메뉴 건너뛰기




Volumn 55, Issue 5, 2012, Pages 2367-2375

Synthesis and characterization of novel 2-amino-3-benzoylthiophene derivatives as biased allosteric agonists and modulators of the adenosine A 1 receptor

Author keywords

[No Author keywords available]

Indexed keywords

2 AMINO 3 BENZOYLTHIOPHENE; 2 AMINO 5 METHYL 4 3 TRIFLUOROMETHYL PHENYL THIOPHEN 3 YL 4 CHLOROPHENYL METHANONE; 2 AMINO 5 METHYL 4 3 TRIFLUOROMETHYL PHENYL THIOPHEN 3 YL PHENYL METHANONE; 2 BENZOYLTHIOPHENE DERIVATIVE; ADENOSINE A1 RECEPTOR; BENZENE DERIVATIVE; BENZOYL PEROXIDE; MITOGEN ACTIVATED PROTEIN KINASE 1; SCAFFOLD PROTEIN; UNCLASSIFIED DRUG;

EID: 84863416234     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm201600e     Document Type: Article
Times cited : (52)

References (33)
  • 1
    • 42149181885 scopus 로고    scopus 로고
    • Structural diversity of G protein-coupled receptors and significance for drug discovery
    • Lagerström, M. C.; Schiöth, H. B. Structural diversity of G protein-coupled receptors and significance for drug discovery Nature Rev. Drug Discovery 2008, 7, 339-357
    • (2008) Nature Rev. Drug Discovery , vol.7 , pp. 339-357
    • Lagerström, M.C.1    Schiöth, H.B.2
  • 2
    • 0036258990 scopus 로고    scopus 로고
    • G Protein-receptor coupling allosterism and complexing
    • Christopoulos, A.; Kenakin, T. G Protein-receptor coupling allosterism and complexing Pharmacol. Rev. 2002, 54, 323-374
    • (2002) Pharmacol. Rev. , vol.54 , pp. 323-374
    • Christopoulos, A.1    Kenakin, T.2
  • 3
    • 0036490942 scopus 로고    scopus 로고
    • Allosteric binding sites on cell-surface receptors: Novel targets for drug discovery
    • Christopoulos, A. Allosteric binding sites on cell-surface receptors: novel targets for drug discovery Nature Rev. Drug Discovery 2002, 1, 198-210
    • (2002) Nature Rev. Drug Discovery , vol.1 , pp. 198-210
    • Christopoulos, A.1
  • 5
    • 58149193205 scopus 로고    scopus 로고
    • Allosteric modulation of GPCRs: A novel approach for the treatment of CNS disorders
    • Conn, J. P.; Christopoulos, A.; Lindsley, C. W. Allosteric modulation of GPCRs: a novel approach for the treatment of CNS disorders Nature Rev. Drug Discovery 2009, 8, 41-54
    • (2009) Nature Rev. Drug Discovery , vol.8 , pp. 41-54
    • Conn, J.P.1    Christopoulos, A.2    Lindsley, C.W.3
  • 6
    • 0025603686 scopus 로고
    • 1 receptor binding and function by 2-amino-3-benzoylthiophenes
    • 1 receptor binding and function by 2-amino-3-benzoylthiophenes Mol. Pharmacol. 1990, 38, 939-949
    • (1990) Mol. Pharmacol. , vol.38 , pp. 939-949
    • Bruns, R.F.1    Fergus, J.H.2
  • 7
    • 0025638880 scopus 로고
    • Structure-activity relationships for enhancement of adenosine A1 receptor binding by 2-amino-3-benzoylthiophenes
    • Bruns, R. F.; Fergus, J. H.; Coughenour, L. L.; Courtland, G. G.; Pugsley, T. A.; Dodd, J. H.; Tinney, F. J. Structure-activity relationships for enhancement of adenosine A1 receptor binding by 2-amino-3-benzoylthiophenes Mol. Pharmacol. 1990, 38, 950-958
    • (1990) Mol. Pharmacol. , vol.38 , pp. 950-958
    • Bruns, R.F.1    Fergus, J.H.2    Coughenour, L.L.3    Courtland, G.G.4    Pugsley, T.A.5    Dodd, J.H.6    Tinney, F.J.7
  • 8
    • 0033539111 scopus 로고    scopus 로고
    • 1 Receptor. Synthesis and Biological Evaluation of Novel 2-Amino-3-benzoylthiophenes as Allosteric Enhancers of Agonist Binding
    • 1 Receptor. Synthesis and Biological Evaluation of Novel 2-Amino-3-benzoylthiophenes as Allosteric Enhancers of Agonist Binding J. Med. Chem. 1999, 42, 3629-3635
    • (1999) J. Med. Chem. , vol.42 , pp. 3629-3635
    • Van Der Klein, P.A.M.1    Kourounakis, A.P.2    Ijzerman, A.P.3
  • 10
    • 0346996805 scopus 로고    scopus 로고
    • 1 adenosine receptors increase receptor-G protein coupling and counteract guanine nucleotide effects on agonist binding
    • 1 adenosine receptors increase receptor-G protein coupling and counteract guanine nucleotide effects on agonist binding Mol. Pharmacol. 2003, 64, 1557-1564
    • (2003) Mol. Pharmacol. , vol.64 , pp. 1557-1564
    • Figler, H.1    Olsson, R.A.2    Linden, J.3
  • 13
    • 38849185360 scopus 로고    scopus 로고
    • 5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers
    • Aurelio, L.; Figler, H.; Flynn, B. L.; Linden, J.; Scammells, P. J. 5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers Bioorg. Med. Chem. 2008, 16, 1319-1327
