-
1
-
-
0024430490
-
Mechanistic studies of lanosterol 14α-methyl demethylase: Substrate requirements for the component reactions catalyzed by a single cytochrome P-450 isozyme
-
Fischer, R. T., and Stam., S. H., Johnson, P. R., Ko, S. S., and Magolda., R. L., Gaylor, J. L., and Trzaskos, J. M. (1989) Mechanistic studies of lanosterol 14α-methyl demethylase: substrate requirements for the component reactions catalyzed by a single cytochrome P-450 isozyme. J. Lipid Res. 30, 1621-1632 (Pubitemid 19271057)
-
(1989)
Journal of Lipid Research
, vol.30
, Issue.10
, pp. 1621-1632
-
-
Fischer, R.T.1
Stam, S.H.2
Johnson, P.R.3
Ko, S.S.4
Magolda, R.L.5
Gaylor, J.L.6
Trzaskos, J.M.7
-
2
-
-
0021717363
-
Cytochrome P-450-dependent oxidation of lanosterol in cholesterol biosynthesis. Microsomal electron transport and C-32 demethylation
-
Trzaskos, J. M., and Bowen., W. D., Shafiee, A., Fischer, R. T., and Gaylor, J. L. (1984) Cytochrome P-450-dependent oxidation of lanosterol in cholesterol biosynthesis. Microsomal electron transport and C-32 demethylation. J. Biol. Chem. 259, 13402-13412 (Pubitemid 15223873)
-
(1984)
Journal of Biological Chemistry
, vol.259
, Issue.21
, pp. 13402-13412
-
-
Trzaskos, J.M.1
Bowen, W.D.2
Shafiee, A.3
-
3
-
-
1542407816
-
CYP51, the omnipotent P450
-
Lepesheva, G. I., and Waterman, M. R. (2004) CYP51, the omnipotent P450. Mol. Cell. Endocrinol. 215, 165-170
-
(2004)
Mol. Cell. Endocrinol.
, vol.215
, pp. 165-170
-
-
Lepesheva, G.I.1
Waterman, M.R.2
-
4
-
-
33846387040
-
Sterol 14α-demethylase cytochrome P450 (CYP51), a P450 in all biological kingdoms
-
DOI 10.1016/j.bbagen.2006.07.018, PII S0304416506002145
-
Lepesheva, G. I., and Waterman, M. R. (2007) Sterol 14a-demethylase cytochrome P450 (CYP51), a P450 in all biological kingdoms. Biochim. Biophys. Acta 1770, 467-477 (Pubitemid 46136743)
-
(2007)
Biochimica et Biophysica Acta - General Subjects
, vol.1770
, Issue.3
, pp. 467-477
-
-
Lepesheva, G.I.1
Waterman, M.R.2
-
5
-
-
0003638861
-
-
University Park Press, Baltimore
-
Nes, W. R., and McKean, M. R. (eds) (1977) Biochemistry of Steroids and Other Isopentenoids, pp. 325-411, University Park Press, Baltimore
-
(1977)
Biochemistry of Steroids and Other Isopentenoids
, pp. 325-411
-
-
Nes, W.R.1
McKean, M.R.2
-
6
-
-
0016386380
-
Chemotherapy of systemic mycoses
-
Bennett, J. E. (1974) Chemotherapy of systemic mycoses. N. Engl. J. Med. 290, 320-323
-
(1974)
N. Engl. J. Med.
, vol.290
, pp. 320-323
-
-
Bennett, J.E.1
-
7
-
-
0002661484
-
-
Ellis Horwood Ltd., Chichester, United Kingdom
-
Vanden Bossche, H. (ed) (1988) Mode of Action of Pyridine, Pyrimidine and Azole Antifungals, pp. 79-119, Ellis Horwood Ltd., Chichester, United Kingdom
-
(1988)
Mode of Action of Pyridine, Pyrimidine and Azole Antifungals
, pp. 79-119
-
-
Vanden Bossche, H.1
-
8
-
-
1642335814
-
History of the development of azole derivatives
-
Maertens, J. A. (2004) History of the development of azole derivatives. Clin. Microbiol. Infect. 10, Suppl. 1, 1-10 (Pubitemid 38379948)
-
(2004)
Clinical Microbiology and Infection
, vol.10
, Issue.SUPPL. 1
, pp. 1-10
-
-
Maertens, J.A.1
-
9
-
-
79960975304
-
Targeting trypanosoma cruzi sterol 14a-demethylase (CYP51)
-
Lepesheva, G.I., Villalta, F., and Waterman, M. R. (2011) Targeting Trypanosoma cruzi sterol 14a-demethylase (CYP51). Adv. Parasitol. 75, 65-87
-
(2011)
Adv. Parasitol.
, vol.75
, pp. 65-87
-
-
Lepesheva, G.I.1
Villalta, F.2
Waterman, M.R.3
-
10
-
-
80051901437
-
Drug developers finally take aim at a neglected disease
-
Leslie, M. (2011) Drug developers finally take aim at a neglected disease. Science 333, 933-935
-
(2011)
Science
, vol.333
, pp. 933-935
-
-
Leslie, M.1
-
11
-
-
0019596893
-
Biochemical and ultrastructural alterations produced by miconazole and econazole in trypanosoma cruzi
-
Docampo, R., and Moreno., S. N., Turrens, J. F., Katzin, A. M., Gonzalez-Cappa, S. M., and Stoppani, A. O. (1981) Biochemical and ultrastructural alterations produced by miconazole and econazole in Trypanosoma cruzi. Mol. Biochem. Parasitol. 3, 169-180
-
(1981)
Mol. Biochem. Parasitol.
