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Pharmacologic stimulation of cytochrome P450 46A1 and cerebral cholesterol turnover in mice.

Mast N, Li Y, Linger M, Clark M, Wiseman J, Pikuleva IA.

J Biol Chem. 2014 Feb 7;289(6):3529-38. doi: 10.1074/jbc.M113.532846. Epub 2013 Dec 18.


Structural basis of drug binding to CYP46A1, an enzyme that controls cholesterol turnover in the brain.

Mast N, Charvet C, Pikuleva IA, Stout CD.

J Biol Chem. 2010 Oct 8;285(41):31783-95. doi: 10.1074/jbc.M110.143313. Epub 2010 Jul 28.


The antifungal drug voriconazole is an efficient inhibitor of brain cholesterol 24S-hydroxylase in vitro and in vivo.

Shafaati M, Mast N, Beck O, Nayef R, Heo GY, Björkhem-Bergman L, Lütjohann D, Björkhem I, Pikuleva IA.

J Lipid Res. 2010 Feb;51(2):318-23. doi: 10.1194/jlr.M900174-JLR200. Epub 2009 May 27.


Crystal structures of substrate-bound and substrate-free cytochrome P450 46A1, the principal cholesterol hydroxylase in the brain.

Mast N, White MA, Bjorkhem I, Johnson EF, Stout CD, Pikuleva IA.

Proc Natl Acad Sci U S A. 2008 Jul 15;105(28):9546-51. doi: 10.1073/pnas.0803717105. Epub 2008 Jul 9.


Binding of a cyano- and fluoro-containing drug bicalutamide to cytochrome P450 46A1: unusual features and spectral response.

Mast N, Zheng W, Stout CD, Pikuleva IA.

J Biol Chem. 2013 Feb 15;288(7):4613-24. doi: 10.1074/jbc.M112.438754. Epub 2013 Jan 3.


Combined use of mass spectrometry and heterologous expression for identification of membrane-interacting peptides in cytochrome P450 46A1 and NADPH-cytochrome P450 oxidoreductase.

Mast N, Liao WL, Pikuleva IA, Turko IV.

Arch Biochem Biophys. 2009 Mar 1;483(1):81-9. doi: 10.1016/ Epub 2009 Jan 10.


CYP46A1 variants influence Alzheimer's disease risk and brain cholesterol metabolism.

Kölsch H, Lütjohann D, Jessen F, Popp J, Hentschel F, Kelemen P, Schmitz S, Maier W, Heun R.

Eur Psychiatry. 2009 Apr;24(3):183-90. doi: 10.1016/j.eurpsy.2008.12.005. Epub 2009 Mar 16.


Chromatin-modifying agents increase transcription of CYP46A1, a key player in brain cholesterol elimination.

Milagre I, Nunes MJ, Moutinho M, Rivera I, Fuso A, Scarpa S, Gama MJ, Rodrigues E.

J Alzheimers Dis. 2010;22(4):1209-21. doi: 10.3233/JAD-2010-100651.


In silico and intuitive predictions of CYP46A1 inhibition by marketed drugs with subsequent enzyme crystallization in complex with fluvoxamine.

Mast N, Linger M, Clark M, Wiseman J, Stout CD, Pikuleva IA.

Mol Pharmacol. 2012 Nov;82(5):824-34. doi: 10.1124/mol.112.080424. Epub 2012 Aug 2.


Broad substrate specificity of human cytochrome P450 46A1 which initiates cholesterol degradation in the brain.

Mast N, Norcross R, Andersson U, Shou M, Nakayama K, Bjorkhem I, Pikuleva IA.

Biochemistry. 2003 Dec 9;42(48):14284-92.


Studies on the transcriptional regulation of cholesterol 24-hydroxylase (CYP46A1): marked insensitivity toward different regulatory axes.

Ohyama Y, Meaney S, Heverin M, Ekström L, Brafman A, Shafir M, Andersson U, Olin M, Eggertsen G, Diczfalusy U, Feinstein E, Björkhem I.

J Biol Chem. 2006 Feb 17;281(7):3810-20. Epub 2005 Nov 30.


Knockout of the cholesterol 24-hydroxylase gene in mice reveals a brain-specific mechanism of cholesterol turnover.

Lund EG, Xie C, Kotti T, Turley SD, Dietschy JM, Russell DW.

J Biol Chem. 2003 Jun 20;278(25):22980-8. Epub 2003 Apr 9.


Plasma efavirenz concentrations and the association with CYP2B6-516G >T polymorphism in HIV-infected Thai children.

Puthanakit T, Tanpaiboon P, Aurpibul L, Cressey TR, Sirisanthana V.

Antivir Ther. 2009;14(3):315-20.


Cholesterol-metabolizing cytochromes P450.

Pikuleva IA.

Drug Metab Dispos. 2006 Apr;34(4):513-20. Epub 2006 Jan 24. Review.


Cholesterol 24-hydroxylase: an enzyme of cholesterol turnover in the brain.

Russell DW, Halford RW, Ramirez DM, Shah R, Kotti T.

Annu Rev Biochem. 2009;78:1017-40. doi: 10.1146/annurev.biochem.78.072407.103859. Review.


The influence of tuberculosis treatment on efavirenz clearance in patients co-infected with HIV and tuberculosis.

Gengiah TN, Holford NH, Botha JH, Gray AL, Naidoo K, Abdool Karim SS.

Eur J Clin Pharmacol. 2012 May;68(5):689-95. doi: 10.1007/s00228-011-1166-5. Epub 2011 Nov 23.


Efavirenz in the therapy of HIV infection.

Rakhmanina NY, van den Anker JN.

Expert Opin Drug Metab Toxicol. 2010 Jan;6(1):95-103. doi: 10.1517/17425250903483207. Review.


Non-nucleoside reverse transcriptase inhibitors efavirenz and nevirapine inhibit cytochrome C oxidase in mouse brain regions.

Streck EL, Ferreira GK, Scaini G, Rezin GT, Gonçalves CL, Jeremias IC, Zugno AI, Ferreira GC, Moreira J, Fochesato CM, Romão PR.

Neurochem Res. 2011 Jun;36(6):962-6. doi: 10.1007/s11064-011-0432-3. Epub 2011 Mar 2.


Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid.

Avery LB, VanAusdall JL, Hendrix CW, Bumpus NN.

Drug Metab Dispos. 2013 Feb;41(2):422-9. doi: 10.1124/dmd.112.049601. Epub 2012 Nov 19.


Cholesterol-24S-hydroxylase (CYP46A1) is specifically expressed in neurons of the neural retina.

Bretillon L, Diczfalusy U, Björkhem I, Maire MA, Martine L, Joffre C, Acar N, Bron A, Creuzot-Garcher C.

Curr Eye Res. 2007 Apr;32(4):361-6.

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