Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists.
暂无分享,去创建一个
[1] R. Seifert,et al. Dimeric carbamoylguanidine-type histamine H2 receptor ligands: A new class of potent and selective agonists. , 2015, Bioorganic & medicinal chemistry.
[2] H. Haas,et al. International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors , 2015, Pharmacological Reviews.
[3] Jennifer D. Venable,et al. Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators. , 2015, Journal of medicinal chemistry.
[4] A. Strasser,et al. Molecular determinants for the high constitutive activity of the human histamine H4 receptor: functional studies on orthologues and mutants , 2015, British journal of pharmacology.
[5] R. Seifert,et al. No Evidence for Histamine H4 Receptor in Human Monocytes , 2014, The Journal of Pharmacology and Experimental Therapeutics.
[6] R. Seifert,et al. Histamine H4-receptor expression in the brain? , 2014, Naunyn-Schmiedeberg's Archives of Pharmacology.
[7] R. Kiss,et al. Novel histamine H4 receptor ligands and their potential therapeutic applications: an update , 2014, Expert opinion on therapeutic patents.
[8] H. Stark,et al. A search for functional histamine H4 receptors in the human, guinea pig and mouse brain , 2014, Naunyn-Schmiedeberg's Archives of Pharmacology.
[9] Hans-Joachim Wittmann,et al. Sodium binding to hH3R and hH4R — a molecular modeling study , 2014, Journal of Molecular Modeling.
[10] Bin Chen,et al. The Histamine H4 Receptor Antagonist, JNJ 39758979, Is Effective in Reducing Histamine-Induced Pruritus in a Randomized Clinical Study in Healthy Subjects , 2014, The Journal of Pharmacology and Experimental Therapeutics.
[11] R. Thurmond,et al. Clinical and Preclinical Characterization of the Histamine H4 Receptor Antagonist JNJ-39758979 , 2014, The Journal of Pharmacology and Experimental Therapeutics.
[12] A. Buschauer,et al. Synthesis and Functional Characterization of Imbutamine Analogs as Histamine H3 and H4 Receptor Ligands , 2014, Archiv der Pharmazie.
[13] R. Thurmond,et al. The histamine H4 receptor mediates inflammation and Th17 responses in preclinical models of arthritis , 2013, Annals of the rheumatic diseases.
[14] H. Stark,et al. Luciferase Reporter Gene Assay on Human, Murine and Rat Histamine H4 Receptor Orthologs: Correlations and Discrepancies between Distal and Proximal Readouts , 2013, PloS one.
[15] Hans-Joachim Wittmann,et al. Molecular modeling studies give hint for the existence of a symmetric hβ2R-Gαβγ-homodimer , 2013, Journal of Molecular Modeling.
[16] R. Seifert,et al. Incomplete activation of human eosinophils via the histamine H4-receptor: evidence for ligand-specific receptor conformations. , 2012, Biochemical pharmacology.
[17] R. Stevens,et al. Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions , 2012, Science.
[18] A. Buschauer,et al. Synthesis and Histamine H3 and H4 Receptor Activity of Conformationally Restricted Cyanoguanidines Related to UR‐PI376 , 2011, Archiv der Pharmazie.
[19] C. Marson. Targeting the histamine H4 receptor. , 2011, Chemical reviews.
[20] S. Rasmussen,et al. Crystal Structure of the β2Adrenergic Receptor-Gs protein complex , 2011, Nature.
[21] Ruben Abagyan,et al. Structure of the human histamine H1 receptor complex with doxepin , 2011, Nature.
[22] A. Strasser,et al. Paradoxical Stimulatory Effects of the “Standard” Histamine H4-Receptor Antagonist JNJ7777120: the H4 Receptor Joins the Club of 7 Transmembrane Domain Receptors Exhibiting Functional Selectivity , 2011, Molecular Pharmacology.
[23] R. Seifert,et al. Expression and functional properties of canine, rat, and murine histamine H4 receptors in Sf9 insect cells , 2011, Naunyn-Schmiedeberg's Archives of Pharmacology.
[24] Patrick Igel,et al. Histamine H4 receptor agonists. , 2010, Bioorganic & medicinal chemistry letters.
[25] R. Seifert,et al. Chiral NG-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity. , 2010, Bioorganic & medicinal chemistry letters.
[26] Wen Jiang,et al. Molecular Determinants of Ligand Binding to H4R Species Variants , 2010, Molecular Pharmacology.
[27] R. Thurmond,et al. The histamine H4 receptor mediates inflammation and pruritus in Th2-dependent dermal inflammation. , 2010, The Journal of investigative dermatology.
[28] R. Seifert,et al. Does the Histamine H4 Receptor Have a Pro- or Anti-Inflammatory Role in Murine Bronchial Asthma? , 2010, Pharmacology.
[29] R. Seifert,et al. No Evidence for Functional Selectivity of Proxyfan at the Human Histamine H3 Receptor Coupled to Defined Gi/Go Protein Heterotrimers , 2010, Journal of Pharmacology and Experimental Therapeutics.
