-
1
-
-
0036830528
-
Malarial dihydroorotate dehydrogenase. Substrate and inhibitor specificity
-
doi:10.1074/jbc.M206854200
-
Baldwin J, Farajallah AM, Malmquist NA, Rathod PK, Phillips MA (2002) Malarial dihydroorotate dehydrogenase. Substrate and inhibitor specificity. J Biol Chem 277:41827. doi:10.1074/jbc.M206854200
-
(2002)
J Biol Chem
, vol.277
, pp. 41827
-
-
Baldwin, J.1
Farajallah, A.M.2
Malmquist, N.A.3
Rathod, P.K.4
Phillips, M.A.5
-
2
-
-
20444470318
-
High-throughput screening for potent and selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase
-
doi:10.1074/jbc.M501100200
-
Baldwin J, Michnoff CH, Malmquist NA, White J, Roth MG, Rathod PK, Phillips MA (2005) High-throughput screening for potent and selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase. J Biol Chem 280:21847. doi:10.1074/jbc.M501100200
-
(2005)
J Biol Chem
, vol.280
, pp. 21847
-
-
Baldwin, J.1
Michnoff, C.H.2
Malmquist, N.A.3
White, J.4
Roth, M.G.5
Rathod, P.K.6
Phillips, M.A.7
-
3
-
-
60849131483
-
Dihydroorotate dehydrogenase inhibitor A771726 (leflunomide) induces apoptosis and diminishes proliferation of multiple myeloma cells
-
doi:10.1158/1535-7163.MCT-08-0664
-
Baumann P, Mandl-Weber S, Volkl A, Adam C, Bumeder I, Oduncu F, Schmidmaier R (2009) Dihydroorotate dehydrogenase inhibitor A771726 (leflunomide) induces apoptosis and diminishes proliferation of multiple myeloma cells. Mol Cancer Ther 8:366. doi:10.1158/1535-7163.MCT-08-0664
-
(2009)
Mol Cancer Ther
, vol.8
, pp. 366
-
-
Baumann, P.1
Mandl-Weber, S.2
Volkl, A.3
Adam, C.4
Bumeder, I.5
Oduncu, F.6
Schmidmaier, R.7
-
4
-
-
7444223383
-
Of malaria, metabolism and membrane transport
-
doi:10.1016/j.pt.2004.09.004
-
Becker K, Kirk K (2004) Of malaria, metabolism and membrane transport. TRENDS Parasitol 20:590. doi:10.1016/j.pt.2004.09.004
-
(2004)
TRENDS Parasitol
, vol.20
, pp. 590
-
-
Becker, K.1
Kirk, K.2
-
5
-
-
13844317355
-
Synthesis of brequinar analogue inhibitors of malaria parasite dihydroorotate dehydrogenase
-
doi:10.1016/j.bmc.2005.01.017
-
Boa AN, Canavan SP, Hirst PR, Ramsey C, Stead AM, McConkey GA (2005) Synthesis of brequinar analogue inhibitors of malaria parasite dihydroorotate dehydrogenase. Bioorg Med Chem 13:1945. doi:10.1016/j.bmc.2005.01.017
-
(2005)
Bioorg Med Chem
, vol.13
, pp. 1945
-
-
Boa, A.N.1
Canavan, S.P.2
Hirst, P.R.3
Ramsey, C.4
Stead, A.M.5
McConkey, G.A.6
-
6
-
-
0034972445
-
The ears of the hippopotamus: Manifestations, determinants, and estimates of the malaria burden
-
Breman JG (2001) The ears of the hippopotamus: manifestations, determinants, and estimates of the malaria burden. Am J Trop Med Hyg 64:1
-
(2001)
Am J Trop Med Hyg
, vol.64
, pp. 1
-
-
Breman, J.G.1
-
7
-
-
0027672324
-
Sample-distance partial least squares: PLS optimized for many variables, with application to CoMFA
-
Bush BL, Nachbar RB Jr (1993) Sample-distance partial least squares: PLS optimized for many variables, with application to CoMFA. J Comput Aided Mol Des 7:587
-
(1993)
J Comput Aided Mol des
, vol.7
, pp. 587
-
-
Bush, B.L.1
Nachbar Jr., R.B.2
-
8
-
-
33646547593
-
Malaria: Therapy, genes and vaccines
-
Chiang PK, Bujnicki JM, Su X, Lanar DE (2006) Malaria: therapy, genes and vaccines. Curr Mol Med 6:309
-
(2006)
Curr Mol Med
, vol.6
, pp. 309
-
-
Chiang, P.K.1
Bujnicki, J.M.2
Su, X.3
Lanar, D.E.4
-
9
-
-
0023751431
-