, vol.3
, pp. 169-180
-
-
Docampo, R.1
Moreno, S.N.2
Turrens, J.F.3
Katzin, A.M.4
Gonzalez-Cappa, S.M.5
Stoppani, A.O.6
-
12
-
-
0022497077
-
Effects of ketoconazole on sterol biosynthesis by Trypanosoma cruzi epimastigotes
-
Beach, D.H., Goad, L. J., and Holz, G. G. (1986) Effects of ketoconazole on sterol biosynthesis by Trypanosoma cruzi epimastigotes. Biochem. Biophys. Res. Commun. 136, 851-856 (Pubitemid 16066708)
-
(1986)
Biochemical and Biophysical Research Communications
, vol.136
, Issue.3
, pp. 851-856
-
-
Beach, D.H.1
Goad, L.J.2
Holz Jr., G.G.3
-
13
-
-
0023681312
-
Antiproliferative synergism of the allylamine SF 86-327 and ketoconazole on epimastigotes and amastigotes of trypanosoma (Schizotrypanum) cruzi
-
Urbina, J. A., Lazardi, K., Aguirre, T., Piras, M. M., and Piras, R. (1988) Antiproliferative synergism of the allylamine SF 86-327 and ketoconazole on epimastigotes and amastigotes of Trypanosoma (Schizotrypanum) cruzi. Antimicrob. Agents Chemother. 32, 1237-1242
-
(1988)
Antimicrob. Agents Chemother.
, vol.32
, pp. 1237-1242
-
-
Urbina, J.A.1
Lazardi, K.2
Aguirre, T.3
Piras, M.M.4
Piras, R.5
-
14
-
-
17944384088
-
Treatment of chronic Chagas' disease with itraconazole and allopurinol
-
Apt, W., Aguilera, X., Arribada, A., Perez, C, Miranda, C, Sanchez, G., Zulantay, I., Cortes, P., Rodriguez, J., and Juri, D. (1998) Treatment of chronic Chagas' disease with itraconazole and allopurinol. Am. J. Trop. Med. Hyg. 59, 133-138 (Pubitemid 28304810)
-
(1998)
American Journal of Tropical Medicine and Hygiene
, vol.59
, Issue.1
, pp. 133-138
-
-
Apt, W.1
Aguilera, X.2
Arribada, A.3
Perez, C.4
Miranda, C.5
Sanchez, G.6
Zulantay, I.7
Cortes, P.8
Rodriguez, J.9
Juri, D.10
-
15
-
-
0343527887
-
A combination of benznidazole and ketoconazole enhances efficacy of chemotherapy of experimental Chagas' disease
-
Araújo, M. S., Martins-Filho, O. A., Pereira, M. E., and Brener, Z. (2000) A combination of benznidazole and ketoconazole enhances efficacy of chemotherapy of experimental Chagas' disease. J. Antimicrob. Chemother. 45, 819-824 (Pubitemid 30348953)
-
(2000)
Journal of Antimicrobial Chemotherapy
, vol.45
, Issue.6
, pp. 819-824
-
-
Araujo, M.S.S.1
Martins-Filho, O.A.2
Pereira, M.E.S.3
Brener, Z.4
-
16
-
-
0033987127
-
Activities of the triazole derivative SCH 56592 (Posaconazole) against drug-resistant strains of the protozoan parasite Trypanosoma (Schizotrypanum) cruzi in immunocompetent and immunosuppressed murine hosts
-
Molina, J., Martins-Filho, O., Brener, Z., and Romanha., A. J., Loebenberg, D., and Urbina, J. A. (2000) Activities of the triazole derivative SCH 56592 (posaconazole) against drug-resistant strains of the protozoan parasite Trypanosoma (Schizotrypanum) cruzi in immunocompetent and immunosuppressed murine hosts. Antimicrob. Agents Chemother. 44, 150-155 (Pubitemid 30010686)
-
(2000)
Antimicrobial Agents and Chemotherapy
, vol.44
, Issue.1
, pp. 150-155
-
-
Molina, J.1
Martins-Filho, O.2
Brener, Z.3
Romanha, A.J.4
Loebenberg, D.5
Urbina, J.A.6
-
17
-
-
69049116505
-
Ergosterol biosynthesis and drug development for chagas disease
-
Urbina, J. A. (2009) Ergosterol biosynthesis and drug development for Chagas disease. Mem. Inst. Oswaldo Cruz 104, Suppl. 1, 311-318
-
(2009)
Mem. Inst. Oswaldo Cruz
, vol.104
, Issue.SUPPL. 1
, pp. 311-318
-
-
Urbina, J.A.1
-
18
-
-
77954207000
-
Chagas disease: Pushing through the pipeline
-
Clayton, J. (2010) Chagas disease: pushing through the pipeline. Nature 465, S12-S15
-
(2010)
Nature
, vol.465
-
-
Clayton, J.1
-
19
-
-
23944466866
-
The protein farnesyltransferase inhibitor tipifarnib as a new lead for the development of drugs against Chagas disease
-
DOI 10.1021/jm050441z
-
Hucke, O., and Gelb., M. H., Verlinde, C L., and Buckner, F. S. (2005) The protein farnesyltransferase inhibitor tipifarnib as a new lead for the development of drugs against Chagas disease. J. Med. Chem. 48, 5415-5418 (Pubitemid 41209239)
-
(2005)
Journal of Medicinal Chemistry
, vol.48
, Issue.17
, pp. 5415-5418
-
-
Hucke, O.1
Gelb, M.H.2
Verlinde, C.L.M.J.3
Buckner, F.S.4
-
20
-
-
84865422539
-
Pharmacological characterization, structural studies, and in vivo activity of anti-chagas disease lead compounds derived from tipifarnib
-
Buckner, F. S., and Bahia., M. T., Suryadevara, P. K., White, K. L., and Shackleford., D. M., Chennamaneni, N. K., Hulverson, M. A., and Laydbak., J. U., Chatelain, E., Scandale, I., Verlinde, C. L., and Charman., S. A., Lepesheva, G. I., and Gelb, M. H. (2012) Pharmacological characterization, structural studies, and in vivo activity of anti-Chagas disease lead compounds derived from tipifarnib. Antimicrob. Agents Chemother. 56, 4914-4921
-
(2012)
Antimicrob. Agents Chemother.
