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In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.

Mast N, Verwilst P, Wilkey CJ, Guengerich FP, Pikuleva IA.

J Med Chem. 2019 Nov 3. doi: 10.1021/acs.jmedchem.9b01383. [Epub ahead of print]


The key genes, phosphoproteins, processes, and pathways affected by efavirenz-activated CYP46A1 in the amyloid-decreasing paradigm of efavirenz treatment.

Petrov AM, Mast N, Li Y, Pikuleva IA.

FASEB J. 2019 Aug;33(8):8782-8798. doi: 10.1096/fj.201900092R. Epub 2019 May 7.


CYP46A1 Activation by Efavirenz Leads to Behavioral Improvement without Significant Changes in Amyloid Plaque Load in the Brain of 5XFAD Mice.

Petrov AM, Lam M, Mast N, Moon J, Li Y, Maxfield E, Pikuleva IA.

Neurotherapeutics. 2019 Jul;16(3):710-724. doi: 10.1007/s13311-019-00737-0.


Cholesterol 24-Hydroxylation by CYP46A1: Benefits of Modulation for Brain Diseases.

Petrov AM, Pikuleva IA.

Neurotherapeutics. 2019 Jul;16(3):635-648. doi: 10.1007/s13311-019-00731-6. Review.


Retinal Vascular Abnormalities and Microglia Activation in Mice with Deficiency in Cytochrome P450 46A1-Mediated Cholesterol Removal.

Saadane A, Mast N, Trichonas G, Chakraborty D, Hammer S, Busik JV, Grant MB, Pikuleva IA.

Am J Pathol. 2019 Feb;189(2):405-425. doi: 10.1016/j.ajpath.2018.10.013. Epub 2018 Nov 16.


Mechanisms that minimize retinal impact of apolipoprotein E absence.

Saadane A, Petrov A, Mast N, El-Darzi N, Dao T, Alnemri A, Song Y, Dunaief JL, Pikuleva IA.

J Lipid Res. 2018 Dec;59(12):2368-2382. doi: 10.1194/jlr.M090043. Epub 2018 Oct 17.


Retinal Cholesterol Content Is Reduced in Simvastatin-Treated Mice Due to Inhibited Local Biosynthesis Albeit Increased Uptake of Serum Cholesterol.

Mast N, Bederman IR, Pikuleva IA.

Drug Metab Dispos. 2018 Nov;46(11):1528-1537. doi: 10.1124/dmd.118.083345. Epub 2018 Aug 16.


N,N-Dimethyl-3β-hydroxycholenamide Reduces Retinal Cholesterol via Partial Inhibition of Retinal Cholesterol Biosynthesis Rather Than its Liver X Receptor Transcriptional Activity.

El-Darzi N, Astafev A, Mast N, Saadane A, Lam M, Pikuleva IA.

Front Pharmacol. 2018 Jul 25;9:827. doi: 10.3389/fphar.2018.00827. eCollection 2018.


Drugs and Scaffold That Inhibit Cytochrome P450 27A1 In Vitro and In Vivo.

Lam M, Mast N, Pikuleva IA.

Mol Pharmacol. 2018 Feb;93(2):101-108. doi: 10.1124/mol.117.110742. Epub 2017 Nov 30.


Transcriptional and post-translational changes in the brain of mice deficient in cholesterol removal mediated by cytochrome P450 46A1 (CYP46A1).

Mast N, Lin JB, Anderson KW, Bjorkhem I, Pikuleva IA.

PLoS One. 2017 Oct 26;12(10):e0187168. doi: 10.1371/journal.pone.0187168. eCollection 2017. Erratum in: PLoS One. 2018 Jan 5;13(1):e0191058.


Cholesterol-metabolizing enzyme cytochrome P450 46A1 as a pharmacologic target for Alzheimer's disease.

Mast N, Saadane A, Valencia-Olvera A, Constans J, Maxfield E, Arakawa H, Li Y, Landreth G, Pikuleva IA.

Neuropharmacology. 2017 Sep 1;123:465-476. doi: 10.1016/j.neuropharm.2017.06.026. Epub 2017 Jun 24.


In vitro cytochrome P450 46A1 (CYP46A1) activation by neuroactive compounds.