Comparative molecular field analysis (CoMFA). 1. Effect of shape on binding of steroids to carrier proteins
-
doi:10.1021/ja00226a005
-
Cramer RD, Patterson DE, Bunce JD (1988) Comparative molecular field analysis (CoMFA). 1. Effect of shape on binding of steroids to carrier proteins. J Am Chem Soc 110:5959. doi:10.1021/ja00226a005
-
(1988)
J Am Chem Soc
, vol.110
, pp. 5959
-
-
Cramer, R.D.1
Patterson, D.E.2
Bunce, J.D.3
-
11
-
-
0030032806
-
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase
-
doi:10.1021/bi952168g
-
Davis JP, Cain GA, Pitts WJ, Magolda RL, Copeland RA (1996) The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase. Biochemistry 35:1270. doi:10.1021/bi952168g
-
(1996)
Biochemistry
, vol.35
, pp. 1270
-
-
Davis, J.P.1
Cain, G.A.2
Pitts, W.J.3
Magolda, R.L.4
Copeland, R.A.5
-
12
-
-
0037404259
-
Active leflunomide metabolite inhibits interleukin 1beta, tumour necrosis factor alpha, nitric oxide, and metalloproteinase-3 production in activated human synovial tissue cultures
-
Elkayam O, Yaron I, Shirazi I, Judovitch R, Caspi D, Yaron M (2003) Active leflunomide metabolite inhibits interleukin 1beta, tumour necrosis factor alpha, nitric oxide, and metalloproteinase-3 production in activated human synovial tissue cultures. Ann Rheum Dis 62:440
-
(2003)
Ann Rheum Dis
, vol.62
, pp. 440
-
-
Elkayam, O.1
Yaron, I.2
Shirazi, I.3
Judovitch, R.4
Caspi, D.5
Yaron, M.6
-
13
-
-
3042550882
-
Antimalarial drug discovery: Efficacy models for compound screening
-
doi:10.1038/nrd1416
-
Fidock DA, Rosenthal PJ, Croft SL, Brun R, Nwaka S (2004) Antimalarial drug discovery: efficacy models for compound screening. Nat Rev Drug Discov 3:509. doi:10.1038/nrd1416
-
(2004)
Nat Rev Drug Discov
, vol.3
, pp. 509
-
-
Fidock, D.A.1
Rosenthal, P.J.2
Croft, S.L.3
Brun, R.4
Nwaka, S.5
-
14
-
-
33644802299
-
Synthesis and biological activity of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 2: 20-substituted triclosan derivatives
-
doi:10.1016/j.bmcl.2006.01.051
-
Freundlich JS, Yu M, Lucumi E, Kuo M, Tsai HC, Valderramos JC, Karagyozov L, Jacobs WR Jr, Schiehser GA, Fidock DA, Jacobus DP, Sacchettini JC (2006) Synthesis and biological activity of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 2: 20-substituted triclosan derivatives. Bioorg Med Chem Lett 16:2163. doi:10.1016/j.bmcl.2006.01.051
-
(2006)
Bioorg Med Chem Lett
, vol.16
, pp. 2163
-
-
Freundlich, J.S.1
Yu, M.2
Lucumi, E.3
Kuo, M.4
Tsai, H.C.5
Valderramos, J.C.6
Karagyozov, L.7
Jacobs Jr., W.R.8
Schiehser, G.A.9
Fidock, D.A.10
Jacobus, D.P.11
Sacchettini, J.C.12
-
15
-
-
34250628103
-
Principles of QSAR models validation: Internal and external
-
Gramatica P (2007) Principles of QSAR models validation: internal and external. QSAR Comb Sci 26:694
-
(2007)
QSAR Comb Sci
, vol.26
, pp. 694
-
-
Gramatica, P.1
-
16
-
-
64549087994
-
Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice
-
doi:10.1021/jm801343r
-
Gujjar R, Marwaha A, El Mazouni F, White J, White KL, Creason S, Shackleford DM, Baldwin J, Charman WN, Buckner FS, Charman S, Rathod PK, Phillips MA (2009) Identification of a metabolically stable triazolopyrimidine- based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice. J Med Chem 52:1864. doi:10.1021/jm801343r
-
(2009)
J Med Chem
, vol.52
, pp. 1864
-
-
Gujjar, R.1
Marwaha, A.2
El Mazouni, F.3
White, J.4
White, K.L.5
Creason, S.6
Shackleford, D.M.7
Baldwin, J.8
Charman, W.N.9
Buckner, F.S.10
Charman, S.11