, vol.56
, pp. 4914-4921
-
-
Buckner, F.S.1
Bahia, M.T.2
Suryadevara, P.K.3
White, K.L.4
Shackleford, D.M.5
Chennamaneni, N.K.6
Hulverson, M.A.7
Laydbak, J.U.8
Chatelain, E.9
Scandale, I.10
Verlinde, C.L.11
Charman, S.A.12
Lepesheva, G.I.13
Gelb, M.H.14
-
21
-
-
10744230525
-
A class of sterol 14-demethylase inhibitors as anti-Trypanosoma cruzi agents
-
DOI 10.1073/pnas.2535442100
-
Buckner, F., Yokoyama, K., Lockman, J., Aikenhead, K., Ohkanda, J., Sadilek, M., Sebti, S., Van Voorhis, W., Hamilton, A., and Gelb, M. H. (2003) A class of sterol 14-demethylase inhibitors as anti-Trypanosoma cruzi agents. Proc. Natl. Acad. Sci. U.S.A. 100, 15149-15153 (Pubitemid 37518031)
-
(2003)
Proceedings of the National Academy of Sciences of the United States of America
, vol.100
, Issue.25
, pp. 15149-15153
-
-
Buckner, F.1
Yokoyama, K.2
Lockman, J.3
Aikenhead, K.4
Ohkanda, J.5
Sadilek, M.6
Sebti, S.7
Van Voorhis, W.8
Hamilton, A.9
Gelb, M.H.10
-
22
-
-
84880235011
-
VNI cures acute and chronic experimental chagas disease
-
Villalta, F., Dobish, M. C, Nde, P. N., and Kleshchenko., Y. Y., Hargrove, T. Y., Johnson, C A., Waterman, M. R., Johnston, J. N., and Lepesheva, G. I. (2013) VNI cures acute and chronic experimental Chagas disease. J. Infect. Dis. 208, 504-511
-
(2013)
J. Infect. Dis.
, vol.208
, pp. 504-511
-
-
Villalta, F.1
Dobish, M.C.2
Nde, P.N.3
Kleshchenko, Y.Y.4
Hargrove, T.Y.5
Johnson, C.A.6
Waterman, M.R.7
Johnston, J.N.8
Lepesheva, G.I.9
-
23
-
-
0037327813
-
Fatty acid and sterol metabolism: Potential antimicrobial targets in apicomplexan and trypanosomatid parasitic protozoa
-
DOI 10.1016/S0166-6851(02)00280-3, PII S0166685102002803
-
Roberts, C W., McLeod, R., Rice, D. W., Ginger, M., Chance, M. L., and Goad, L. J. (2003) Fatty acid and sterol metabolism: potential antimicrobial targets in apicomplexan and trypanosomatid parasitic protozoa. Mol. Biochem. Parasitol. 126, 129-142 (Pubitemid 36255612)
-
(2003)
Molecular and Biochemical Parasitology
, vol.126
, Issue.2
, pp. 129-142
-
-
Roberts, C.W.1
McLeod, R.2
Rice, D.W.3
Ginger, M.4
Chance, M.L.5
Goad, L.J.6
-
24
-
-
0025114817
-
Ultrastructural alterations induced by two ergosterol biosynthesis inhibitors, ketoconazole and terbinafine, on epimastigotes and amastigotes of Trypanosoma (Schizotrypanum) cruzi
-
Lazardi, K., and Urbina., J. A., and de Souza, W. (1990) Ultrastructural alterations induced by two ergosterol biosynthesis inhibitors, ketoconazole and terbinafine, on epimastigotes and amastigotes of Trypanosoma (Schizotrypanum) cruzi. Antimicrob. Agents Chemother. 34, 2097-2105 (Pubitemid 20373840)
-
(1990)
Antimicrobial Agents and Chemotherapy
, vol.34
, Issue.11
, pp. 2097-2105
-
-
Lazardi, K.1
Urbina, J.A.2
De Souza, W.3
-
25
-
-
77955477571
-
Structural insights into inhibition of sterol 14a-demethylase in the human pathogen trypanosoma cruzi
-
Lepesheva, G. I., and Hargrove., T. Y., Anderson, S., Kleshchenko, Y., Furtak, V., Wawrzak, Z., Villalta, F., and Waterman, M. R. (2010) Structural insights into inhibition of sterol 14a-demethylase in the human pathogen Trypanosoma cruzi. J. Biol. Chem. 285, 25582-25590
-
(2010)