Mast N, Anderson KW, Johnson KM, Phan TTN, Guengerich FP, Pikuleva IA.

J Biol Chem. 2017 Aug 4;292(31):12934-12946. doi: 10.1074/jbc.M117.794909. Epub 2017 Jun 22.


Cytochrome P450 27A1 Deficiency and Regional Differences in Brain Sterol Metabolism Cause Preferential Cholestanol Accumulation in the Cerebellum.

Mast N, Anderson KW, Lin JB, Li Y, Turko IV, Tatsuoka C, Bjorkhem I, Pikuleva IA.

J Biol Chem. 2017 Mar 24;292(12):4913-4924. doi: 10.1074/jbc.M116.774760. Epub 2017 Feb 11.


On the importance of albumin binding for the flux of 7α-hydroxy-3-oxo-4-cholestenoic acid in the brain.

Saeed AA, Edström E, Pikuleva I, Eggertsen G, Björkhem I.

J Lipid Res. 2017 Feb;58(2):455-459. doi: 10.1194/jlr.P073403. Epub 2016 Dec 12.


Retinal Hypercholesterolemia Triggers Cholesterol Accumulation and Esterification in Photoreceptor Cells.

Saadane A, Mast N, Dao T, Ahmad B, Pikuleva IA.

J Biol Chem. 2016 Sep 23;291(39):20427-39. doi: 10.1074/jbc.M116.744656. Epub 2016 Aug 11.


Mapping of the Allosteric Site in Cholesterol Hydroxylase CYP46A1 for Efavirenz, a Drug That Stimulates Enzyme Activity.

Anderson KW, Mast N, Hudgens JW, Lin JB, Turko IV, Pikuleva IA.

J Biol Chem. 2016 May 27;291(22):11876-86. doi: 10.1074/jbc.M116.723577. Epub 2016 Apr 7.


Cholesterol in mouse retina originates primarily from in situ de novo biosynthesis.

Lin JB, Mast N, Bederman IR, Li Y, Brunengraber H, Björkhem I, Pikuleva IA.

J Lipid Res. 2016 Feb;57(2):258-64. doi: 10.1194/jlr.M064469. Epub 2015 Dec 2.


Cholesterol hydroperoxides as substrates for cholesterol-metabolizing cytochrome P450 enzymes and alternative sources of 25-hydroxycholesterol and other oxysterols.

van Lier JE, Mast N, Pikuleva IA.

Angew Chem Int Ed Engl. 2015 Sep 14;54(38):11138-42. doi: 10.1002/anie.201505002. Epub 2015 Jul 29.


Histone H3 Ser57 and Thr58 phosphorylation in the brain of 5XFAD mice.

Anderson KW, Mast N, Pikuleva IA, Turko IV.

FEBS Open Bio. 2015 Jun 25;5:550-6. doi: 10.1016/j.fob.2015.06.009. eCollection 2015.


Marketed Drugs Can Inhibit Cytochrome P450 27A1, a Potential New Target for Breast Cancer Adjuvant Therapy.

Mast N, Lin JB, Pikuleva IA.

Mol Pharmacol. 2015 Sep;88(3):428-36. doi: 10.1124/mol.115.099598. Epub 2015 Jun 16.


Quantification of histone deacetylase isoforms in human frontal cortex, human retina, and mouse brain.

Anderson KW, Chen J, Wang M, Mast N, Pikuleva IA, Turko IV.

PLoS One. 2015 May 11;10(5):e0126592. doi: 10.1371/journal.pone.0126592. eCollection 2015.


Mass spectrometry detection of isolevuglandin adduction to specific protein residues.

Charvet CD, Pikuleva IA.

Methods Mol Biol. 2015;1208:285-98. doi: 10.1007/978-1-4939-1441-8_21.


Pathways of cholesterol homeostasis in mouse retina responsive to dietary and pharmacologic treatments.

Zheng W, Mast N, Saadane A, Pikuleva IA.

J Lipid Res. 2015 Jan;56(1):81-97. doi: 10.1194/jlr.M053439. Epub 2014 Oct 7.