Rathod, P.K.12
Phillips, M.A.13
-
17
-
-
0032773737
-
A771726, the active metabolite of leflunomide, directly inhibits the activity of cyclooxygenase-2 in vitro and in vivo in a substrate-sensitive manner
-
doi:10.1038/sj.bjp.0702708
-
Hamilton LC, Vojnovic I, Warner TD (1999) A771726, the active metabolite of leflunomide, directly inhibits the activity of cyclooxygenase-2 in vitro and in vivo in a substrate-sensitive manner. Br J Pharmacol 127:1589. doi:10.1038/sj.bjp.0702708
-
(1999)
Br J Pharmacol
, vol.127
, pp. 1589
-
-
Hamilton, L.C.1
Vojnovic, I.2
Warner, T.D.3
-
18
-
-
27744519288
-
The first de novo designed inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase
-
doi:10.1016/j.bmcl.2005.09.045
-
Heikkila T, Thirumalairajan S, Davies M, Parsons MR, McConkey AG, Fishwick CW, Johnson AP (2006) The first de novo designed inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase. Bioorg Med Chem Lett 16:88. doi:10.1016/j.bmcl.2005.09.045
-
(2006)
Bioorg Med Chem Lett
, vol.16
, pp. 88
-
-
Heikkila, T.1
Thirumalairajan, S.2
Davies, M.3
Parsons, M.R.4
McConkey, A.G.5
Fishwick, C.W.6
Johnson, A.P.7
-
19
-
-
33846407609
-
Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase
-
doi:10.1021/jm060687j
-
Heikkila T, Ramsey C, Davies M, Galtier C, Stead AM, Johnson AP, Fishwick CW, Boa AN, McConkey GA (2007) Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase. J Med Chem 50:186. doi:10.1021/jm060687j
-
(2007)
J Med Chem
, vol.50
, pp. 186
-
-
Heikkila, T.1
Ramsey, C.2
Davies, M.3
Galtier, C.4
Stead, A.M.5
Johnson, A.P.6
Fishwick, C.W.7
Boa, A.N.8
McConkey, G.A.9
-
20
-
-
33646583490
-
Structure of Plasmodium falciparum dihydroorotate dehydrogenase with a bound inhibitor
-
doi:10.1107/S0907444905042642
-
Hurt DE, Widom J, Clardy J (2006) Structure of Plasmodium falciparum dihydroorotate dehydrogenase with a bound inhibitor. Acta Crystallogr D 62:312. doi:10.1107/S0907444905042642
-
(2006)
Acta Crystallogr D
, vol.62
, pp. 312
-
-
Hurt, D.E.1
Widom, J.2
Clardy, J.3
-
22
-
-
0542451678
-
Comparative molecular similarity indices analysis: CoMSIA
-
doi:10.1023/A:1017025803403
-
Klebe G (1998) Comparative molecular similarity indices analysis: CoMSIA. Perspect Drug Discov Des 12:87. doi:10.1023/A:1017025803403
-
(1998)
Perspect Drug Discov des
, vol.12
, pp. 87
-
-
Klebe, G.1
-
23
-
-
0027944195
-
Molecular similarity indices in a comparative analysis (CoMSIA) of drug molecules to correlate and predict their biological activity
-
Klebe G, Abraham U, Mietzner T (1994) Molecular similarity indices in a comparative analysis (CoMSIA) of drug molecules to correlate and predict their biological activity. J Med Chem 37:4130
-
(1994)
J Med Chem
, vol.37
, pp. 4130
-
-
Klebe, G.1
Abraham, U.2
Mietzner, T.3
-
24
-
-
3242762374
-
The active metabolite of leflunomide, A771726, inhibits both the generation of and the bone-resorbing activity of osteoclasts by acting directly on cells of the osteoclast lineage
-
doi:10.1007/s00774-003-0489-4
-
Kobayashi Y, Ueyama S, Arai Y, Yoshida Y, Kaneda T, Sato T, Shin K, Kumegawa M, Hakeda Y (2004) The active metabolite of leflunomide, A771726, inhibits both the generation of and the bone-resorbing activity of osteoclasts by acting directly on cells of the osteoclast lineage. J Bone Miner Metab 22:318. doi:10.1007/s00774-003-0489-4
-
(2004)
J Bone Miner Metab
, vol.22
, pp. 318
-
-
Kobayashi, Y.1
Ueyama, S.2
Arai, Y.3