J. Biol. Chem.
, vol.285
, pp. 25582-25590
-
-
Lepesheva, G.I.1
Hargrove, T.Y.2
Anderson, S.3
Kleshchenko, Y.4
Furtak, V.5
Wawrzak, Z.6
Villalta, F.7
Waterman, M.R.8
-
26
-
-
36049032778
-
Sterol 14α-Demethylase as a Potential Target for Antitrypanosomal Therapy: Enzyme Inhibition and Parasite Cell Growth
-
DOI 10.1016/j.chembiol.2007.10.011, PII S1074552107003626
-
Lepesheva, G. I., and Ott., R. D., Hargrove, T. Y., Kleshchenko, Y. Y., Schuster, I., and Nes., W. D., Hill, G. C, Villalta, F., and Waterman, M. R. (2007) Sterol 14a-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth. Chem. Biol. 14, 1283-1293 (Pubitemid 350102245)
-
(2007)
Chemistry and Biology
, vol.14
, Issue.11
, pp. 1283-1293
-
-
Lepesheva, G.I.1
Ott, R.D.2
Hargrove, T.Y.3
Kleshchenko, Y.Y.4
Schuster, I.5
Nes, W.D.6
Hill, G.C.7
Villalta, F.8
Waterman, M.R.9
-
27
-
-
57149132525
-
CYP51: A major drug target in the cytochrome P450 superfamily
-
Lepesheva, G. I., and Hargrove., T. Y., Kleshchenko, Y., Nes, W. D., Villalta, F., and Waterman, M. R. (2008) CYP51: a major drug target in the cytochrome P450 superfamily. Lipids 43, 1117-1125
-
(2008)
Lipids
, vol.43
, pp. 1117-1125
-
-
Lepesheva, G.I.1
Hargrove, T.Y.2
Kleshchenko, Y.3
Nes, W.D.4
Villalta, F.5
Waterman, M.R.6
-
28
-
-
84882301162
-
In vitro and in vivo studies of the antiparasitic activity of sterol 14a-demethylase (CYP51) inhibitor VNI against drug-resistant strains of trypanosoma cruzi
-
Soeiro Mde, N, de Souza, E. M., da Silva, C. F., Batista Dda, G., Batista, M. M., Pavão, B. P., Araújo, J. S., Aiub, C. A., da Silva, P. B., Lionel, J., Britto, C., Kim, K., Sulikowski, G., Hargrove, T. Y., Waterman, M. R., and Lepesheva, G. I. (2013) In vitro and in vivo studies of the antiparasitic activity of sterol 14a-demethylase (CYP51) inhibitor VNI against drug-resistant strains of Trypanosoma cruzi. Antimicrob. Agents Chemother. 57, 4151-4163
-
(2013)
Antimicrob. Agents Chemother.
, vol.57
, pp. 4151-4163
-
-
Soeiro Mde, N.1
De Souza, E.M.2
Da Silva, C.F.3
Batista Dda, G.4
Batista, M.M.5
Pavão, B.P.6
Araújo, J.S.7
Aiub, C.A.8
Da Silva, P.B.9
Lionel, J.10
Britto, C.11
Kim, K.12
Sulikowski, G.13
Hargrove, T.Y.14
Waterman, M.R.15
Lepesheva, G.I.16
-
29
-
-
33645639221
-
CYP51 from Trypanosoma cruzi: A phyla-specific residue in the B′ helix defines substrate preferences of sterol 14α-demethylase
-
DOI 10.1074/jbc.M510317200
-
Lepesheva, G. I., Zaitseva, N G., Nes, W. D., Zhou, W., Arase, M., Liu, J., Hill, G. C, and Waterman, M. R. (2006) CYP51 from Trypanosoma cruzi: a phyla-specific residue in the B' helix defines substrate preferences of sterol 14alpha-demethylase. J. Biol. Chem. 281, 3577-3585 (Pubitemid 43845975)
-
(2006)
Journal of Biological Chemistry
, vol.281
, Issue.6
, pp. 3577-3585
-
-
Lepesheva, G.I.1
Zaitseva, N.G.2
Nes, W.D.3
Zhou, W.4
Arase, M.5
Liu, J.6
Hill, G.C.7
Waterman, M.R.8
-
30
-
-
4143104606
-
CYP51 from Trypanosoma brucei is obtusifoliol-specific
-
DOI 10.1021/bi048967t
-
Lepesheva, G. I., and Nes., W. D., Zhou, W., Hill, G. C, and Waterman, M. R. (2004) CYP51 from Trypanosoma brucei is obtusifoliol-specific. Biochemistry 43, 10789-10799 (Pubitemid 39096721)
-
(2004)
Biochemistry
, vol.43
, Issue.33
, pp. 10789-10799
-
-
Lepesheva, G.I.1
Nes, W.D.2
Zhou, W.3
Hill, G.C.4
Waterman, M.R.5
-
31
-
-
79960662249
-
Substrate preferences and catalytic parameters determined by structural characteristics of sterol 14a-demethylase (CYP51) from leishmania infantum
-
Hargrove, T. Y., Wawrzak, Z., Liu, J., Nes, W. D., and Waterman., M. R., and Lepesheva, G. I. (2011) Substrate preferences and catalytic parameters determined by structural characteristics of sterol 14a-demethylase (CYP51) from Leishmania infantum. J. Biol. Chem. 286, 26838-26848
-
(2011)