    • (2008) Bioorg. Med. Chem. , vol.16 , pp. 1319-1327
    • Aurelio, L.1    Figler, H.2    Flynn, B.L.3    Linden, J.4    Scammells, P.J.5
  • 19
    • 79960502280 scopus 로고    scopus 로고
    • Ligand functional selectivity and quantitative pharmacology at G protein-coupled receptors
    • Stallaert, W.; Christopoulos, A.; Bouvier, M. Ligand functional selectivity and quantitative pharmacology at G protein-coupled receptors Expert Opin. Drug Discovery 2011, 6, 811-825
    • (2011) Expert Opin. Drug Discovery , vol.6 , pp. 811-825
    • Stallaert, W.1    Christopoulos, A.2    Bouvier, M.3
  • 23
    • 77951223981 scopus 로고    scopus 로고
    • Identification of Orthosteric and Allosteric Site Mutations in M2 Muscarinic Acetylcholine Receptors That Contribute to Ligand-Selective Signaling Bias
    • Gregory, K. J.; Hall, N. E.; Tobin, A. B.; Sexton, P. M.; Christopoulos, A. Identification of Orthosteric and Allosteric Site Mutations in M2 Muscarinic Acetylcholine Receptors That Contribute to Ligand-Selective Signaling Bias J. Biol. Chem. 2010, 285, 7459-7474
    • (2010) J. Biol. Chem. , vol.285 , pp. 7459-7474
    • Gregory, K.J.1    Hall, N.E.2    Tobin, A.B.3    Sexton, P.M.4    Christopoulos, A.5
  • 24
    • 77956249652 scopus 로고    scopus 로고
    • Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: Implications for drug screening
    • Koole, C.; Wootten, D.; Simms, J.; Valant, C.; Sridhar, R.; Woodman, O. L.; Miller, L. J.; Summers, R. J.; Christopoulos, A.; Sexton, P. M. Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: implications for drug screening Mol. Pharmacol. 2010, 78, 465-465
    • (2010) Mol. Pharmacol. , vol.78 , pp. 465-465
    • Koole, C.1    Wootten, D.2    Simms, J.3    Valant, C.4    Sridhar, R.5    Woodman, O.L.6    Miller, L.J.7    Summers, R.J.8    Christopoulos, A.9    Sexton, P.M.10
  • 26
    • 78149496159 scopus 로고    scopus 로고
    • Allosteric modulation of G protein-coupled receptors: A pharmacological perspective
    • Keov, P.; Sexton, P. M.; Christopoulos, A. Allosteric modulation of G protein-coupled receptors: a pharmacological perspective Neuropharmacology 2011, 60, 24-35
    • (2011) Neuropharmacology , vol.60 , pp. 24-35
    • Keov, P.1    Sexton, P.M.2    Christopoulos, A.3
  • 27
    • 84855290525 scopus 로고    scopus 로고
    • A Monod-Wyman-Changeux Mechanism Can Explain G Protein-Coupled Receptor (GPCR) Allosteric Modulation
    • Canals, M.; Lane, J. R.; Wen, A.; Scammells, P. J.; Sexton, P. M.; Christopoulos, A. A Monod-Wyman-Changeux Mechanism Can Explain G Protein-Coupled Receptor (GPCR) Allosteric Modulation J. Biol. Chem. 2012, 287, 650-659
    • (2012) J. Biol. Chem. , vol.287 , pp. 650-659
    • Canals, M.1    Lane, J.R.2    Wen, A.3    Scammells, P.J.4    Sexton, P.M.5    Christopoulos, A.6
  • 28
    • 34447632041 scopus 로고    scopus 로고
    • Allosteric GPCR modulators: Taking advantage of permissive receptor pharmacology
    • Leach, K.; Sexton, P. M.; Christopoulos, A. Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology Trends Pharmacol. Sci. 2007, 28, 382-389
    • (2007) Trends Pharmacol. Sci. , vol.28 , pp. 382-389
    • Leach, K.1    Sexton, P.M.2    Christopoulos, A.3
  • 29
    • 84863408610 scopus 로고    scopus 로고
    • Measurement of ligand-G protein-coupled receptor interactions
    • In; Poyner, D. R. Wheatley, M. Wiley-Blackwell: Oxford, UK
    • Leach, K.; Valant, C.; Sexton, P. M.; Christopoulos, A. Measurement of ligand-G protein-coupled receptor interactions. In G Protein-Coupled Receptors; Poyner, D. R.; Wheatley, M., Eds.; Wiley-Blackwell: Oxford, UK, 2010; pp 1-29.
    • (2010) G Protein-Coupled Receptors , pp. 1-29
    • Leach, K.1    Valant, C.2    Sexton, P.M.3    Christopoulos, A.4
  • 32
    • 33646767009 scopus 로고    scopus 로고
    • ORTEP-3 for windows-a version of ORTEP-III with a graphical user interface (GUI)
    • Farrugia, L. J. ORTEP-3 for windows-a version of ORTEP-III with a graphical user interface (GUI) J. Appl. Crystallogr. 1997, 30, 565
    • (1997) J. Appl. Crystallogr. , vol.30 , pp. 565
    • Farrugia, L.J.1
  • 33
    • 0141452964 scopus 로고    scopus 로고
    • WinGX suite for small-molecule single-crystal crystallography
    • Farrugia, L. J. WinGX suite for small-molecule single-crystal crystallography J. Appl. Crystallogr. 1999, 32, 837-838
    • (1999) J. Appl. Crystallogr. , vol.32 , pp. 837-838
    • Farrugia, L.J.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.