Yoshida, Y.4
Kaneda, T.5
Sato, T.6
Shin, K.7
Kumegawa, M.8
Hakeda, Y.9
-
25
-
-
2542441062
-
Effects of leflunomide and its active metabolite on the production and mRNA expression of TNF-alpha in peritoneal macrophages and synovial cells with adjuvant arthritis in rats
-
Li WD, Lin ZB (2002) Effects of leflunomide and its active metabolite on the production and mRNA expression of TNF-alpha in peritoneal macrophages and synovial cells with adjuvant arthritis in rats. Yao Xue Xue Bao 37:767
-
(2002)
Yao Xue Xue Bao
, vol.37
, pp. 767
-
-
Li, W.D.1
Lin, Z.B.2
-
26
-
-
0036155407
-
RNA interference (RNAi) inhibits growth of Plasmodium falciparum
-
doi+S0166685101004297[pii]
-
McRobert L, McConkey GA (2002) RNA interference (RNAi) inhibits growth of Plasmodium falciparum. Mol Biochem Parasitol 119:273. doi: S0166685101004297[pii]
-
(2002)
Mol Biochem Parasitol
, vol.119
, pp. 273
-
-
McRobert, L.1
McConkey, G.A.2
-
27
-
-
39149137841
-
Leflunomide-induced lung injury that developed after its withdrawal, coinciding with peripheral blood lymphocyte count decrease
-
doi:10.1007/s10165-007-0014-z
-
Otsuka T, Koyama T, Ohtani R, Niiro H, Yoshizawa S, Harada M, Inokuma S (2008) Leflunomide-induced lung injury that developed after its withdrawal, coinciding with peripheral blood lymphocyte count decrease. Mod Rheumatol 18:96. doi:10.1007/s10165-007-0014-z
-
(2008)
Mod Rheumatol
, vol.18
, pp. 96
-
-
Otsuka, T.1
Koyama, T.2
Ohtani, R.3
Niiro, H.4
Yoshizawa, S.5
Harada, M.6
Inokuma, S.7
-
28
-
-
0037450952
-
Microwave effects in solvent-free esters aminolysis
-
doi:10.1016/S0040-4020(03)00151-0
-
Perreux L, Loupy A, Delmotte M (2003) Microwave effects in solvent-free esters aminolysis. Tetrahedron 59:2185. doi:10.1016/S0040-4020(03)00151-0
-
(2003)
Tetrahedron
, vol.59
, pp. 2185
-
-
Perreux, L.1
Loupy, A.2
Delmotte, M.3
-
29
-
-
45749119578
-
Triazolopyrimidine-based dihydroorotate dehydrogenase inhibitors with potent and selective activity against the malaria parasite Plasmodium falciparum
-
doi:10.1021/jm8001026
-
Phillips MA, Gujjar R, Malmquist NA, White J, El Mazouni F, Baldwin J, Rathod PK (2008) Triazolopyrimidine-based dihydroorotate dehydrogenase inhibitors with potent and selective activity against the malaria parasite Plasmodium falciparum. J Med Chem 51:3649. doi:10.1021/jm8001026
-
(2008)
J Med Chem
, vol.51
, pp. 3649
-
-
Phillips, M.A.1
Gujjar, R.2
Malmquist, N.A.3
White, J.4
El Mazouni, F.5
Baldwin, J.6
Rathod, P.K.7
-
30
-
-
33751269892
-
An improved and highly sensitive microfluorimetric method for assessing susceptibility of Plasmodium falciparum to antimalarial drugs in vitro
-
doi:10.1186/1475-2875-5-95
-
Quashie NB, de Koning HP, Ranford-Cartwright LC (2006) An improved and highly sensitive microfluorimetric method for assessing susceptibility of Plasmodium falciparum to antimalarial drugs in vitro. Malar J 5:95. doi:10.1186/1475-2875-5-95
-
(2006)
Malar J
, vol.5
, pp. 95
-
-
Quashie, N.B.1
De Koning, H.P.2
Ranford-Cartwright, L.C.3
-
31
-
-
84987100711
-
Crossvalidation, bootstrapping, and partial least squares compared with multiple regression in conventional QSAR studies
-
Richard D, Cramer RD III, Bunce JD, Patterson DE, Frank IE (1988) Crossvalidation, bootstrapping, and partial least squares compared with multiple regression in conventional QSAR studies. Quant. Struct. Act. Relat. 7:18
-
(1988)
Quant. Struct. Act. Relat.