J. Biol. Chem.
, vol.286
, pp. 26838-26848
-
-
Hargrove, T.Y.1
Wawrzak, Z.2
Liu, J.3
Nes, W.D.4
Waterman, M.R.5
Lepesheva, G.I.6
-
32
-
-
84862909219
-
Structural complex of sterol 14a-demethylase (CYP51) with 14a-methylenecyclopropyl-A7-24, 25-dihydrolanosterol
-
Hargrove, T. Y., Wawrzak, Z., Liu, J., Waterman, M. R., and Nes., W. D., and Lepesheva, G. I. (2012) Structural complex of sterol 14a-demethylase (CYP51) with 14a-methylenecyclopropyl-A7-24, 25-dihydrolanosterol. J. Lipid Res. 53, 311-320
-
(2012)
J. Lipid Res.
, vol.53
, pp. 311-320
-
-
Hargrove, T.Y.1
Wawrzak, Z.2
Liu, J.3
Waterman, M.R.4
Nes, W.D.5
Lepesheva, G.I.6
-
33
-
-
65649090152
-
Indomethacin amides as a novel molecular scaffold for targeting trypanosoma cruzi sterol 14α-demethylase
-
Konkle, M. E., and Hargrove., T. Y., Kleshchenko, Y. Y., von Kries, J. P., Ridenour, W., Uddin, M. J., Caprioli, R. M., Marnett, L. J., Nes, W. D., Villalta, F., Waterman, M. R., and Lepesheva, G. I. (2009) Indomethacin amides as a novel molecular scaffold for targeting Trypanosoma cruzi sterol 14α-demethylase. J. Med. Chem. 52, 2846-2853
-
(2009)
J. Med. Chem.
, vol.52
, pp. 2846-2853
-
-
Konkle, M.E.1
Hargrove, T.Y.2
Kleshchenko, Y.Y.3
Von Kries, J.P.4
Ridenour, W.5
Uddin, M.J.6
Caprioli, R.M.7
Marnett, L.J.8
Nes, W.D.9
Villalta, F.10
Waterman, M.R.11
Lepesheva, G.I.12
-
34
-
-
84875755952
-
Antitrypanosomal lead discovery: Identification of a ligand-efficient inhibitor of trypanosoma cruzi CYP51 and parasite growth
-
Andriani, G., Amata, E., Beatty, J., Clements, Z., and Coffey., B. J., Courtemanche, G., Devine, W., Erath, J., and Juda., C. E., Wawrzak, Z., Wood, J. T., and Lepesheva., G. I., Rodriguez, A., and Pollastri, M. P. (2013) Antitrypanosomal lead discovery: identification of a ligand-efficient inhibitor of Trypanosoma cruzi CYP51 and parasite growth. J. Med. Chem. 56, 2556-2567
-
(2013)
J. Med. Chem.
, vol.56
, pp. 2556-2567
-
-
Andriani, G.1
Amata, E.2
Beatty, J.3
Clements, Z.4
Coffey, B.J.5
Courtemanche, G.6
Devine, W.7
Erath, J.8
Juda, C.E.9
Wawrzak, Z.10
Wood, J.T.11
Lepesheva, G.I.12
Rodriguez, A.13
Pollastri, M.P.14
-
35
-
-
76249100348
-
Crystal structures of trypanosoma brucei sterol 14a-demethylase and implications for selective treatment of human infections
-
Lepesheva, G. I., and Park., H. W., Hargrove, T. Y., Vanhollebeke, B., Wawrzak, Z., and Harp., J. M., Sundaramoorthy, M., Nes, W. D., Pays, E., Chaudhuri, M., Villalta, F., and Waterman, M. R. (2010) Crystal structures of Trypanosoma brucei sterol 14a-demethylase and implications for selective treatment of human infections. J. Biol. Chem. 285, 1773-1780
-
(2010)
J. Biol. Chem.
, vol.285
, pp. 1773-1780
-
-
Lepesheva, G.I.1
Park, H.W.2
Hargrove, T.Y.3
Vanhollebeke, B.4
Wawrzak, Z.5
Harp, J.M.6
Sundaramoorthy, M.7
Nes, W.D.8
Pays, E.9
Chaudhuri, M.10
Villalta, F.11
Waterman, M.R.12
-
36
-
-
78649446542
-
Structural basis for conservation in the CYP51 family
-
Lepesheva, G. I., and Waterman, M. R. (2011) Structural basis for conservation in the CYP51 family. Biochim. Biophys. Acta 1814, 88-93
-
(2011)
Biochim. Biophys. Acta
, vol.1814
, pp. 88-93
-
-
Lepesheva, G.I.1
Waterman, M.R.2
-
37
-
-
80051697828
-
Sterol 14a-demethylase (CYP51) as a therapeutic target for human trypanosomiasis and leishmaniasis
-
Lepesheva, G. I., and Waterman, M. R. (2011) Sterol 14a-demethylase (CYP51) as a therapeutic target for human trypanosomiasis and leishmaniasis. Curr. Top. Med. Chem. 11, 2060-2071
-
(2011)
Curr. Top. Med. Chem.
