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1
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33846844912
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For comprehensive reviews on DPP-4 inhibitors, see:
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For comprehensive reviews on DPP-4 inhibitors, see:. Idris I., and Donnelly R. Diabetes Obes. Metab. 9 (2007) 153
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Idris, I.1
Donnelly, R.2
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6
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0036228243
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Pospisilik J.A., Stafford S.G., Demuth H.-U., Brownsey R., Parkhouse W., Finegood D.T., McIntosh C.H.S., and Pederson R.A. Diabetes 51 (2002) 943
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Pospisilik, J.A.1
Stafford, S.G.2
Demuth, H.-U.3
Brownsey, R.4
Parkhouse, W.5
Finegood, D.T.6
McIntosh, C.H.S.7
Pederson, R.A.8
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7
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33947690115
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For a discussion of toxicities associated with thiazolidides like P32/98, see:
-
For a discussion of toxicities associated with thiazolidides like P32/98, see:. Thornberry N.A., and Weber A.E. Curr. Top. Med. Chem. 7 (2007) 557
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Thornberry, N.A.1
Weber, A.E.2
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8
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25144476018
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Hulin B., Cabral S., Lopaze M.G., Van Volkenberg M.A., Andrews K.M., and Parker J.C. Bioorg. Med. Chem. Lett. 15 (2005) 4770
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Hulin, B.1
Cabral, S.2
Lopaze, M.G.3
Van Volkenberg, M.A.4
Andrews, K.M.5
Parker, J.C.6
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9
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33745151060
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Edmondson S.D., Mastracchio A., Mathvink R.J., He J., Harper B., Park Y.-J., Beconi M., Di Salvo J., Eiermann G.J., He H., Leiting B., Leone J.F., Levorse D.A., Lyons K., Patel R.A., Patel S.B., Petrov A., Scapin G., Shang J., Roy R.S., Smith A., Wu J.K., Xu S., Zhu B., Thornberry N.A., and Weber A.E. J. Med. Chem. 49 (2006) 3614
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Edmondson, S.D.1
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Mathvink, R.J.3
He, J.4
Harper, B.5
Park, Y.-J.6
Beconi, M.7
Di Salvo, J.8
Eiermann, G.J.9
He, H.10
Leiting, B.11
Leone, J.F.12
Levorse, D.A.13
Lyons, K.14
Patel, R.A.15
Patel, S.B.16
Petrov, A.17
Scapin, G.18
Shang, J.19
Roy, R.S.20
Smith, A.21
Wu, J.K.22
Xu, S.23
Zhu, B.24
Thornberry, N.A.25
Weber, A.E.26
more..
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11
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61849100672
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-
note
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6O: C, 55.73; H, 6.60; N, 22.94. Found: C, 55.78; H, 6.54; N, 22.68.
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-
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13
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0023851313
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DPP-3 substrate 125 μM Arg-Arg-AMC. See:
-
DPP-3 substrate 125 μM Arg-Arg-AMC. See:. Abramic M., Zubanovic M., and Vitale L. Biol. Chem. 369 (1988) 29-38
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(1988)
Biol. Chem.
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-
Abramic, M.1
Zubanovic, M.2
Vitale, L.3
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14
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0033780088
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-
DPP-8 substrate 200 μM Ala-Pro-AMC. See:
-
DPP-8 substrate 200 μM Ala-Pro-AMC. See:. Abbot C.A., Yu D.M., Woollatt E., Sutherland G.R., McCaughan G.W., and Gorrell M.D. Eur. J. Biochem. 267 (2000) 6140-6150
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Eur. J. Biochem.
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Abbot, C.A.1
Yu, D.M.2
Woollatt, E.3
Sutherland, G.R.4
McCaughan, G.W.5
Gorrell, M.D.6
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15
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0037121086
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DPP-9 substrate 200 μM Ala-Pro-AMC. See:
-
DPP-9 substrate 200 μM Ala-Pro-AMC. See:. Olsen C., and Wagtmann N. Gene 299 (2002) 185-193
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(2002)
Gene
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Olsen, C.1
Wagtmann, N.2
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16
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0028286026
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FAP substrate 200 μM Ala-Pro-AMC. See:
-
FAP substrate 200 μM Ala-Pro-AMC. See:. Scanlan M.J., Raj B.K.M., Calvo B., Garin-Chesa P., Sanz-Moncasi M.P., Healey J.H., Old L.J., and Rettig W.J. Proc. Natl. Acad. Sci. U.S.A. 91 (1994) 5657-5661
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(1994)
Proc. Natl. Acad. Sci. U.S.A.
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Scanlan, M.J.1
Raj, B.K.M.2
Calvo, B.3
Garin-Chesa, P.4
Sanz-Moncasi, M.P.5
Healey, J.H.6
Old, L.J.7
Rettig, W.J.8
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17
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0026457193
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-
APP substrate 500 μM Arg-Pro-Pro. See:
-
APP substrate 500 μM Arg-Pro-Pro. See:. Rusu I., and Yaron A. Eur. J. Biochem. 210 (1992) 93-100
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(1992)
Eur. J. Biochem.