[30] A. Strasser,et al. Synthesis and Structure−Activity Relationships of Cyanoguanidine-Type and Structurally Related Histamine H4 Receptor Agonists§ , 2009 .
[31] R. Smits,et al. Major advances in the development of histamine H4 receptor ligands. , 2009, Drug discovery today.
[32] Krzysztof Palczewski,et al. Conserved waters mediate structural and functional activation of family A (rhodopsin-like) G protein-coupled receptors , 2009, Proceedings of the National Academy of Sciences.
[33] R. Seifert,et al. N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent. , 2009, Journal of medicinal chemistry.
[34] Roland Seifert,et al. High constitutive activity and a G-protein-independent high-affinity state of the human histamine H(4)-receptor. , 2009, Biochemistry.
[35] R. Seifert,et al. Tritium‐Labeled N1‐[3‐(1H‐imidazol‐4‐yl)propyl]‐N2‐propionylguanidine ([3H]UR‐PI294), a High‐Affinity Histamine H3 and H4 Receptor Radioligand , 2009, ChemMedChem.
[36] R. Seifert,et al. Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists. , 2008, Journal of medicinal chemistry.
[37] R. Smits,et al. Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist. , 2006, Journal of medicinal chemistry.
[38] Jennifer D. Venable,et al. The histamine H4 receptor in autoimmune disease , 2006, Expert opinion on investigational drugs.
[39] S. Shuto,et al. Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure. , 2006, Journal of medicinal chemistry.
[40] R. Smits,et al. The emerging role of the histamine H4 receptor in anti-inflammatory therapy. , 2006, Current topics in medicinal chemistry.
[41] R. Seifert,et al. Probing Ligand-Specific Histamine H1- and H2-Receptor Conformations with NG-Acylated Imidazolylpropylguanidines , 2006, Journal of Pharmacology and Experimental Therapeutics.
[42] R. Thurmond,et al. The histamine H4 receptor as a new therapeutic target for inflammation. , 2005, Trends in pharmacological sciences.
[43] Rob Leurs,et al. Evaluation of Histamine H1-, H2-, and H3-Receptor Ligands at the Human Histamine H4 Receptor: Identification of 4-Methylhistamine as the First Potent and Selective H4 Receptor Agonist , 2005, Journal of Pharmacology and Experimental Therapeutics.
[44] J. Mieloszynski,et al. Ruthenium catalysed oxidation without CCl4 of oleic acid, other monoenic fatty acids and alkenes , 2005 .
[45] A. W. Schüttelkopf,et al. PRODRG: a tool for high-throughput crystallography of protein-ligand complexes. , 2004, Acta crystallographica. Section D, Biological crystallography.
[46] J. A. Jablonowski,et al. The first potent and selective non-imidazole human histamine H4 receptor antagonists. , 2003, Journal of medicinal chemistry.
[47] T. Bürckstümmer,et al. Multiple Differences in Agonist and Antagonist Pharmacology between Human and Guinea Pig Histamine H1-Receptor , 2003, Journal of Pharmacology and Experimental Therapeutics.
[48] Rob Leurs,et al. A selective human H(4)-receptor agonist: (-)-2-cyano-1-methyl-3-[(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-y] methylguanidine. , 2003, Journal of medicinal chemistry.
[49] T. Bürckstümmer,et al. The human histamine H2‐receptor couples more efficiently to Sf9 insect cell Gs‐proteins than to insect cell Gq‐proteins: limitations of Sf9 cells for the analysis of receptor/Gq‐protein coupling , 2002, Journal of neurochemistry.
[50] J. Schwartz,et al. Histamine H3‐receptor‐mediated [35S]GTPγ[S] binding: evidence for constitutive activity of the recombinant and native rat and human H3 receptors , 2002, British journal of pharmacology.
[51] T. Bürckstümmer,et al. Distinct interaction of human and guinea pig histamine H2-receptor with guanidine-type agonists. , 2001, Molecular pharmacology.
[52] R. Seifert,et al. Similar apparent constitutive activity of human histamine H(2)-receptor fused to long and short splice variants of G(salpha). , 2001, The Journal of pharmacology and experimental therapeutics.
[53] T. Lovenberg,et al. Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation. , 2001, The Journal of pharmacology and experimental therapeutics.
[54] J. Boutin,et al. Structure and expression of the human histamine H4-receptor gene. , 2001, Biochemical and biophysical research communications.
[55] B. Kobilka,et al. Functional differences between full and partial agonists: evidence for ligand-specific receptor conformations. , 2001, The Journal of pharmacology and experimental therapeutics.
[56] V. Setola,et al. Discovery of a novel member of the histamine receptor family. , 2001, Molecular pharmacology.
[57] L B Hough,et al. Genomics meets histamine receptors: new subtypes, new receptors. , 2001, Molecular pharmacology.
[58] Nicholas J. Carruthers,et al. Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. , 2001, Molecular pharmacology.
[59] C. M. Davenport,et al. Cloning, expression, and pharmacological characterization of a novel human histamine receptor. , 2001, Molecular pharmacology.
