메뉴 건너뛰기




Volumn 52, Issue 4, 2009, Pages 904-907

Discovery of XL335 (WAY-362450), a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR)

Author keywords

[No Author keywords available]

Indexed keywords

3 [2 [2 CHLORO 4 [3 (2,6 DICHLOROPHENYL) 5 ISOPROPYL 4 ISOXAZOLYLMETHOXY]PHENYL]VINYL]BENZOIC ACID; 6 ALPHA ETHYL CHENODEOXYCHOLILC ACID; AZEPINO[4,5 B]INDOLE; CHOLESTEROL; FARNESOID X RECEPTOR; INDOLE DERIVATIVE; TRIACYLGLYCEROL; UNCLASSIFIED DRUG; WAY 362450; XL 335;

EID: 64349115048     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm8014124     Document Type: Article
Times cited : (150)

References (29)
  • 2
    • 0028836714 scopus 로고
    • Isolation of proteins that interact specifically with the retinoid X receptor: Two novel orphan receptors
    • Seol, W.; Choi, H. S.; Moore, D. D. Isolation of proteins that interact specifically with the retinoid X receptor: two novel orphan receptors. Mol. Endocrinol. 1995, 9, 72-85.
    • (1995) Mol. Endocrinol , vol.9 , pp. 72-85
    • Seol, W.1    Choi, H.S.2    Moore, D.D.3
  • 4
    • 0033574663 scopus 로고    scopus 로고
    • A unified nomenclature system for the nuclear receptor superfamily
    • Nuclear Receptor Nomenclature Committee
    • Nuclear Receptor Nomenclature Committee. A unified nomenclature system for the nuclear receptor superfamily. Cell 1999, 97, 161 - 163.
    • (1999) Cell , vol.97 , pp. 161-163
  • 5
    • 33748950271 scopus 로고    scopus 로고
    • Lee, F. Y.; Lee, H.; Hubbert, M. L.; Edwards, P.A. FXR, a multipurpose nuclear receptor. Trends Biochem. Sci. 2006, 31, 572-580.
    • Lee, F. Y.; Lee, H.; Hubbert, M. L.; Edwards, P.A. FXR, a multipurpose nuclear receptor. Trends Biochem. Sci. 2006, 31, 572-580.
  • 6
    • 0034664729 scopus 로고    scopus 로고
    • Targeted disruption of the nuclear receptor FXR/BAR impairs bile acid and lipid homeostasis
    • Sinal, C. J.; Tohkin, M.; Miyata, M.; Ward, J. M.; Lambert, G.; Gonzalez, F. J. Targeted disruption of the nuclear receptor FXR/BAR impairs bile acid and lipid homeostasis. Cell 2000, 102, 731-744.
    • (2000) Cell , vol.102 , pp. 731-744
    • Sinal, C.J.1    Tohkin, M.2    Miyata, M.3    Ward, J.M.4    Lambert, G.5    Gonzalez, F.J.6
  • 7
    • 37349010675 scopus 로고    scopus 로고
    • FXR signaling in metabolic disease
    • Zhang, Y; Edwards, P. FXR signaling in metabolic disease. FEBS Lett. 2008, 582, 10-18.
    • (2008) FEBS Lett , vol.582 , pp. 10-18
    • Zhang, Y.1    Edwards, P.2
  • 8
    • 0036164154 scopus 로고    scopus 로고
    • BAREing it all: The adoption of LXR and FXR and their roles in lipid homeostasis
    • Edwards, P. A.; Kast, H. R.; Anisfeld, A. M. BAREing it all: the adoption of LXR and FXR and their roles in lipid homeostasis. J. Lipid Res. 2002, 43, 2-12.
    • (2002) J. Lipid Res , vol.43 , pp. 2-12
    • Edwards, P.A.1    Kast, H.R.2    Anisfeld, A.M.3
  • 9
    • 33645983221 scopus 로고    scopus 로고
    • LXRs and FXR: The yin and yang of cholesterol and fat metabolism
    • Kalaany, N. Y.; Mangelsdorf, D. J. LXRs and FXR: the yin and yang of cholesterol and fat metabolism. Annu. Rev. Physiol. 2006, 68, 159-191.
    • (2006) Annu. Rev. Physiol , vol.68 , pp. 159-191
    • Kalaany, N.Y.1    Mangelsdorf, D.J.2
  • 12
    • 0033026760 scopus 로고    scopus 로고
    • Endogenous bile acids are ligands for the nuclear receptor FXR/BAR
    • (c)Wang, H.; Chen, J.; Hollister, K.; Sowers, L. C.; Forman, B. M. Endogenous bile acids are ligands for the nuclear receptor FXR/BAR. Mol. Cell 1999, 3, 543-553.
    • (1999) Mol. Cell , vol.3 , pp. 543-553
    • Wang, H.1    Chen, J.2    Hollister, K.3    Sowers, L.C.4    Forman, B.M.5
  • 13
    • 33749344968 scopus 로고    scopus 로고
    • Nuclear bile acid receptor FXR as pharmacological target: Are we there yet?
    • Modica, S.; Moschetta, A. Nuclear bile acid receptor FXR as pharmacological target: are we there yet? FEBS Lett. 2006, 580, 5492-5499.
    • (2006) FEBS Lett , vol.580 , pp. 5492-5499
    • Modica, S.1    Moschetta, A.2
  • 19
    • 64349088419 scopus 로고    scopus 로고