, vol.11
, pp. 2060-2071
-
-
Lepesheva, G.I.1
Waterman, M.R.2
-
38
-
-
84861021112
-
Analogues of fenarimol are potent inhibitors of trypanosoma cruzi and are efficacious in a murine model of chagas disease
-
Keenan, M., and Abbott., M. J., Alexander, P. W., Armstrong, T., Best, W. M., Berven, B., Botero, A., Chaplin, J. H., and Charman., S. A., Chatelain, E., von Geldern, T. W., Kerfoot, M., Khong, A., Nguyen, T., McManus, J. D., Morizzi, J., Ryan, E., Scandale, I., Thompson, R. A., Wang, S. Z., and White, K. L. (2012) Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease. J. Med. Chem. 55, 4189-4204
-
(2012)
J. Med. Chem.
, vol.55
, pp. 4189-4204
-
-
Keenan, M.1
Abbott, M.J.2
Alexander, P.W.3
Armstrong, T.4
Best, W.M.5
Berven, B.6
Botero, A.7
Chaplin, J.H.8
Charman, S.A.9
Chatelain, E.10
Von Geldern, T.W.11
Kerfoot, M.12
Khong, A.13
Nguyen, T.14
McManus, J.D.15
Morizzi, J.16
Ryan, E.17
Scandale, I.18
Thompson, R.A.19
Wang, S.Z.20
White, K.L.21
more..
-
39
-
-
84875219457
-
Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of trypanosoma cruzi
-
Keenan, M., and Alexander., P. W., Diao, H, and Best., W. M., Khong, A., Kerfoot, M., Thompson, R. C, White, K. L., and Shackleford., D. M., Ryan, E., Gregg, A. D., and Charman., S. A., von Geldern, T. W., Scandale, I., and Chatelain, E. (2013) Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of Trypanosoma cruzi. Bioorg. Med. Chem. 21, 1756-1763
-
(2013)
Bioorg. Med. Chem.
, vol.21
, pp. 1756-1763
-
-
Keenan, M.1
Alexander, P.W.2
Diao, H.3
Best, W.M.4
Khong, A.5
Kerfoot, M.6
Thompson, R.C.7
White, K.L.8
Shackleford, D.M.9
Ryan, E.10
Gregg, A.D.11
Charman, S.A.12
Von Geldern, T.W.13
Scandale, I.14
Chatelain, E.15
-
40
-
-
0029861640
-
Efficient technique for screening drugs for activity against Trypanosoma cruzi using parasites expressing β-galactosidase
-
Buckner, F. S., and Verlinde., C. L., La Flamme, A. C, and Van Voorhis, W. C. (1996) Efficient technique for screening drugs for activity against Trypanosoma cruzi using parasites expressing β-galactosidase. Antimicrob. Agents Chemother. 40, 2592-2597 (Pubitemid 26367650)
-
(1996)
Antimicrobial Agents and Chemotherapy
, vol.40
, Issue.11
, pp. 2592-2597
-
-
Buckner, F.S.1
Verlinde, C.L.M.J.2
La Flamme, A.C.3
Van Voorhis, W.C.4
-
41
-
-
0041664878
-
Conservation in the CYP51 family. Role of the B′ helix/BC loop and helices F and G in enzymatic function
-
DOI 10.1021/bi034663f
-
Lepesheva, G. I., Virus, C, and Waterman, M. R. (2003) Conservation in the CYP51 family. Role of the B' helix/BC loop and helices F and G in enzymatic function. Biochemistry 42, 9091-9101 (Pubitemid 36935417)
-
(2003)
Biochemistry
, vol.42
, Issue.30
, pp. 9091-9101
-
-
Lepesheva, G.I.1
Virus, C.2
Waterman, M.R.3
-
42
-
-
78651165715
-
The carbon monoxide-binding pigment of liver microsomes. I. Evidence for its hemoprotein nature
-
Omura, T., and Sato, R. (1964) The carbon monoxide-binding pigment of liver microsomes. I. Evidence for its hemoprotein nature. J. Biol. Chem. 239, 2370-2378
-
(1964)
J. Biol. Chem.
, vol.239
, pp. 2370-2378
-
-
Omura, T.1
Sato, R.2
-
43
-
-
84861723942
-
Unusual spectroscopic and ligand binding properties of the cytochrome P450-flavodoxin fusion enzyme XplA
-
Bui, S. H, McLean, K. J., and Cheesman., M. R., Bradley, J. M., Rigby, S. E., and Levy., C. W., Leys, D., and Munro, A. W. (2012) Unusual spectroscopic and ligand binding properties of the cytochrome P450-flavodoxin fusion enzyme XplA. J. Biol. Chem. 287, 19699-19714
-
(2012)
J. Biol. Chem.
, vol.287
, pp. 19699-19714
-
-
Bui, S.H.1
McLean, K.J.2
Cheesman, M.R.3
Bradley, J.M.4
Rigby, S.E.5
Levy, C.W.6
Leys, D.7
Munro, A.W.8
-
44
-
-
33644874235
-
The integration of macromolecular diffraction data
-
Leslie, A. (2006) The integration of macromolecular diffraction data. Acta Crystallogr. D Biol. Crystallogr. 62, 48-57
-
(2006)
Acta Crystallogr. D Biol. Crystallogr.
