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Volumn 4, Issue 1, 2013, Pages 63-68

Identification of tetrahydropyrido[4,3-d]pyrimidine amides as a new class of orally bioavailable TGR5 agonists

Author keywords

agonist; diabetes; GLP 1; GPCR; TGR5

Indexed keywords

G PROTEIN COUPLED RECEPTOR; PYRIMIDINE DERIVATIVE; TAKEDA G PROTEIN COUPLED RECEPTOR 5; TETRAHYDROPYRIDO[4,3 D]PYRIMIDINE AMIDE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 84872285850     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml300277t     Document Type: Article
Times cited : (44)

References (23)
  • 1
    • 67349288052 scopus 로고    scopus 로고
    • TGR5: An Emerging Bile Acid G-protein Coupled Receptor Target for the Potential Treatment of Metabolic Disorders
    • Tiwari, A.; Maiti, P. TGR5: An Emerging Bile Acid G-protein Coupled Receptor Target for the Potential Treatment of Metabolic Disorders Drug Discovery Today 2009, 14, 523-530
    • (2009) Drug Discovery Today , vol.14 , pp. 523-530
    • Tiwari, A.1    Maiti, P.2
  • 2
    • 77949425951 scopus 로고    scopus 로고
    • TGR5 as a Therapeutic Target for Treating Obesity
    • Zhong, M. TGR5 as a Therapeutic Target for Treating Obesity Curr. Top. Med. Chem. 2010, 10, 386-396
    • (2010) Curr. Top. Med. Chem. , vol.10 , pp. 386-396
    • Zhong, M.1
  • 3
    • 79956088562 scopus 로고    scopus 로고
    • The Bile Acid Membrane Receptor TGR5 as an Emerging Target in Metabolism and Inflammation
    • Pols, T. W.; Noriega, L. G.; Nomura, M.; Auwerx, J.; Schoonjans, K. The Bile Acid Membrane Receptor TGR5 as an Emerging Target in Metabolism and Inflammation J. Hepatol. 2011, 54, 1263-1272
    • (2011) J. Hepatol. , vol.54 , pp. 1263-1272
    • Pols, T.W.1    Noriega, L.G.2    Nomura, M.3    Auwerx, J.4    Schoonjans, K.5
  • 4
    • 80054098593 scopus 로고    scopus 로고
    • Bile Acid Receptor Modulators in Metabolic Diseases
    • Xu, Y. Bile Acid Receptor Modulators in Metabolic Diseases Annu. Rep. Med. Chem. 2011, 46, 69-87
    • (2011) Annu. Rep. Med. Chem. , vol.46 , pp. 69-87
    • Xu, Y.1
  • 5
    • 13844299425 scopus 로고    scopus 로고
    • Bile Acids Promote Glucagon-like Peptide-1 Secretion Through TGR5 in a Murine Enteroendocrine Cell Line STC-1
    • Katsuma, S.; Hirasawa, A.; Tsujimoto, G. Bile Acids Promote Glucagon-like Peptide-1 Secretion Through TGR5 in a Murine Enteroendocrine Cell Line STC-1 Biochem. Biophys. Res. Commun. 2005, 329, 386-390
    • (2005) Biochem. Biophys. Res. Commun. , vol.329 , pp. 386-390
    • Katsuma, S.1    Hirasawa, A.2    Tsujimoto, G.3
  • 8
    • 80053308007 scopus 로고    scopus 로고
    • The G-Protein-Coupled Bile Acid Receptor, Gpbar1 (TGR5), Negatively Regulates Hepatic Inflammatory Response Through Antagonizing Nuclear Factor Kappa Light-Chain Enhancer of Activated B Cells (NF-κB) in Mice
    • Wang, Y.-D.; Chen, W.-D.; Yu, D.; Forman, B. M.; Huang, W. The G-Protein-Coupled Bile Acid Receptor, Gpbar1 (TGR5), Negatively Regulates Hepatic Inflammatory Response Through Antagonizing Nuclear Factor Kappa Light-Chain Enhancer of Activated B Cells (NF-κB) in Mice Hepatology 2011, 54, 1421-1432
    • (2011) Hepatology , vol.54 , pp. 1421-1432
    • Wang, Y.-D.1    Chen, W.-D.2    Yu, D.3    Forman, B.M.4    Huang, W.5
  • 11
    • 41149144697 scopus 로고    scopus 로고
    • Novel Potent and Selective Bile Acid Derivatives as TGR5 Agonists: Biological Screening, Structure-Activity Relationships, and Molecular Modeling Studies
    • Sato, H.; Macchiarulo, A.; Thomas, C.; Gioiello, A.; Une, M.; Hofmann, A. F.; Saladin, R.; Schoonjans, K.; Pellicciari, R.; Auwerx, J. Novel Potent and Selective Bile Acid Derivatives as TGR5 Agonists: Biological Screening, Structure-Activity Relationships, and Molecular Modeling Studies J. Med. Chem. 2008, 51, 1831-1841
    • (2008) J. Med. Chem. , vol.51 , pp. 1831-1841
    • Sato, H.1    MacChiarulo, A.2    Thomas, C.3    Gioiello, A.4    Une, M.5    Hofmann, A.F.6    Saladin, R.7    Schoonjans, K.8    Pellicciari, R.9    Auwerx, J.10
  • 17
    • 84872308971 scopus 로고    scopus 로고
    • Agonists: The Measurement of Affinity and Efficacy in Functional Assays
    • In, 3 rd ed. Academic Press: New York, Chapter 5
    • Kenakin, T. Agonists: The Measurement of Affinity and Efficacy in Functional Assays. In A Pharmacology Primer: Theory, Applications, and Methods, 3 rd ed.; Academic Press: New York, 2009; Chapter 5, pp 81-100.
    • (2009) A Pharmacology Primer: Theory, Applications, and Methods , pp. 81-100
    • Kenakin, T.1
  • 21
    • 0035913059 scopus 로고    scopus 로고
    • oct: A Tool for Lipophilicity Determination in Drug Discovery. 2. Basic and Neutral Compounds
    • oct: A Tool for Lipophilicity Determination in Drug Discovery. 2. Basic and Neutral Compounds J. Med. Chem. 2001, 44, 2490-2497
    • (2001) J. Med. Chem. , vol.44 , pp. 2490-2497
    • Lombardo, F.1    Shalaeva, M.Y.2    Tupper K A, K.A.3    Gao, F.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.