of A1 adenosine receptors.
Niddk
Binary drugs: conjugates of purines and a peptide that bind to both adenosine and substance P receptors.
TBA
Functionalized congeners of adenosine: preparation of analogues with high affinity for A1-adenosine receptors.
TBA
Design, synthesis and binding affinity of 3'-fluoro analogues of Cl-IB-MECA as adenosine A3 receptor ligands.
Seoul National University
Ring-Constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5'-uronamide and 2'-deoxy modifications.
Niddk
New base-altered adenosine analogues: Synthesis and affinity at adenosine A1 and A2A receptors
TBA
Synthesis and P2Y2 receptor agonist activities of uridine 5'-phosphonate analogues.
Ghent University
Evaluation of molecular modeling of agonist binding in light of the crystallographic structure of an agonist-bound A2A adenosine receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-activity relationships of truncated C2- or C8-substituted adenosine derivatives as dual acting A2A and A3 adenosine receptor ligands.
Ewha Womans University
Synthesis and Biological Evaluation of a New Series of 1,2,4-Triazolo[1,5-a]-1,3,5-triazines as Human A(2A) Adenosine Receptor Antagonists with Improved Water Solubility.
Universita Di Trieste
Pyrimidine nucleotides with 4-alkyloxyimino and terminal tetraphosphated-ester modifications as selective agonists of the P2Y(4) receptor.
Niddk
Molecular probes for the A2A adenosine receptor based on a pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine scaffold.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists.
Niddk
Design, synthesis, and binding of homologated truncated 4'-thioadenosine derivatives at the human A3 adenosine receptors.
Ewha Womans University
Pyrimidine ribonucleotides with enhanced selectivity as P2Y(6) receptor agonists: novel 4-alkyloxyimino, (S)-methanocarba, and 5'-triphosphate gamma-ester modifications.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and pharmacological characterization of a new series of 5,7-disubstituted-[1,2,4]triazolo[1,5-a][1,3,5]triazine derivatives as adenosine receptor antagonists: A preliminary inspection of ligand-receptor recognition process.
National University of Singapore
2-Dialkynyl derivatives of (N)-methanocarba nucleosides: 'Clickable' A(3) adenosine receptor-selective agonists.
Niddk
Structure-activity relationship of (N)-Methanocarba phosphonate analogues of 5'-AMP as cardioprotective agents acting through a cardiac P2X receptor.
National Institutes of Diabetes and Digestive and Kidney Diseases
Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists.
Ewha Womans University
Molecular recognition in the P2Y(14) receptor: Probing the structurally permissive terminal sugar moiety of uridine-5'-diphosphoglucose.
National Institute of Diabetes and Digestive and Kidney Diseases
Functionalized congeners of A3 adenosine receptor-selective nucleosides containing a bicyclo[3.1.0]hexane ring system.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists.
Ewha Womans University
Synthesis and P2Y receptor activity of nucleoside 5'-phosphonate derivatives.
Ghent University
Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.
Ewha Womans University
Structure-activity relationships of 1,4-dihydropyridines that act as enhancers of the vanilloid receptor 1 (TRPV1).
National Institute of Diabetes and Digestive and Kidney Diseases
Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure activity relationships of 5-HT2B and 5-HT2C serotonin receptor antagonists: N6, C2 and 5'-Modified (N)-methanocarba-adenosine derivatives.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Activity Relationship of Truncated 4'-Selenonucleosides: A3 Adenosine Receptor Activity and Binding Selectivity.
Seoul National University
Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor.
Institute of Science and Technology
Lipid Trolling to Optimize A3 Adenosine Receptor-Positive Allosteric Modulators (PAMs).
National Institute of Diabetes and Digestive and Kidney Diseases
Structural Modification and Biological Evaluation of 2,8-Disubstituted Adenine and Its Nucleosides as A2A Adenosine Receptor Antagonists: Exploring the Roles of Ribose at Adenosine Receptors.
Seoul National University
2-Amino-5-arylethynyl-thiophen-3-yl-(phenyl)methanones as A
National Institute of Diabetes and Digestive and Kidney Disease
P2Y1 antagonists: combining receptor-based modeling and QSAR for a quantitative prediction of the biological activity based on consensus scoring.
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4'-thioadenosine derivatives without 4'-hydroxymethyl group as highly potent and selective antagonists.
Ewha Womans University
Structure-Activity Relationship of Truncated 2,8-Disubstituted-Adenosine Derivatives as Dual A
Seoul National University
Structure-activity relationship of uridine 5'-diphosphoglucose analogues as agonists of the human P2Y14 receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
Alicyclic Ring Size Variation of 4-Phenyl-2-naphthoic Acid Derivatives as P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists.
Ghent University
Expanding the repertoire of methanocarba nucleosides from purinergic signaling to diverse targets.
National Institute of Diabetes & Digestive & Kidney Diseases
Synthesis and pharmacological characterization of multiply substituted 2H-chromene derivatives as P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.
Leiden University
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as highly potent and selective agonists at the human A3 adenosine receptor.
Ewha Womans University
Human P2Y(6) receptor: molecular modeling leads to the rational design of a novel agonist based on a unique conformational preference.
Niddk
Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprotection.
National Institute of Diabetes and Digestive and Kidney Diseases
Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5'-ribofuran-uronamide moiety.
National Institute of Diabetes and Digestive and Kidney Diseases
"Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists.
National Institute of Diabetes and Digestive and Kidney Diseases
GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A
University of Southern California
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Activity Relationship and Neuroprotective Activity of 1,5-Dihydro-2
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Activity Studies of 1
National Institute of Diabetes and Digestive and Kidney Diseases
Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Activity Relationship of 3-Methylcytidine-5'-α,β-methylenediphosphates as CD73 Inhibitors.
