-
1
-
-
2942581416
-
-
Alonso A., Sasin J., Bottini N., Friedberg I., Friedberg I., Osterman A., Godzik A., Hunter T., Dixon J., and Mustelin T. Cell 117 (2004) 699
-
(2004)
Cell
, vol.117
, pp. 699
-
-
Alonso, A.1
Sasin, J.2
Bottini, N.3
Friedberg, I.4
Friedberg, I.5
Osterman, A.6
Godzik, A.7
Hunter, T.8
Dixon, J.9
Mustelin, T.10
-
7
-
-
0028990357
-
-
Kole H.K., Akamatsu M., Ye B., Yan X., Barford D., Roller P.P., and Burke T.R. Biochem. Biophys. Res. Commun. 209 (1995) 817
-
(1995)
Biochem. Biophys. Res. Commun.
, vol.209
, pp. 817
-
-
Kole, H.K.1
Akamatsu, M.2
Ye, B.3
Yan, X.4
Barford, D.5
Roller, P.P.6
Burke, T.R.7
-
8
-
-
0028785789
-
-
Chen L., Wu L., Otaka A., Smyth M.S., Roller P.R., Burke T.R., den Hertog J., and Zhang Z.-Y. Biochem. Biophys. Res. Commun. 216 (1995) 976
-
(1995)
Biochem. Biophys. Res. Commun.
, vol.216
, pp. 976
-
-
Chen, L.1
Wu, L.2
Otaka, A.3
Smyth, M.S.4
Roller, P.R.5
Burke, T.R.6
den Hertog, J.7
Zhang, Z.-Y.8
-
9
-
-
0032503030
-
-
Huyer G., Kelly J., Moffat J., Zamboni R., Jia Z., Gresser M.J., and Ramachandran C. Anal. Biochem. 258 (1998) 19
-
(1998)
Anal. Biochem.
, vol.258
, pp. 19
-
-
Huyer, G.1
Kelly, J.2
Moffat, J.3
Zamboni, R.4
Jia, Z.5
Gresser, M.J.6
Ramachandran, C.7
-
10
-
-
1842424803
-
-
Romsicki Y., Reece M., Gauthier J.-Y., Asante-Appiah E., and Kennedy B.P. J. Biol. Chem. 279 (2004) 12868
-
(2004)
J. Biol. Chem.
, vol.279
, pp. 12868
-
-
Romsicki, Y.1
Reece, M.2
Gauthier, J.-Y.3
Asante-Appiah, E.4
Kennedy, B.P.5
-
12
-
-
0036235963
-
-
Leung C., Lee J., Meyer N., Jia C., Grzyb J., Liu S., Hum G., and Taylor S.D. Bioorg. Med. Chem. 10 (2002) 2309
-
(2002)
Bioorg. Med. Chem.
, vol.10
, pp. 2309
-
-
Leung, C.1
Lee, J.2
Meyer, N.3
Jia, C.4
Grzyb, J.5
Liu, S.6
Hum, G.7
Taylor, S.D.8
-
14
-
-
0000524510
-
-
Burke T.R., Ye B., Yan X., Wang S., Jia Z., Chen L., Zhang Z.-Y., and Barford D. Biochemistry 35 (1996) 15898
-
(1996)
Biochemistry
, vol.35
, pp. 15898
-
-
Burke, T.R.1
Ye, B.2
Yan, X.3
Wang, S.4
Jia, Z.5
Chen, L.6
Zhang, Z.-Y.7
Barford, D.8
-
15
-
-
0034193474
-
-
Gao Y., Wu L., Luo J.H., Guo R., Yang D., Zhang Z.-Y., and Burke T.R. Bioorg. Med. Chem. Lett. 10 (2000) 923
-
(2000)
Bioorg. Med. Chem. Lett.
, vol.10
, pp. 923
-
-
Gao, Y.1
Wu, L.2
Luo, J.H.3
Guo, R.4
Yang, D.5
Zhang, Z.-Y.6
Burke, T.R.7
-
16
-
-
47349130121
-
-
Sing, L. C.; Lau, C. K.; Therien, M.; Gauthier, J.-Y.; Bayly, C.; Dufresne, C.; Fortin, R.; Leblanc, Y. International Application, Patent Cooperation Treaty Patent WO 2001/70753.
-
Sing, L. C.; Lau, C. K.; Therien, M.; Gauthier, J.-Y.; Bayly, C.; Dufresne, C.; Fortin, R.; Leblanc, Y. International Application, Patent Cooperation Treaty Patent WO 2001/70753.