[60] F. Monsma,et al. Cloning and characterization of a novel human histamine receptor. , 2001, The Journal of pharmacology and experimental therapeutics.
[61] K. Tanaka,et al. Molecular cloning and characterization of a new human histamine receptor, HH4R. , 2000, Biochemical and biophysical research communications.
[62] Y. Masuho,et al. Molecular Cloning and Characterization of a Novel Type of Histamine Receptor Preferentially Expressed in Leukocytes* , 2000, The Journal of Biological Chemistry.
[63] A. Yamatodani,et al. Synthesis of 4(5)-[5-(Aminomethyl)tetrahydrofuran-2-yl- or 5-(Aminomethyl)-2,5-dihydrofuran-2-yl]imidazoles by Efficient Use of a PhSe Group: Application to Novel Histamine H3-Ligands1 , 1999 .
[64] A. Yamatodani,et al. Synthesis of imifuramine and its stereoisomers exhibiting histamine H3-agonistic activity , 1999 .
[65] S. Sprang,et al. The structure of the G protein heterotrimer Giα1 β 1 γ 2 , 1995, Cell.
[66] J. Lange,et al. Two novel syntheses of the histamine H3 antagonist thioperamide , 1995 .
[67] K. Jakobs,et al. Muscarinic acetylcholine receptor-stimulated binding of guanosine 5'-O-(3-thiotriphosphate) to guanine-nucleotide-binding proteins in cardiac membranes. , 1989, European journal of biochemistry.
[68] D. Davey,et al. Convenient synthesis of 4-methylhistamine and racemic .alpha.,4-dimethylhistamine and .alpha.,4-dimethylhistidine , 1989 .
[69] R. S. Hinks,et al. Enzymes in organic synthesis. 33. Stereoselective pig liver esterase-catalyzed hydrolyses of meso cyclopentyl-, tetrahydrofuranyl-, and tetrahydrothiophenyl-1,3-diesters , 1985 .
[70] C. W. Scott,et al. Reconstitution of catecholamine-stimulated binding of guanosine 5'-O-(3-thiotriphosphate) to the stimulatory GTP-binding protein of adenylate cyclase. , 1984, Biochemistry.
[71] R. Webb,et al. Diphenyl cyanocarbonimidate. A versatile synthon for the construction of heterocyclic systems , 1982 .
[72] T. Walseth,et al. The enzymatic preparation of [α-32P]nucleoside triphosphates, cyclic [32P]AMP, and cyclic [32P]GMP☆ , 1979 .
[73] Y. Cheng,et al. Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. , 1973, Biochemical pharmacology.
[74] C. Pak,et al. Selective reductions. XIX. Rapid reaction of carboxylic acids with borane-tetrahydrofuran. Remarkably convenient procedure for the selective conversion of carboxylic acids to the corresponding alcohols in the presence of other functional groups , 1973 .
[75] O. Mitsunobu,et al. Preparation of Esters of Phosphoric Acid by the Reaction of Trivalent Phosphorus Compounds with Diethyl Azodicarboxylate in the Presence of Alcohols , 1967 .
[76] C. Pontes,et al. Is the H4 receptor a new drug target for allergies and asthma? , 2013, Frontiers in bioscience.
[77] Hans-Joachim Wittmann,et al. Species-dependent activities of G-protein-coupled receptor ligands: lessons from histamine receptor orthologs. , 2013, Trends in pharmacological sciences.
[78] P. Bonaventure,et al. The future antihistamines: histamine H3 and H4 receptor ligands. , 2010, Advances in experimental medicine and biology.
[79] Erwin W. Gelfand,et al. The role of histamine H1 and H4 receptors in allergic inflammation: the search for new antihistamines , 2008, Nature Reviews Drug Discovery.
[80] G. Büchi,et al. A two-step synthesis of imidazoles from aldehydes via 4-tosyloxazolines , 1994 .
[81] R. Chěnevert,et al. Chemoenzymatic enantioselective synthesis of amidinomycin , 1994 .
[82] R. Chěnevert,et al. Enantioselective synthesis of (+) and (-)-cis-3-aminocyclo-pentanecarboxylic acids by enzymatic asymmetrization , 1992 .
[83] W. Szarek,et al. Synthesis of cyclopentane analogs of 1-(2′,3′-dideoxy-β-glycero-pentofuranosyl)pyrimidine nucleosides , 1988 .
[84] D. Eggleston,et al. Diphenyl cyancarbonimidate and dichlorodiphenoxymethane as synthons for the construction of heterocyclic systems of medicinal interest , 1987 .
[85] D. Swern,et al. Oxidation of alcohols by “activated” dimethyl sulfoxide. a preparative, steric and mechanistic study , 1978 .
[86] S. Birch,et al. 502. The configurations of the isomeric forms of 1: 3-dimethylcyclopentane , 1953 .
[87] R. Thurmond,et al. Dovepress Open Access to Scientific and Medical Research Open Access Full Text Article Pharmacological Characterization of Oxime Agonists of the Histamine H 4 Receptor , 2022 .