Retinal and nonocular abnormalities in Cyp27a1(-/-)Cyp46a1(-/-) mice with dysfunctional metabolism of cholesterol.

Saadane A, Mast N, Charvet CD, Omarova S, Zheng W, Huang SS, Kern TS, Peachey NS, Pikuleva IA.

Am J Pathol. 2014 Sep;184(9):2403-19. doi: 10.1016/j.ajpath.2014.05.024. Epub 2014 Jul 25.


Effects of a disrupted blood-brain barrier on cholesterol homeostasis in the brain.

Saeed AA, Genové G, Li T, Lütjohann D, Olin M, Mast N, Pikuleva IA, Crick P, Wang Y, Griffiths W, Betsholtz C, Björkhem I.

J Biol Chem. 2014 Aug 22;289(34):23712-22. doi: 10.1074/jbc.M114.556159. Epub 2014 Jun 27.


Cholesterol in the retina: the best is yet to come.

Pikuleva IA, Curcio CA.

Prog Retin Eye Res. 2014 Jul;41:64-89. doi: 10.1016/j.preteyeres.2014.03.002. Epub 2014 Apr 4. Review.


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.


7α-hydroxy-3-oxo-4-cholestenoic acid in cerebrospinal fluid reflects the integrity of the blood-brain barrier.

Saeed A, Floris F, Andersson U, Pikuleva I, Lövgren-Sandblom A, Bjerke M, Paucar M, Wallin A, Svenningsson P, Björkhem I.

J Lipid Res. 2014 Feb;55(2):313-8. doi: 10.1194/jlr.P044982. Epub 2013 Dec 8.


Pretreatment with pyridoxamine mitigates isolevuglandin-associated retinal effects in mice exposed to bright light.

Charvet CD, Saadane A, Wang M, Salomon RG, Brunengraber H, Turko IV, Pikuleva IA.

J Biol Chem. 2013 Oct 11;288(41):29267-80. doi: 10.1074/jbc.M113.498832. Epub 2013 Aug 22. Erratum in: J Biol Chem. 2013 Nov 22;288(47):34054. Dosage error in article text.


Mass spectrometry quantification of PICALM and AP180 in human frontal cortex and neural retina.

Chen J, Pikuleva IA, Turko IV.

Anal Biochem. 2013 Nov 15;442(2):253-8. doi: 10.1016/j.ab.2013.08.005. Epub 2013 Aug 13.


Cytochromes p450: roles in diseases.

Pikuleva IA, Waterman MR.

J Biol Chem. 2013 Jun 14;288(24):17091-8. doi: 10.1074/jbc.R112.431916. Epub 2013 Apr 30. Review.


Antifungal Azoles: Structural Insights into Undesired Tight Binding to Cholesterol-Metabolizing CYP46A1.

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

Mol Pharmacol. 2013 Jul;84(1):86-94. doi: 10.1124/mol.113.085902. Epub 2013 Apr 19.


Posttranslational modification by an isolevuglandin diminishes activity of the mitochondrial cytochrome P450 27A1.

Charvet CD, Laird J, Xu Y, Salomon RG, Pikuleva IA.

J Lipid Res. 2013 May;54(5):1421-9. doi: 10.1194/jlr.M035790. Epub 2013 Mar 11.


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.


Inhibition and stimulation of activity of purified recombinant CYP11A1 by therapeutic agents.

Mast N, Linger M, Pikuleva IA.

Mol Cell Endocrinol. 2013 May 22;371(1-2):100-6. doi: 10.1016/j.mce.2012.10.013. Epub 2012 Oct 23.


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.


Abnormal vascularization in mouse retina with dysregulated retinal cholesterol homeostasis.

Omarova S, Charvet CD, Reem RE, Mast N, Zheng W, Huang S, Peachey NS, Pikuleva IA.

J Clin Invest. 2012 Aug;122(8):3012-23. doi: 10.1172/JCI63816. Epub 2012 Jul 23.


Spatial distribution of the pathways of cholesterol homeostasis in human retina.

Zheng W, Reem RE, Omarova S, Huang S, DiPatre PL, Charvet CD, Curcio CA, Pikuleva IA.

PLoS One. 2012;7(5):e37926. doi: 10.1371/journal.pone.0037926. Epub 2012 May 22.


