-
3
-
-
0031581088
-
-
Sawzdargo M., George S.R., Nguyen T., Xu S., Kolakowski L.F., and O'Dowd B.F. Biochem. Biophys. Res. Commun. 239 (1997) 543
-
(1997)
Biochem. Biophys. Res. Commun.
, vol.239
, pp. 543
-
-
Sawzdargo, M.1
George, S.R.2
Nguyen, T.3
Xu, S.4
Kolakowski, L.F.5
O'Dowd, B.F.6
-
5
-
-
0038363378
-
-
Brown A.J., Goldsworthy S.M., Barnes A.A., Eilert M.M., Tcheang L., Daniels D., Muir A.I., Wigglesworth M.J., Kinghorn I., Fraser N.J., Pike N.B., Strum J.C., Steplewski K.M., Murdock P.R., Holder J.C., Marshall F.H., Szekeres P.G., Wilson S., Ignar D.M., Foord S.M., Wise A., and Dowell S.J. J. Biol. Chem. 278 (2003) 11312
-
(2003)
J. Biol. Chem.
, vol.278
, pp. 11312
-
-
Brown, A.J.1
Goldsworthy, S.M.2
Barnes, A.A.3
Eilert, M.M.4
Tcheang, L.5
Daniels, D.6
Muir, A.I.7
Wigglesworth, M.J.8
Kinghorn, I.9
Fraser, N.J.10
Pike, N.B.11
Strum, J.C.12
Steplewski, K.M.13
Murdock, P.R.14
Holder, J.C.15
Marshall, F.H.16
Szekeres, P.G.17
Wilson, S.18
Ignar, D.M.19
Foord, S.M.20
Wise, A.21
Dowell, S.J.22
more..
-
6
-
-
0038491435
-
-
Le Poul E., Loison C., Struyf S., Springael J.Y., Lannoy V., Decobecq M.E., Brezillon S., Dupriez V., Vassart G., Van Damme J., Parmentier M., and Detheux M. J. Biol. Chem. 278 (2003) 25481
-
(2003)
J. Biol. Chem.
, vol.278
, pp. 25481
-
-
Le Poul, E.1
Loison, C.2
Struyf, S.3
Springael, J.Y.4
Lannoy, V.5
Decobecq, M.E.6
Brezillon, S.7
Dupriez, V.8
Vassart, G.9
Van Damme, J.10
Parmentier, M.11
Detheux, M.12
-
10
-
-
27844440904
-
-
Hong Y.H., Nishimura Y., Hishikawa D., Tsuzuki H., Miyahara H., Gotoh C., Choi K.C., Feng D.D., Chen C., Lee H.G., Katoh K., Roh S.G., and Sasaki S. Endocrinology 146 (2005) 5092
-
(2005)
Endocrinology
, vol.146
, pp. 5092
-
-
Hong, Y.H.1
Nishimura, Y.2
Hishikawa, D.3
Tsuzuki, H.4
Miyahara, H.5
Gotoh, C.6
Choi, K.C.7
Feng, D.D.8
Chen, C.9
Lee, H.G.10
Katoh, K.11
Roh, S.G.12
Sasaki, S.13
-
11
-
-
50449087891
-
-
Ge H., Li X., Weiszmann J., Wang P., Baribault H., Chen J.-L., Tian H., and Li Y. Endocrinology 149 (2008) 4519
-
(2008)
Endocrinology
, vol.149
, pp. 4519
-
-
Ge, H.1
Li, X.2
Weiszmann, J.3
Wang, P.4
Baribault, H.5
Chen, J.-L.6
Tian, H.7
Li, Y.8
-
13
-
-
72249110998
-
-
note
-
4) with 25 mM HEPES and 0.01% (w/v) BSA were stimulated with forskolin (5 μM final in 5 μl/well) in the presence of serially diluted test ligands (5 μl/well) in a 384-well Optiplate (Perkin-Elmer) at room temperature for 30 min before adding antibody and lysis reagents according to manufacturer's protocol. The plates were further incubated in the dark overnight after adding detection solution, and read in CLIPR (Molecular Devices) for 1 min per plate. Data were expressed as Relative Luminescence Unit (RLU).
-
-
-
-
14
-
-
72249120084
-
-
note
-
Separated on ChiralPak AD-H column using 5% 2-propanol in hexanes. Retention times are 10.4 min for compound 3 and 13.8 min for compound 2.