, vol.7
, pp. 18
-
-
Richard, D.1
Cramer III, R.D.2
Bunce, J.D.3
Patterson, D.E.4
Frank, I.E.5
-
32
-
-
0037034009
-
Medical need, scientific opportunity and the drive for antimalarial drugs
-
doi:10.1038/415686a
-
Ridley RG (2002) Medical need, scientific opportunity and the drive for antimalarial drugs. Nature 415:686. doi:10.1038/415686a
-
(2002)
Nature
, vol.415
, pp. 686
-
-
Ridley, R.G.1
-
33
-
-
0030537683
-
Bootstrap model selection
-
Shao J (1996) Bootstrap model selection. J Am Stat Assoc 91:655
-
(1996)
J Am Stat Assoc
, vol.91
, pp. 655
-
-
Shao, J.1
-
34
-
-
0002309097
-
-
Kubinyi H (ed) ESCOM Science Publishers, Leiden
-
Wold S, Johansson E, Cocchi M (1993) In: Kubinyi H (ed) 3D QSAR in drug design: theory, methods and applications. ESCOM Science Publishers, Leiden, p 523
-
(1993)
3D QSAR in Drug Design: Theory, Methods and Applications
, pp. 523
-
-
Wold, S.1
Johansson, E.2
Cocchi, M.3
-
35
-
-
3142677793
-
A 771726, the active metabolite of leflunomide, inhibits TNF-alpha and IL-1 from Kupffer cells
-
Yao HW, Li J, Chen JQ, Xu SY (2004a) A 771726, the active metabolite of leflunomide, inhibits TNF-alpha and IL-1 from Kupffer cells. Inflammation 28:97
-
(2004)
Inflammation
, vol.28
, pp. 97
-
-
Yao, H.W.1
Li, J.2
Chen, J.Q.3
Xu, S.Y.4
-
36
-
-
28744433733
-
The active metabolite of leflunomide A771726 inhibits proliferation and collagen synthesis of hepatic stellate cell
-
Yao HW, Li J, Chen JQ, Xu SY (2004b) The active metabolite of leflunomide A771726 inhibits proliferation and collagen synthesis of hepatic stellate cell. Zhejiang Xue Xue Bao Yi Xue Ban 33:515
-
(2004)
Zhejiang Xue Xue Bao Yi Xue Ban
, vol.33
, pp. 515
-
-
Yao, H.W.1
Li, J.2
Chen, J.Q.3
Xu, S.Y.4
-
37
-
-
33745530646
-
An exploratory study on in vitro effects and mechanism of leflunomide on dendritic cells of systemic lupus erythematosus
-
Zhang X, Zhou H, Dong GF, Shi YZ (2005) An exploratory study on in vitro effects and mechanism of leflunomide on dendritic cells of systemic lupus erythematosus. Zhonghua Nei Ke Za Zhi 44:370
-
(2005)
Zhonghua Nei Ke Za Zhi
, vol.44
, pp. 370
-
-
Zhang, X.1
Zhou, H.2
Dong, G.F.3
Shi, Y.Z.4
-
38
-
-
45749157232
-
The active metabolite of leflunomide A771726 inhibits corneal neovascularization
-
doi:10.1007/s11596-008-0332-1
-
Zhang M, Hao N, Bian F (2008) The active metabolite of leflunomide A771726 inhibits corneal neovascularization. J Huazhong Univ Sci Technol Med Sci 28:364. doi:10.1007/s11596-008-0332-1
-
(2008)
J Huazhong Univ Sci Technol Med Sci
, vol.28
, pp. 364
-
-
Zhang, M.1
Hao, N.2
Bian, F.3
|