Sample prefractionation for mass spectrometry quantification of low-abundance membrane proteins.

Wang M, Heo GY, Omarova S, Pikuleva IA, Turko IV.

Anal Chem. 2012 Jun 19;84(12):5186-91. doi: 10.1021/ac300587v. Epub 2012 May 30.


Features of the retinal environment which affect the activities and product profile of cholesterol-metabolizing cytochromes P450 CYP27A1 and CYP11A1.

Heo GY, Liao WL, Turko IV, Pikuleva IA.

Arch Biochem Biophys. 2012 Feb 15;518(2):119-26. doi: 10.1016/ Epub 2011 Dec 29.


Isolevuglandins and mitochondrial enzymes in the retina: mass spectrometry detection of post-translational modification of sterol-metabolizing CYP27A1.

Charvet C, Liao WL, Heo GY, Laird J, Salomon RG, Turko IV, Pikuleva IA.

J Biol Chem. 2011 Jun 10;286(23):20413-22. doi: 10.1074/jbc.M111.232546. Epub 2011 Apr 15.


Conversion of 7-ketocholesterol to oxysterol metabolites by recombinant CYP27A1 and retinal pigment epithelial cells.

Heo GY, Bederman I, Mast N, Liao WL, Turko IV, Pikuleva IA.

J Lipid Res. 2011 Jun;52(6):1117-27. doi: 10.1194/jlr.M014217. Epub 2011 Mar 16.


Marked accumulation of 27-hydroxycholesterol in the brains of Alzheimer's patients with the Swedish APP 670/671 mutation.

Shafaati M, Marutle A, Pettersson H, Lövgren-Sandblom A, Olin M, Pikuleva I, Winblad B, Nordberg A, Björkhem I.

J Lipid Res. 2011 May;52(5):1004-10. doi: 10.1194/jlr.M014548. Epub 2011 Feb 19.


Structural basis for three-step sequential catalysis by the cholesterol side chain cleavage enzyme CYP11A1.

Mast N, Annalora AJ, Lodowski DT, Palczewski K, Stout CD, Pikuleva IA.

J Biol Chem. 2011 Feb 18;286(7):5607-13. doi: 10.1074/jbc.M110.188433. Epub 2010 Dec 15.


Quantification of cholesterol-metabolizing P450s CYP27A1 and CYP46A1 in neural tissues reveals a lack of enzyme-product correlations in human retina but not human brain.

Liao WL, Heo GY, Dodder NG, Reem RE, Mast N, Huang S, Dipatre PL, Turko IV, Pikuleva IA.

J Proteome Res. 2011 Jan 7;10(1):241-8. doi: 10.1021/pr1008898. Epub 2010 Nov 16.


Structural and biochemical characterization of Mycobacterium tuberculosis CYP142: evidence for multiple cholesterol 27-hydroxylase activities in a human pathogen.

Driscoll MD, McLean KJ, Levy C, Mast N, Pikuleva IA, Lafite P, Rigby SE, Leys D, Munro AW.

J Biol Chem. 2010 Dec 3;285(49):38270-82. doi: 10.1074/jbc.M110.164293. Epub 2010 Sep 30.


Cholestenoic Acid is an important elimination product of cholesterol in the retina: comparison of retinal cholesterol metabolism with that in the brain.

Mast N, Reem R, Bederman I, Huang S, DiPatre PL, Bjorkhem I, Pikuleva IA.

Invest Ophthalmol Vis Sci. 2011 Feb 1;52(1):594-603. doi: 10.1167/iovs.10-6021. Print 2011 Jan.


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.


Marked variability in hepatic expression of cytochromes CYP7A1 and CYP27A1 as compared to cerebral CYP46A1. Lessons from a dietary study with omega 3 fatty acids in hamsters.

Mast N, Shafaati M, Zaman W, Zheng W, Prusak D, Wood T, Ansari GA, Lövgren-Sandblom A, Olin M, Bjorkhem I, Pikuleva I.

Biochim Biophys Acta. 2010 Jun;1801(6):674-81. doi: 10.1016/j.bbalip.2010.03.005. Epub 2010 Mar 16.

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