-
-
-
-
17
-
-
10744228071
-
-
Lau C.K., Bayly C.I., Gauthier J.-Y., Li C.S., Therien M., Asante-Appiah E., Cromlish W., Boie Y., Forghani F., Desmarais S., Wang Q., Skorey K., Waddleton D., Payette P., Ramachandran C., Kennedy B.P., and Giovana Scapin G. Bioorg. Med. Chem. Lett. 14 (2004) 1043
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 1043
-
-
Lau, C.K.1
Bayly, C.I.2
Gauthier, J.-Y.3
Li, C.S.4
Therien, M.5
Asante-Appiah, E.6
Cromlish, W.7
Boie, Y.8
Forghani, F.9
Desmarais, S.10
Wang, Q.11
Skorey, K.12
Waddleton, D.13
Payette, P.14
Ramachandran, C.15
Kennedy, B.P.16
Giovana Scapin, G.17
-
18
-
-
10744228866
-
-
Dufresne C., Roy P., Wang Z., Asante-Appiah E., Cromlish W., Boie Y., Forghani F., Desmarais S., Wang Q., Skorey K., Waddleton D., Ramachandran C., Kennedy B.P., Xu L., Gordon R., Chan C.C., and Leblanc Y. Bioorg. Med. Chem. Lett. 14 (2004) 1039
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 1039
-
-
Dufresne, C.1
Roy, P.2
Wang, Z.3
Asante-Appiah, E.4
Cromlish, W.5
Boie, Y.6
Forghani, F.7
Desmarais, S.8
Wang, Q.9
Skorey, K.10
Waddleton, D.11
Ramachandran, C.12
Kennedy, B.P.13
Xu, L.14
Gordon, R.15
Chan, C.C.16
Leblanc, Y.17
-
19
-
-
33847202286
-
-
Julien S.G., Dube N., Read M., Penney J., Paquet M., Yongxin Han Y., Brian P Kennedy B.P., Muller W.J., and Tremblay M.L. Nat. Genet. 39 (2007) 338
-
(2007)
Nat. Genet.
, vol.39
, pp. 338
-
-
Julien, S.G.1
Dube, N.2
Read, M.3
Penney, J.4
Paquet, M.5
Yongxin Han, Y.6
Brian P Kennedy, B.P.7
Muller, W.J.8
Tremblay, M.L.9
-
20
-
-
33750006859
-
-
Cromlish W.A., Tang M., Kyskan R., Tran L., and Kennedy B.P. Biochem. Pharmacol. 72 (2006) 1279
-
(2006)
Biochem. Pharmacol.
, vol.72
, pp. 1279
-
-
Cromlish, W.A.1
Tang, M.2
Kyskan, R.3
Tran, L.4
Kennedy, B.P.5
-
21
-
-
85033821017
-
-
Differding E., Duthaler R.O., Kreiger A., Ruegg G.M., and Schmit C. Synlett (1991) 395
-
(1991)
Synlett
, pp. 395
-
-
Differding, E.1
Duthaler, R.O.2
Kreiger, A.3
Ruegg, G.M.4
Schmit, C.5
-
24
-
-
0037132579
-
-
note
-
Benzyl bromide 21 has been prepared in 77% yield by refluxing a solution of 3-bromo-4-methylbenzoic acid methyl ester, N-bromosuccinimide, and cat. benzoyl peroxide in carbon tetrachloride for 10 h. See: Curran, D. P.; Yang, F.; Cheong, J.-h. J. Am. Chem. Soc. 2002, 124, 14993. We have found that compound 21 can be prepared in a 93% yield by subjecting a refluxing solution of 3-bromo-4-methylbenzoic acid methyl ester, N-bromosuccinimide, and cat. benzoyl peroxide in benzene to a 250 W lamp for 6 h.
-
-
-
-
32
-
-
47349110198
-
-
note
-
m of the substrate, DIFMUP, under our conditions was found to be the same (5 μM) as that determined by MerckFrosst in the absence of DMSO (see Ref. 20).
-
-
-
-
33
-
-
0027336612
-
-
3Na)OH and standard manual Fmoc solid-phase peptide synthesis techniques. See:
-
3Na)OH and standard manual Fmoc solid-phase peptide synthesis techniques. See:. Miranda M.T.M., Liddle R.A., and Rivier J.E. J. Med. Chem. 36 (1993) 1681
-
(1993)
J. Med. Chem.
, vol.36
, pp. 1681
-
-
Miranda, M.T.M.1
Liddle, R.A.2
Rivier, J.E.3
-
34
-
-
47349115598
-
-
note
-
It is also possible that this large difference in potency between the DFMS and DFMP inhibitors is because the DFMP group is dianionic at pH 6.5 and PTP1B prefers to bind the dianionic DFMP-based inhibitors as opposed to the monoanionic DFMS-based inhibitors. However, as mentioned earlier, previous studies (see Refs. 5c and 10) suggest that PTP1B binds the monoanionic and dianionic forms of DFMP-bearing inhibitors equally well.