-
-
-
-
15
-
-
72249111202
-
-
note
-
1H NMR and LC-MS.
-
-
-
-
19
-
-
72249101400
-
-
note
-
Separated on ChiralCel OJ-H using 15% 2-propanol in hexanes. Retention times are 11.8 min for (S)-enantiomer 87 and 17.2 min for its (R)-enantiomer.
-
-
-
-
20
-
-
72249086677
-
-
note
-
The chiral center was preserved under the coupling condition (step d in Scheme 1). The ee (enantiomeric excess) of 58 was determined to be >99%, by comparing to a mixture of S,R enantiomers (S/R = 3:1) that was obtained by running the same reaction using DBU (instead of 2,4,6-colidine) at room temperature. Retention times are 19.7 min for (S)-enantiomer 58 and 35.5 min for its (R)-enantiomer on ChiralPak AD-H using 5% 2-propanol in hexanes.
-
-
-
-
21
-
-
57349142454
-
-
Lee T., Schwandner R., Swaminath G., Weiszmann J., Cardozo M., Greenberg J., Jaeckel P., Ge H., Wang Y., Jiao X., Liu J., Kayser F., Tian H., and Li Y. Mol. Pharmacol. 74 (2008) 1599
-
(2008)
Mol. Pharmacol.
, vol.74
, pp. 1599
-
-
Lee, T.1
Schwandner, R.2
Swaminath, G.3
Weiszmann, J.4
Cardozo, M.5
Greenberg, J.6
Jaeckel, P.7
Ge, H.8
Wang, Y.9
Jiao, X.10
Liu, J.11
Kayser, F.12
Tian, H.13
Li, Y.14
-
22
-
-
72249117894
-
-
manuscript in preparation
-
Swaminath, G.; Jaeckel, P.; Guo, Q.; Cardozo, M.; Weiszmann, J.; Lindberg, R.; Wang, Y.; Schwandner, R.; Li, Y., manuscript in preparation.
-
-
-
Swaminath, G.1
Jaeckel, P.2
Guo, Q.3
Cardozo, M.4
Weiszmann, J.5
Lindberg, R.6
Wang, Y.7
Schwandner, R.8
Li, Y.9
-
25
-
-
72249084623
-
-
note
-
Age-matched male FFA2 knockout (KO) or wild type (WT) mice (C57Bl/6 background) were used in the studies. Mice were fasted overnight before the experiment. Compound or vehicle alone (10% dimethyl acetamide, 10% ethanol, 30% propylene glycol, 50% saline) was intraperitoneally (ip) injected (10 ml/kg) into mice at indicated doses. Blood samples were collected before and 15 minutes after injection by tail bleeding. Plasma FFA levels were measured using a Wako HR Series FFA-HR (2) kit following manufacturers instructions.
-
-
-
-
26
-
-
72249121989
-
-
note
-
At a high dose (20 mg/kg), however, compound 44 also reduced FFA levels in FFA2 KO mice, although to a lesser extent than in WT animals. This could be due to some off-target effects of compound 44, which was not extensively profiled against other targets. Compound 44 was inactive against a small panel of GPCRs that included FFA1, FFA3, GPR109A, GHSR, ETBR, CCR2, CXCR3, CXCR4, and CCR7 at concentrations up to 30 μM.
-
-
-
-
27
-
-
33646258753
-
-
Cheng K., Wu T.-J., Wu K.K., Sturino C., Metters K., Gottesdiener K., Wright S.D., Wang Z., O'Neill G., Lai E., and Waters M.G. Proc. Natl. Acad. Sci. U.S.A. 103 (2006) 6682
-
(2006)
Proc. Natl. Acad. Sci. U.S.A.
, vol.103
, pp. 6682
-
-
Cheng, K.1
Wu, T.-J.2
Wu, K.K.3
Sturino, C.4
Metters, K.5
Gottesdiener, K.6
Wright, S.D.7
Wang, Z.8
O'Neill, G.9
Lai, E.10
Waters, M.G.11
-
28
-
-
0028203880
-
-
Worm D., Henriksen J.E., Vaag A., Thye-Ronn P., Melander A., and Beck-Nielsen H. J. Clin. Endocrinol. Metab. 78 (1994) 717
-
(1994)
J. Clin. Endocrinol. Metab.
, vol.78
, pp. 717
-
-
Worm, D.1
Henriksen, J.E.2
Vaag, A.3
Thye-Ronn, P.4
Melander, A.5
Beck-Nielsen, H.6
|