    • Compound 6m (XL335) has also been presented as WAY-362450 (FXR-450): Indoleazepines as a New Class of Nonsteroidal Agonists of the Farnesoid X Receptor: Identification of WAY-362450 (FXR- 450) as a Clinical Candidate for the Treatment of Dyslipidemia. Abstracts of Papers, 235th National Meeting of the American Chemical Society, New Orleans, LA, Apr 6-10, 2008; American Chemical Society: Washington, DC, 2008.
    • Compound 6m (XL335) has also been presented as WAY-362450 (FXR-450): Indoleazepines as a New Class of Nonsteroidal Agonists of the Farnesoid X Receptor: Identification of WAY-362450 (FXR- 450) as a Clinical Candidate for the Treatment of Dyslipidemia. Abstracts of Papers, 235th National Meeting of the American Chemical Society, New Orleans, LA, Apr 6-10, 2008; American Chemical Society: Washington, DC, 2008.
  • 20
    • 64349113519 scopus 로고    scopus 로고
    • Azepinoindole and Pyridoindole Derivatives As Pharmaceutical Agents
    • U.S. Patent Application US 20040023947
    • Martin, R.; Wang, T.-L.; Flatt, B. T.; Gu, X.-H.; Griffith, R. Azepinoindole and Pyridoindole Derivatives As Pharmaceutical Agents. U.S. Patent Application US 20040023947, 2004.
    • (2004)
    • Martin, R.1    Wang, T.-L.2    Flatt, B.T.3    Gu, X.-H.4    Griffith, R.5
  • 22
    • 64349103493 scopus 로고    scopus 로고
    • Kuehne et al. propose that the rearrangement of carbolines to the corresponding azepino[4,5- b]indoles occurs via intramolecular N-alkylation followed by opening of the resulting aziridine.
    • (b) Kuehne et al. propose that the rearrangement of carbolines to the corresponding azepino[4,5- b]indoles occurs via intramolecular N-alkylation followed by opening of the resulting aziridine.
  • 23
    • 0034664729 scopus 로고    scopus 로고
    • Targeted disruption of the nuclear receptor FXR/BAR impairs bile acid and lipid homeostasis
    • (a) Sinal, C. J.; Tohkin, M.; Miyata, M.; Ward, J. M.; Lambert, G.; Gonzales, F. J. Targeted disruption of the nuclear receptor FXR/BAR impairs bile acid and lipid homeostasis. Cell 2000, 102, 731-744.
    • (2000) Cell , vol.102 , pp. 731-744
    • Sinal, C.J.1    Tohkin, M.2    Miyata, M.3    Ward, J.M.4    Lambert, G.5    Gonzales, F.J.6
  • 25
    • 0033637121 scopus 로고    scopus 로고
    • Goodwin, B.; Jones, S. A.; Price, R. R.; Watson, M. A.; McKee, D. D.; Moore, L. B.; Galardi, C.; Wilson, J. G.; Lewis, M. C.; Roth, M. E.; Maloney, P. R.; Willson, T. M.; Kliewer, S. A. A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis. Mol. Cell 2000, 6, 517-526.
    • (a) Goodwin, B.; Jones, S. A.; Price, R. R.; Watson, M. A.; McKee, D. D.; Moore, L. B.; Galardi, C.; Wilson, J. G.; Lewis, M. C.; Roth, M. E.; Maloney, P. R.; Willson, T. M.; Kliewer, S. A. A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis. Mol. Cell 2000, 6, 517-526.
  • 27
    • 0033570028 scopus 로고    scopus 로고
    • Identification of a bile acid-responsive element in the human ileal bile acid-binding protein gene
    • Grober, J.; Zaghini, I.; Fujii, H.; Jones, S. A.; Kliewer, S. A.; Willson, T. M.; Ono, T.; Besnard, P. Identification of a bile acid-responsive element in the human ileal bile acid-binding protein gene. J. Biol. Chem. 1999, 274, 29749-29754.
    • (1999) J. Biol. Chem , vol.274 , pp. 29749-29754
    • Grober, J.1    Zaghini, I.2    Fujii, H.3    Jones, S.A.4    Kliewer, S.A.5    Willson, T.M.6    Ono, T.7    Besnard, P.8
  • 28
    • 14844304328 scopus 로고    scopus 로고
    • Regulation of complement C3 expression by the bile acid receptor FXR
    • Li, J.; Pircher, P. C.; Schulman, I. G.; Westin, S. K. Regulation of complement C3 expression by the bile acid receptor FXR. J. Biol. Chem. 2005, 280, 7427-7434.
    • (2005) J. Biol. Chem , vol.280 , pp. 7427-7434
    • Li, J.1    Pircher, P.C.2    Schulman, I.G.3    Westin, S.K.4
  • 29
    • 0035800772 scopus 로고    scopus 로고
    • Human bile salt export pump promoter is transactivated by the farnesoid X receptor/bile acid receptor
    • Ananthanarayanan, M.; Balasubramanian, N.; Makishima, M.; Mangelsdorf, D. J.; Suchy, F. J. Human bile salt export pump promoter is transactivated by the farnesoid X receptor/bile acid receptor. J. Biol. Chem. 2001, 276, 28857-28865.
    • (2001) J. Biol. Chem , vol.276 , pp. 28857-28865
    • Ananthanarayanan, M.1    Balasubramanian, N.2    Makishima, M.3    Mangelsdorf, D.J.4    Suchy, F.J.5


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.