Acitretin, an enhancer of alpha-secretase expression, crosses the blood-brain barrier and is not eliminated by P-glycoprotein

Neurodegenerative Diseases

Volumn 10, Issue 1-4, 2012, Pages 224-228

  Holthoewer, David ^a   Endres, Kristina ^a   Schuck, Florian ^a   Hiemke, Christoph ^a   Schmitt, Ulrich ^a   Fahrenholz, Falk ^a  

^a JOHANNES GUTENBERG UNIVERSITY   (Germany)

Author keywords

A disintegrin and metalloproteinase 10; Alzheimer's disease; Blood brain barrier; Clinical trial; P glycoprotein; Retinoids

Indexed keywords

ADAM10 ENDOPEPTIDASE; ETRETIN; GLYCOPROTEIN P; MULTIDRUG RESISTANCE PROTEIN 1; TAMIBAROTENE;

ALZHEIMER DISEASE; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BLOOD BRAIN BARRIER; CELL CULTURE; DRUG DISPOSITION; DRUG DISTRIBUTION; DRUG EFFECT; DRUG ELIMINATION; DRUG PENETRATION; DRUG POTENCY; HUMAN; HUMAN CELL; MALE; MOUSE; NEUROBLASTOMA CELL; NONHUMAN; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN TRANSPORT;

ACITRETIN; ADAM PROTEINS; AMYLOID PRECURSOR PROTEIN SECRETASES; ANALYSIS OF VARIANCE; ANIMALS; BLOOD-BRAIN BARRIER; CELL LINE, TUMOR; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; GENE EXPRESSION REGULATION; HUMANS; MALE; MEMBRANE PROTEINS; MICE; MICE, KNOCKOUT; NEUROBLASTOMA; P-GLYCOPROTEIN; P-GLYCOPROTEINS; TIME FACTORS; TRANSFECTION;

EID: 84860226091     PISSN: 16602854     EISSN: 16602862     Source Type: Journal    
DOI: 10.1159/000334300     Document Type: Article

References (17)

1. Goodman AB, Pardee AB: Evidence for defective retinoid transport and function in late onset Alzheimer's disease. Proc Natl Acad Sci USA 2003; 100: 2901-2905.
2. Goodman AB: Retinoid receptors, transporters, and metabolizers as therapeutic targets in late onset Alzheimer disease. J Cell Physiol 2006; 209: 598-603.
3. Shudo K, Fukasawa H, Nakagomi M, Yamagata N: Towards retinoid therapy for Alzheimer's disease. Curr Alzheimer Res 2009; 6: 302-311.
4. Ono K, Yoshiike Y, Takashima A, Hasegawa K, Naiki H, Yamada M: Vitamin A exhibits potent antiamyloidogenic and fibril-destabilizing effects in vitro. Exp Neurol 2004; 189: 380-392.
5. Prinzen C, Muller U, Endres K, Fahrenholz F, Postina R: Genomic structure and functional characterization of the human ADAM10 promoter. FASEB J 2005; 19: 1522-1524.
6. Tippmann F, Hundt J, Schneider A, Endres K, Fahrenholz F: Up-regulation of the alphasecretase ADAM10 by retinoic acid receptors and acitretin. FASEB J 2009; 23: 1643-1654.
7. Endres K, Fahrenholz F: Upregulation of the alpha-secretase ADAM10 - Risk or reason for hope? FEBS J 2010; 277: 1585-1596.
8. Kagechika H, Kawachi E, Hashimoto Y, Shudo K: New type inducers of differentiation of human HL-60 promyelocytic leukemia cells. Terephthalic anilides. Chem Pharm Bull (Tokyo) 1984; 32: 4209-4212.
9. Umemiya H, Fukasawa H, Ebisawa M, Eyrolles L, Kawachi E, Eisenmann G, Gronemeyer H, Hashimoto Y, Shudo K, Kagechika H: Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers. J Med Chem 1997; 40: 4222-4234.
10. Armstrong JL, Ruiz M, Boddy AV, Redfern CP, Pearson AD, Veal GJ: Increasing the intracellular availability of all-trans retinoic acid in neuroblastoma cells. Br J Cancer 2005; 92: 696-704.
11. Eisenhardt EU, Bickel MH: Kinetics of tissue distribution and elimination of retinoid drugs in the rat. 1I. Acitretin. Drug Metab Dispos 1994; 22: 26-30.
12. Schinkel AH, Mayer U, Wagenaar E, Mol CA, van Deemter L, Smit JJ, van der Valk MA, Voordouw AC, Spits H, van Tellingen O, Zijlmans JM, Fibbe WE, Borst P: Normal viability and altered pharmacokinetics in mice lacking mdr1-type (drug-transporting) P-glycoproteins. Proc Natl Acad Sci USA 1997; 94: 4028-4033.
13. Doran A, Obach RS, Smith BJ, Hosea NA, Becker S, Callegari E, Chen C, Chen X, Choo E, Cianfrogna J, Cox LM, Gibbs JP, Gibbs MA, Hatch H, Hop CE, Kasman IN, Laperle J, Liu J, Liu X, Logman M, Maclin D, Nedza FM, Nelson F, Olson E, Rahematpura S, Raunig D, Rogers S, Schmidt K, Spracklin DK, Szewc M, Troutman M, Tseng E, Tu M, Van Deusen JW, Venkatakrishnan K, Walens G, Wang EQ, Wong D, Yasgar AS, Zhang C: The impact of P-glycoprotein on the disposition of drugs targeted for indications of the central nervous system: evaluation using the MDR1A/1B knockout mouse model. Drug Metab Dispos 2005; 33: 165-174.
14. Kirschbaum KM, Henken S, Hiemke C, Schmitt U: Pharmacodynamic consequences of P-glycoprotein-dependent pharmacokinetics of risperidone and haloperidol in mice. Behav Brain Res 2008; 188: 298-303.
15. Decker MA, Zimmerman CL: Simultaneous determination of etretinate, acitretin and their metabolites in perfusate, perfusate plasma, bile or hepatic tissue with reversedphase high-performance liquid chromatography. J Chromatogr B Biomed Appl 1995; 667: 105-113.
16. Chang C, Bahadduri PM, Polli JE, Swaan PW, Ekins S: Rapid identification of P-glycoprotein substrates and inhibitors. Drug Metab Dispos 2006; 34: 1976-1984.
17. Kirschbaum KM, Uhr M, Holthoewer D, Namendorf C, Pietrzik C, Hiemke C, Schmitt U: Pharmacokinetics of acute and subchronic aripiprazole in P-glycoprotein deficient mice. Neuropharmacology 2010; 59: 474-479.