, vol.62
, pp. 48-57
-
-
Leslie, A.1
-
45
-
-
0028103275
-
The CCP4 suite: Programs for protein crystallography
-
Collaborative Computational Project, Number 4
-
Collaborative Computational Project, Number 4 (1994) The CCP4 suite: programs for protein crystallography. Acta Crystallogr. D Biol. Crystallogr. 50, 760-763
-
(1994)
Acta Crystallogr. D Biol. Crystallogr.
, vol.50
, pp. 760-763
-
-
-
46
-
-
77949535720
-
Features and development of coot
-
Emsley, P., Lohkamp, B., Scott, W. G., and Cowtan, K. (2010) Features and development of Coot. Acta Crystallogr. D Biol. Crystallogr. 66, 486-501
-
(2010)
Acta Crystallogr. D Biol. Crystallogr.
, vol.66
, pp. 486-501
-
-
Emsley, P.1
Lohkamp, B.2
Scott, W.G.3
Cowtan, K.4
-
47
-
-
16644364842
-
REFMAC5 dictionary: Organisation of prior chemical knowledge and guidelines for its use
-
Vagin, A. A., and Steiner., R. S., Lebedev, A. A., Potterton, L., McNicholas, S., Long, F., and Murshudov, G. N. (2004) REFMAC5 dictionary: organisation of prior chemical knowledge and guidelines for its use. Acta Crystallogr. D Biol. Crystallogr. 60, 2284-2295
-
(2004)
Acta Crystallogr. D Biol. Crystallogr.
, vol.60
, pp. 2284-2295
-
-
Vagin, A.A.1
Steiner, R.S.2
Lebedev, A.A.3
Potterton, L.4
McNicholas, S.5
Long, F.6
Murshudov, G.N.7
-
48
-
-
33645050104
-
Cytochrome P450s and other enzymes in drug metabolism and toxicity
-
Guengerich, F. P. (2006) Cytochrome P450s and other enzymes in drug metabolism and toxicity. AAPS J. 8, E101-E111
-
(2006)
AAPS J.
, vol.8
-
-
Guengerich, F.P.1
-
49
-
-
0035958915
-
Folding requirements are different between sterol 14α-demethylase (CYP51) from mycobacterium tuberculosis and human or fungal orthologs
-
Lepesheva, G. I., and Podust., L. M., Bellamine, A., and Waterman, M. R. (2001) Folding requirements are different between sterol 14α-demethylase (CYP51) from Mycobacterium tuberculosis and human or fungal orthologs. J. Biol. Chem. 276, 28413-28420
-
(2001)
J. Biol. Chem.
, vol.276
, pp. 28413-28420
-
-
Lepesheva, G.I.1
Podust, L.M.2
Bellamine, A.3
Waterman, M.R.4
-
50
-
-
84863811756
-
CYP51 structures and structure-based development of novel, pathogen-specific inhibitory scaffolds
-
Hargrove, T. Y., Kim, K., de Nazaré Correia Soeiro, M., da Silva, C. F., Batista, D. D., Batista, M. M., Yazlovitskaya, E. M., Waterman, M. R., Sulikowski, G.A., and Lepesheva, G.I. (2012) CYP51 structures and structure-based development of novel, pathogen-specific inhibitory scaffolds. Int. J. Parasitol. Drugs Drug Resist. 2, 178-186
-
(2012)
Int. J. Parasitol. Drugs Drug Resist.