National Institute of Diabetes and Digestive and Kidney Diseases
Subtle Chemical Changes Cross the Boundary between Agonist and Antagonist: New A
Ewha Womans University
Structure-activity relationships of pyrimidine nucleotides containing a 5'-α,β-methylene diphosphonate at the P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists.
Niddk
Structure activity relationship of 3-nitro-2-(trifluoromethyl)-2H-chromene derivatives as P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Activity Relationship of Heterocyclic P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Direct Comparison of (N)-Methanocarba and Ribose-Containing 2-Arylalkynyladenosine Derivatives as A
National Institute of Diabetes and Digestive and Kidney Disease
Novel cyanothiouracil and cyanothiocytosine derivatives as concentration-dependent selective inhibitors of U87MG glioblastomas: Adenosine receptor binding and potent PDE4 inhibition.
Istanbul Medipol University
Synthesis, biological properties, and molecular modeling investigation of the first potent, selective, and water-soluble human A(3) adenosine receptor antagonist.
TBA
Discovery and Structure-Activity Relationships of Novel Template, Truncated 1'-Homologated Adenosine Derivatives as Pure Dual PPARγ/δ Modulators.
Seoul National University
Structure activity relationship of novel antiviral nucleosides against Enterovirus A71.
National Institute of Diabetes and Digestive and Kidney Disease
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.
National Institute of Diabetes & Digestive & Kidney Diseases
Biological Evaluation of 5'-(
National Institute of Diabetes and Digestive and Kidney Diseases
Identification of a New Heterocyclic Scaffold for Inhibitors of the Polo-Box Domain of Polo-like Kinase 1.
National Cancer Institute
Acyclic and cyclopropyl analogues of adenosine bisphosphate antagonists of the P2Y1 receptor: structure-activity relationships and receptor docking.
National Institute of Diabetes
Synthesis and purine receptor affinity of 6-oxopurine nucleosides and nucleotides containing (N)-methanocarba-pseudoribose rings.
Niddk
Fluorosulfonyl- and bis-(beta-chloroethyl)amino-phenylamino functionalized pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives: irreversible antagonists at the human A3 adenosine receptor and molecular modeling studies.
Università
Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptors.
National Institute of Diabetes and Digestive and Kidney Diseases
Exploration of Alternative Scaffolds for P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
South (S)- and North (N)-Methanocarba-7-Deazaadenosine Analogues as Inhibitors of Human Adenosine Kinase.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Based Design of 3-(4-Aryl-1H-1,2,3-triazol-1-yl)-Biphenyl Derivatives as P2Y14 Receptor Antagonists.
National Institute of Diabetes and Digestive and Kidney Diseases
Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.
National Institute of Diabetes
The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family.
Chembridge
Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A
Medical College of Wisconsin
Selective A(3) adenosine receptor antagonists: water-soluble 3, 5-diacyl-1,2,4-trialkylpyridinium salts and their oxidative generation from dihydropyridine precursors.
National Institute of Diabetes
Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists.
National Institute of Diabetes
Structure-Activity Relationship of Purine and Pyrimidine Nucleotides as Ecto-5'-Nucleotidase (CD73) Inhibitors.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis, CoMFA analysis, and receptor docking of 3,5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
National Institute of Diabetes
Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.
National Institute of Diabetes
A pyridoxine cyclic phosphate and its 6-azoaryl derivative selectively potentiate and antagonize activation of P2X1 receptors.
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists.
National Institute of Diabetes
Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.
National Institute of Diabetes
Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
National Institute of Diabetes
Structure-Based Design, Synthesis by Click Chemistry and
National Institute of Diabetes and Digestive and Kidney Diseases
Interactions of flavonoids and other phytochemicals with adenosine receptors.
National Institute of Diabetes
Tetrahydrobenzothiophenone derivatives as a novel class of adenosine receptor antagonists.
National Institute of Diabetes
Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists.
National Institute of Diabetes
Effect of trifluoromethyl and other substituents on activity of xanthines at adenosine receptors.
National Institutes of Health
4-Alkyloxyimino-cytosine nucleotides: tethering approaches to molecular probes for the P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and anti-renal fibrosis activity of conformationally locked truncated 2-hexynyl-N(6)-substituted-(N)-methanocarba-nucleosides as A3 adenosine receptor antagonists and partial agonists.
Seoul National University
Structure-activity relationships of 1,3-dialkylxanthine derivatives at rat A3 adenosine receptors.
National Institute of Diabetes
Distinct structural changes in a G protein-coupled receptor caused by different classes of agonist ligands.
Niddk
Functionalized congeners of 1,3-dialkylxanthines: preparation of analogues with high affinity for adenosine receptors.
TBA
Structure-Guided Modification of Heterocyclic Antagonists of the P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Functionalized congener approach to muscarinic antagonists: analogues of pirenzepine.
Niddk
Selective histone deactylase 6 inhibitors
H. Lee Moffitt Cancer Center and Research Institute
Altered enthalpy-entropy compensation in picomolar transition state analogues of human purine nucleoside phosphorylase.
Albert Einstein College of Medicine
Neoflavonoids and Tetrahydroquinolones as Possible Cancer Chemopreventive Agents.
Central Institute of Medicinal and Aromatic Plants
Inhibitory effect of the 4-aminotetrahydroquinoline derivatives, selective chemoattractant receptor-homologous molecule expressed on T helper 2 cell antagonists, on eosinophil migration induced by prostaglandin D2.
Kyowa Hakko Kogyo
Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences.
Eli Lilly
Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist.
Pfizer