, vol.210
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-
Rusu, I.1
Yaron, A.2
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19
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33744830876
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-
The dipeptidyl peptidase enzyme inhibition assays and rat pharmacokinetic assays are described in:
-
The dipeptidyl peptidase enzyme inhibition assays and rat pharmacokinetic assays are described in:. Wright S.W., Ammirati M.J., Andrews K.M., Brodeur A.M., Danley D.E., Doran S.D., Lillquist J.S., McClure L.D., McPherson R.K., Orena S.J., Parker J.C., Polivkova J., Qiu X., Soeller W.C., Soglia C.B., Treadway J.L., VanVolkenberg M.A., Wang H., Wilder D.C., and Olson T.V. J. Med. Chem. 49 (2006) 3068
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J. Med. Chem.
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Wright, S.W.1
Ammirati, M.J.2
Andrews, K.M.3
Brodeur, A.M.4
Danley, D.E.5
Doran, S.D.6
Lillquist, J.S.7
McClure, L.D.8
McPherson, R.K.9
Orena, S.J.10
Parker, J.C.11
Polivkova, J.12
Qiu, X.13
Soeller, W.C.14
Soglia, C.B.15
Treadway, J.L.16
VanVolkenberg, M.A.17
Wang, H.18
Wilder, D.C.19
Olson, T.V.20
more..
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20
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19944427998
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The pharmacodynamic assay is described in:
-
The pharmacodynamic assay is described in:. Kim D., Wang L., Beconi M., Eiermann G.J., Fisher M.H., He H., Hickey G.J., Kowalchick J.E., Leiting B., Lyons K., Marsilio F., McCann M.E., Patel R.A., Petrov A., Scapin G., Patel S.B., Sinha Roy R., Wu J.K., Wyvratt M.J., Zhang B.B., Zhu L., Thornberry N.A., and Weber A.E. J. Med. Chem. 48 (2005) 141
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J. Med. Chem.
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Kim, D.1
Wang, L.2
Beconi, M.3
Eiermann, G.J.4
Fisher, M.H.5
He, H.6
Hickey, G.J.7
Kowalchick, J.E.8
Leiting, B.9
Lyons, K.10
Marsilio, F.11
McCann, M.E.12
Patel, R.A.13
Petrov, A.14
Scapin, G.15
Patel, S.B.16
Sinha Roy, R.17
Wu, J.K.18
Wyvratt, M.J.19
Zhang, B.B.20
Zhu, L.21
Thornberry, N.A.22
Weber, A.E.23
more..
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21
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61849105107
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-
Affinity-Assay for the Human ERG Potassium Channel; Greengrass, P. M, Stewart, M, Wood, C. M. PCT Patent Application WO 03/021271
-
Affinity-Assay for the Human ERG Potassium Channel; Greengrass, P. M.; Stewart, M.; Wood, C. M. PCT Patent Application WO 03/021271.
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22
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34347233484
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Singleton D.H., Boyd H., Steidl-Nichols J.V., Deacon M., de Groot M.J., Price D., Nettleton D.O., Wallace N.K., Troutman M.D., Williams C., and Boyd J.G. J. Med. Chem. 50 (2007) 2931
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J. Med. Chem.
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Singleton, D.H.1
Boyd, H.2
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Deacon, M.4
de Groot, M.J.5
Price, D.6
Nettleton, D.O.7
Wallace, N.K.8
Troutman, M.D.9
Williams, C.10
Boyd, J.G.11
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23
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0019441262
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-
Hamill O.P., Marty A., Neher E., Sakmann B., and Sigworth F.J. Eur. J. Physiol. 391 (1981) 85-100
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(1981)
Eur. J. Physiol.
, vol.391
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Hamill, O.P.1
Marty, A.2
Neher, E.3
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Sigworth, F.J.5
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24
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7444240355
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Diaz G.J., Daniell K., Leitza S.T., Martin R.L., Su Z., McDermott J.S., Cox B.F., and Gintant G.A. J. Pharmacol. Toxicol. Methods 50 (2004) 187
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Diaz, G.J.1
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Martin, R.L.4
Su, Z.5
McDermott, J.S.6
Cox, B.F.7
Gintant, G.A.8
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25
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61849110860
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-
note
-
The structure has been deposited in the Protein Data Bank with the deposition code 3F8S.
-
-
-
-
26
-
-
61849124371
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-
note
-
In vitro clearance values for compound 5: Human liver microsome intrinsic clearance (HLM CLint) < 7.0 mg/mL/kg, n = 4. Human hepatocyte intrinsic clearance (HH Clint) < 7.1 mg/mL/kg, n = 2.
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27
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43149126332
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Dai H., Gustavson S.M., Preston G.M., Eskra J.D., Calle R., and Hirshberg B. Diabetes Obes. Metab. 10 (2008) 506
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Dai, H.1
Gustavson, S.M.2
Preston, G.M.3
Eskra, J.D.4
Calle, R.5
Hirshberg, B.6
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