, vol.2
, pp. 178-186
-
-
Hargrove, T.Y.1
Kim, K.2
De Nazaré Correia Soeiro, M.3
Da Silva, C.F.4
Batista, D.D.5
Batista, M.M.6
Yazlovitskaya, E.M.7
Waterman, M.R.8
Sulikowski, G.A.9
Lepesheva, G.I.10
-
51
-
-
84892244187
-
Inhibition of cytochrome P450 enzymes
-
(Ortiz de Montellano, P. R., ed) Plenum Publishing Corp., New York
-
Correia, M. A., and Ortiz de Montellano, P. R. (2005) Inhibition of cytochrome P450 enzymes, in Cytochrome P450: Structure, Mechanism, and Biochemistry (Ortiz de Montellano, P. R., ed) pp. 246-322, Plenum Publishing Corp., New York
-
(2005)
Cytochrome P450: Structure, Mechanism, and Biochemistry
, pp. 246-322
-
-
Correia, M.A.1
Ortiz De Montellano, P.R.2
-
52
-
-
0036176695
-
Inhibition of cytochromes P450 by antifungal imidazole derivatives
-
DOI 10.1124/dmd.30.3.314
-
Zhang, W., Ramamoorthy, Y., Kilicarslan, T., Nolte, H., and Tyndale., R. F., and Sellers, E. M. (2002) Inhibition of cytochromes P450 by antifungal imidazole derivatives. Drug. Metab. Dispos. 30, 314-318 (Pubitemid 34175023)
-
(2002)
Drug Metabolism and Disposition
, vol.30
, Issue.3
, pp. 314-318
-
-
Zhang, W.1
Ramamoorthy, Y.2
Kilicarslan, T.3
Nolte, H.4
Tyndale, R.F.5
Sellers, E.M.6
-
53
-
-
29244447987
-
The utility of in vitro cytochrome P450 inhibition data in the prediction of drug-drug interactions
-
DOI 10.1124/jpet.105.093229
-
Obach, R. S., and Walsky., R. L., Venkatakrishnan, K., Gaman, E. A., and Houston., J. B., and Tremaine, L. M. (2006) The utility of in vitro cytochrome P450 inhibition data in the prediction of drug-drug interactions. J. Pharmacol. Exp. Ther. 316, 336-348 (Pubitemid 41832613)
-
(2006)
Journal of Pharmacology and Experimental Therapeutics
, vol.316
, Issue.1
, pp. 336-348
-
-
Obach, R.S.1
Walsky, R.L.2
Venkatakrishnan, K.3
Gaman, E.A.4
Houston, J.B.5
Tremaine, L.M.6
-
54
-
-
34548394436
-
Inhibition of cytochromes P450: Existing and new promising therapeutic targets
-
DOI 10.1080/03602530701498455, PII 781827648
-
Schuster, I., and Bernhardt, R. (2007) Inhibition of cytochromes P450: existing and new promising therapeutic targets. Drug. Metab. Rev. 39, 481-499 (Pubitemid 47355725)
-
(2007)
Drug Metabolism Reviews
, vol.39
, Issue.2-3
, pp. 481-499
-
-
Schuster, I.1
Bernhardt, R.2
-
55
-
-
77954627675
-
Azole antimycotics and drug interactions in the perioperative period
-
Saari, T. I., and Olkkola, K. T. (2010) Azole antimycotics and drug interactions in the perioperative period. Curr. Opin. Anaesthesiol. 23, 441-448
-
(2010)
Curr. Opin. Anaesthesiol.
, vol.23
, pp. 441-448
-
-
Saari, T.I.1
Olkkola, K.T.2
-
56
-
-
80054724621
-
Triazole antifungal agents drug-drug interactions involving hepatic cytochrome P450
-
Gubbins, P. O. (2011) Triazole antifungal agents drug-drug interactions involving hepatic cytochrome P450. Expert Opin. Drug. Metab. Toxicol. 7, 1411-1429
-
(2011)
Expert Opin. Drug. Metab. Toxicol.
, vol.7
, pp. 1411-1429
-
-
Gubbins, P.O.1
-
57
-
-
84879070955
-
Antifungal azoles: Structural insights into undesired tight binding to cholesterol-metabolizing CYP46A1
-
Mast, N., Zheng, W., Stout, C. D., and Pikuleva, I. A. (2013) Antifungal azoles: structural insights into undesired tight binding to cholesterol- metabolizing CYP46A1. Mol. Pharmacol. 84, 86-94
-
(2013)
Mol. Pharmacol.
, vol.84
, pp. 86-94
-
-
Mast, N.1
Zheng, W.2
Stout, C.D.3
Pikuleva, I.A.4
-
58
-
-
39349086422
-
Resistance to antifungal agents: Mechanisms and clinical impact
-
DOI 10.1086/524071
-
Kanafani, Z. A., and Perfect, J. R. (2008) Resistance to antifungal agents: mechanisms and clinical impact. Clin. Infect. Dis. 46, 120-128 (Pubitemid 351263573)
-
(2008)
Clinical Infectious Diseases
, vol.46
, Issue.1
, pp. 120-128
-
-
Kanafani, Z.A.1
Perfect, J.R.2
-
59
-
-
44849143048
-
Mechanisms of resistance to antifungal agents: Yeasts and filamentous fungi
-
Espinel-Ingroff, A. (2008) Mechanisms of resistance to antifungal agents: yeasts and filamentous fungi. Rev. Iberoam. Micol. 25, 101-106 (Pubitemid 351798337)
-
(2008)
Revista Iberoamericana de Micologia
, vol.25
, Issue.2
, pp. 101-106
-
-
Espinel-Ingroff, A.1
-
60
-
-
84871585821
-
Organocatalytic, enantioselective synthesis of VNI: A robust therapeutic development platform for chagas, a neglected tropical disease
-
Dobish, M. C., Villalta, F., Waterman, M. R., and Lepesheva., G. I., and Johnston, J. N. (2012) Organocatalytic, enantioselective synthesis of VNI: a robust therapeutic development platform for Chagas, a neglected tropical disease. Org. Lett. 14, 6322-6325
-
(2012)
Org. Lett.
, vol.14
, pp. 6322-6325
-
-
Dobish, M.C.1
Villalta, F.2
Waterman, M.R.3
Lepesheva, G.I.4
Johnston, J.N.5
-
61
-
-
77950023120
-
Structural basis of human CYP51 inhibition by antifungal azoles
-
Strushkevich, N., and Usanov., S. A., and Park, H. W. (2010) Structural basis of human CYP51 inhibition by antifungal azoles. J. Mol. Biol. 397, 1067-1078
-
(2010)
J. Mol. Biol.
, vol.397
, pp. 1067-1078
-
-
Strushkevich, N.1
Usanov, S.A.2
Park, H.W.3
|