-
-
-
-
37
-
-
33745953734
-
-
Amarasinghe K.K.D., Evidokimov A.G., Xu K., Clark C.M., Maier M.B., Srivastava A., Colson A.-O., Gerwe G.S., Stake G.E., Howard B.W., Pokross M.E., Gray J.L., and Peters K.G. Bioorg. Med. Chem. Lett. 16 (2006) 4252
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 4252
-
-
Amarasinghe, K.K.D.1
Evidokimov, A.G.2
Xu, K.3
Clark, C.M.4
Maier, M.B.5
Srivastava, A.6
Colson, A.-O.7
Gerwe, G.S.8
Stake, G.E.9
Howard, B.W.10
Pokross, M.E.11
Gray, J.L.12
Peters, K.G.13
-
38
-
-
47349087089
-
-
Xin Z., liu G., Abad-Zapatero C., Pei Z., Szczepankiewicz B.G., Li X., Zhang T., Hutchins C.W., Hajduk P.J., Ballron S.J., Stashko M.A., Lubben T.H., Trevillyan J.M., and Jirousek M.R. Bioorg. Med. Chem. Lett. 16 (2006) 4252
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 4252
-
-
Xin, Z.1
liu, G.2
Abad-Zapatero, C.3
Pei, Z.4
Szczepankiewicz, B.G.5
Li, X.6
Zhang, T.7
Hutchins, C.W.8
Hajduk, P.J.9
Ballron, S.J.10
Stashko, M.A.11
Lubben, T.H.12
Trevillyan, J.M.13
Jirousek, M.R.14
-
39
-
-
0141680857
-
-
Liu G., Xin Z., Pei Z., Hajduk P.J., Abad-Zapatero C., Hutchins C.W., Zhao H., Lubben T.H., Ballron S.J., Haasch D.L., Kaszubska W., Rondinone C.M., Trevillyan J.M., and Jirousek M.R. J. Med. Chem. 46 (2003) 4232
-
(2003)
J. Med. Chem.
, vol.46
, pp. 4232
-
-
Liu, G.1
Xin, Z.2
Pei, Z.3
Hajduk, P.J.4
Abad-Zapatero, C.5
Hutchins, C.W.6
Zhao, H.7
Lubben, T.H.8
Ballron, S.J.9
Haasch, D.L.10
Kaszubska, W.11
Rondinone, C.M.12
Trevillyan, J.M.13
Jirousek, M.R.14
-
40
-
-
47349087654
-
-
Erlanson, D. A.; McDowell, R. S.; He, M. M.; Randal, M.; Simmons, R. L.; Kung, J.; Waight, A.; Hansen, S. K.
-
Erlanson, D. A.; McDowell, R. S.; He, M. M.; Randal, M.; Simmons, R. L.; Kung, J.; Waight, A.; Hansen, S. K.
-
-
-
-
41
-
-
37549060353
-
-
and references therein
-
Douty B., Wayland B., Ala P.J., Bower M.J., Pruitt J., Bostrom L., Wei M., Klabe R., Gonneville L., Wynn R., Burn T.C., Liu P.C.C., Combs A.P., and Yue E.W. Bioorg. Med. Chem. Lett. 18 (2008) 66 and references therein
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 66
-
-
Douty, B.1
Wayland, B.2
Ala, P.J.3
Bower, M.J.4
Pruitt, J.5
Bostrom, L.6
Wei, M.7
Klabe, R.8
Gonneville, L.9
Wynn, R.10
Burn, T.C.11
Liu, P.C.C.12
Combs, A.P.13
Yue, E.W.14
-
42
-
-
0000749654
-
-
Gilbert A.M., Katz T.J., Geiger W.E., Robben M.P., and Reingold A.L. J. Am. Chem. Soc. 115 (1993) 3199
-
(1993)
J. Am. Chem. Soc.
, vol.115
, pp. 3199
-
-
Gilbert, A.M.1
Katz, T.J.2
Geiger, W.E.3
Robben, M.P.4
Reingold, A.L.5
-
43
-
-
0035854750
-
-
A pFLAG plasmid expressing the catalytic domain (residues 1-298) of human PTP1B was expressed in BL21 (DE3) cells and purified according to a two-step purification protocol (Cibracon blue affinity column and Sepharose Q anion exchange column) previously described by Asante-Appiah et al. See:
-
A pFLAG plasmid expressing the catalytic domain (residues 1-298) of human PTP1B was expressed in BL21 (DE3) cells and purified according to a two-step purification protocol (Cibracon blue affinity column and Sepharose Q anion exchange column) previously described by Asante-Appiah et al. See:. Asante-Appiah E., Ball K., Bateman K., Skorey K., Friesen R., Desponts C., Payette P., Bayly C., Zamboni R., Scapin G., Ramachandran C., Kennedy B.P. J. Biol. Chem. 276 (2001) 26036
-
(2001)
J. Biol. Chem.
, vol.276
, pp. 26036
-
-
Asante-Appiah, E.1
Ball, K.2
Bateman, K.3
Skorey, K.4
Friesen, R.5
Desponts, C.6
Payette, P.7
Bayly, C.8
Zamboni, R.9
Scapin, G.10
Ramachandran, C.11
Kennedy, B.P.12
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