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9
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0141461415
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M.J. During, L. Cao, D.S. Zuzga, J.S. Francis, H.L. Fitzsimons, X. Jiao, R.J. Bland, M. Klugmann, W.A. Banks, D.J. Drucker, and C.N. Haile Nat. Med. 9 2003 1173
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During, M.J.1
Cao, L.2
Zuzga, D.S.3
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Fitzsimons, H.L.5
Jiao, X.6
Bland, R.J.7
Klugmann, M.8
Banks, W.A.9
Drucker, D.J.10
Haile, C.N.11
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10
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2442482515
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B. Ahren, M. Landin-Olsson, P.-A. Jansson, M. Svensson, D. Holmes, and A. Schweizer J. Clin. Endocrin. Metab. 89 2004 2078
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Ahren, B.1
Landin-Olsson, M.2
Jansson, P.-A.3
Svensson, M.4
Holmes, D.5
Schweizer, A.6
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11
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20944439078
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Xu, J; Wei, L.; Mathvink, R.; He, J.; Park, Y.-J.; He, H.; Leiting, B.; Lyons, K. A.; Marsilio, F.; Patel, R. A.; Wu, J. K.; Thornberry, N. A.; Weber, A. E.; Parmee, E. R. Bioorg. Med. Chem. Lett. 2005, 15, 2533
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Xu, J.1
Wei, L.2
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He, H.6
Leiting, B.7
Lyons, K.A.8
Marsilio, F.9
Patel, R.A.10
Wu, J.K.11
Thornberry, N.A.12
Weber, A.E.13
Parmee, E.R.14
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12
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4544315126
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-
50 determinations for hERG was carried out as described in R.W. Friesen, Y. Ducharme, R.G. Ball, M. Blouin, L. Boulet, B. Cote, R. Frenette, M. Girard, D. Guay, Z. Huang, T.R. Jones, F. Laliberte, J.J. Lynch, J. Mancini, E. Martins, P. Masson, E. Muise, D.J. Pon, P.K.S. Siegel, A. Styhler, N.N. Tsou, M.J. Turner, R.N. Young, and Y. Girard J. Med. Chem. 46 2003 2017
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Friesen, R.W.1
Ducharme, Y.2
Ball, R.G.3
Blouin, M.4
Boulet, L.5
Cote, B.6
Frenette, R.7
Girard, M.8
Guay, D.9
Huang, Z.10
Jones, T.R.11
Laliberte, F.12
Lynch, J.J.13
Mancini, J.14
Martins, E.15
Masson, P.16
Muise, E.17
Pon, D.J.18
Siegel, P.K.S.19
Styhler, A.20
Tsou, N.N.21
Turner, M.J.22
Young, R.N.23
Girard, Y.24
more..
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17
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10744233045
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C.G. Caldwell, P. Chen, J. He, E.R. Parmee, B. Leiting, F. Marsilio, R.A. Patel, J.K. Wu, G.J. Eiermann, A. Petrov, H. He, K.A. Lyons, N.A. Thornberry, and A.E. Weber Bioorg. Med. Chem. Lett. 14 2004 1265
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Caldwell, C.G.1
Chen, P.2
He, J.3
Parmee, E.R.4
Leiting, B.5
Marsilio, F.6
Patel, R.A.7
Wu, J.K.8
Eiermann, G.J.9
Petrov, A.10
He, H.11
Lyons, K.A.12
Thornberry, N.A.13
Weber, A.E.14
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18
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19944368450
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note
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1H NMR and LC-MS
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-
-
-
19
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0037964447
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50 determinations for DPP-IV and other proline peptidases were carried out as described in B. Leiting, K.D. Pryor, J.K. Wu, F. Marsilio, R.A. Patel, C.S. Craik, J.A. Ellman, R.T. Cummings, and N.A. Thornberry Biochem. J. 371 2003 525
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Biochem. J.
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Leiting, B.1
Pryor, K.D.2
Wu, J.K.3
Marsilio, F.4
Patel, R.A.5
Craik, C.S.6
Ellman, J.A.7
Cummings, R.T.8
Thornberry, N.A.9
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20
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0242267905
-
-
1 position of dipeptide α-amino amide inhibitors has been investigated with DPP-IV and QPP (DPP-II). For a lead reference, see: K. Senten, P.V. Veken, I. De Meeser, A.-M. Lambeir, S. Scharpe, A. Haemers, and K. Augustyns J. Med. Chem. 46 2003 5005
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J. Med. Chem.
, vol.46
, pp. 5005
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Senten, K.1
Veken, P.V.2
De Meeser, I.3
Lambeir, A.-M.4
Scharpe, S.5
Haemers, A.6
Augustyns, K.7
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21
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4544227213
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G. Lankas, B. Leiting, R. Sinha Roy, G. Eiermann, T. Biftu, D. Kim, H. Ok, A.E. Weber, and N.A. Thornberry Diabetes 53 2004 A2
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(2004)
Diabetes
, vol.53
, pp. 2
-
-
Lankas, G.1
Leiting, B.2
Sinha Roy, R.3
Eiermann, G.4
Biftu, T.5
Kim, D.6
Ok, H.7
Weber, A.E.8
Thornberry, N.A.9
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22
-
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19944411526
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note
-
50's against human calcium and sodium channels were also measured, and activity at hERG is indicative of activity at these other ion channels
-
-
-
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23
-
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19944369124
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-
note
-
It should be noted that the % inhibition as determined using the in vitro assay underestimates the % inhibition achieved in vivo, since compound 22 is a competitive, reversible inhibitor and the assay of plasma DPP-IV activity requires dilution of plasma (resulting in dilution of the total inhibitor) and the presence of substrate that competes with inhibitor for binding to the enzyme
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