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Volumn 17, Issue 14, 2007, Pages 3916-3920

Co-crystal structure guided array synthesis of PPARγ inverse agonists

Author keywords

Inverse agonist; PPAR

Indexed keywords

2 CHLORO 5 NITRO N (4 PYRIDYL)BENZAMIDE; 2 CHLORO 5 NITROBENZANILIDE; 2,4 THIAZOLIDINEDIONE DERIVATIVE; CARBOXYLIC ACID; FARGLITAZAR; GLUCOSE; GSK 5737; GSK 5775; GW 0072; LIPID; PD 068235; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA AGONIST; TRANSCRIPTION FACTOR GAL4; UNCLASSIFIED DRUG;

EID: 34250313113     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.04.111     Document Type: Article
Times cited : (16)

References (21)
  • 4
  • 11
    • 34250305198 scopus 로고    scopus 로고
    • Buckholz, R. G.; Trump, R. P.; Zhao, S.; Iannone, M. A.; Leesnitzer, L. M.; Merrihew, R. V.; Lobe, D. C.; Winegar, D. A.; Lazar, M. A.; Cobb, J. E.; Willson, T. M.; Hoekstra, W. J.; Billin, A. B. Biochem. Biophys. Res. Commun., submitted for publication; also see supplemental material.
  • 14
    • 34250362406 scopus 로고    scopus 로고
    • note
    • Co-crystals of compound 2t with the PPARγ LBD were grown from a complex containing 15 mg/ml protein (20 mM Tris, pH 8.0, 5 mM DTT, 100 mM NaCl, 2 mM EDTA) complexed at a 5:1 molar ratio with the compound (at 50 mM in DMSO) using the vapor phase diffusion method. The two co-crystals' PDB codes are 2pob (2t) and 1fm9 (farglitazar).
  • 16
    • 34250325576 scopus 로고    scopus 로고
    • note
    • 3, 300 MHz) δ 8.1 (d, J = 6.1, 2H), 7.5 (m, 2H), 7.4 (m, 6H), 7.3 (m, 1H), 7.2 (s, 3H), 7.0 (m, 2H), 6.8 (d, J = 8.6, 1H), 6.7 (d, J = 8.6, 2H), 4.2 (t, J = 6.1, 2H), 3.0 (d, J = 5.8, 2H), 2.8 (m, 1H), 2.4 (s, 3H), 2.0 (s, 1H), 1.9 (s, 3H), 1.8 (m, 2H), 1.2 (m, 1H). MS (APCI) m/z 574 (M+1).
  • 18
    • 34250331687 scopus 로고    scopus 로고
    • note
    • 11 Because only array members shown in Table 2 were run in this assay, results for other high MW array members with an arene/two-carbon tether motif are not available.
  • 21
    • 34250359533 scopus 로고    scopus 로고
    • note
    • The study of a PPARγ inverse agonist in a diabetic animal model will be disclosed in a future communication.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.