Alpha-1-acid glycoprotein

F. Bree, G. Houin, J. Barre, J. L. Moretti, V. Wirquin, and J.-P. Tillement, Pharmacokinetics of intravenously administered 125I-labelled human alpha-1-acid glycoprotein, Clin. Pharmacokinet, 11, 336-342 (1986). 

C. G. Gahmberg and L. C. Anderson, Leucocyte surface origin of human alpha-1-acid glycoprotein (oroso-mucoid), J. Exp. Med, 148, 507-521 (1978). 

Chatterjee M, Harris AL (1990) Reversal of acquired resistance to adriamycin in CHO cells by tamoxifen and 4-hydroxy tamoxifen role of drug interaction with alpha 1 acid glycoprotein. Br J Cancer 62(5) 712-717... 

Finally, nucleolin has also been identified as a repressor of polymerase II transcription (Yang et al 1994). Biochemical and functional studies further established that nucleolin is a transcription repressor for regulation of alpha-1 acid glycoprotein (AGP)... 

Pharmacokinetics Ticlopidine is rapidly absorbed (more than 80%), with peak plasma levels occurring at approximately 2 hours after dosing, and is extensively metabolized. Administration after meals results in a 20% increase in the area under the plasma concentration-time curve (AUC). Ticlopidine displays nonlinear pharmacokinetics and clearance decreases markedly on repeated dosing. Ticlopidine binds reversibly (98%) to plasma proteins, mainly to serum albumin and lipoproteins. The binding to albumin and lipoproteins is nonsaturable over a wide concentration range. Ticlopidine also binds to alpha-1 acid glycoprotein at concentrations attained with the recommended dose, 15% or less in plasma is bound to this protein. 

The plasma protein binding of tacrolimus is approximately 99%. Tacrolimus is bound mainly to albumin and alpha-1-acid glycoprotein and has a high level of association with erythrocytes. It is extensively metabolized by the mixed-function oxidase system, primarily the cytochrome P450 system (CYP3A). The disposition of tacrolimus from whole blood was biphasic with a terminal elimination half-life of 11.7 hours in liver transplant patients. 

Abernethy DR, Kertzner L. Age effects on alpha-1-acid glycoprotein concentration and imipramine plasma protein binding. J Am Geriatr Soc 1984 32 705-708. 

Larghero J, Leguay T, Mourah S et al. Relationship between elevated levels of the alpha 1 acid glycoprotein in chronic myelogenous leukemia in blast crisis and pharmacological resistance to imatinib (Gleevec) in vitro and in vivo. Biochem Pharmacol 2003 66 1907-1913. 

Kishino S, Nomura A, Di ZS, Sugawara M, Iseki K, Kakinoki S et al. Alpha-1-acid glycoprotein concentration and the protein binding of disopyramide in healthy subjects. J Clin Pharmacol 1995 35 510-4. 

Nicollet, I., Lebreton, J. P., Fontaine, M., and Hiron, M. (1981) Evidence for alpha-1-acid glycoprotein populauons of different pi values after concanavalin A affinity chromatography. Study of their evoluuon during inflammauon in man. Biochtm. Biophys. Acta 668, 235-245. 

Doyle, M.J. Halsall, H.B. Heineman, W.R. Enzyme-linked immunoasorbent assay with electrochemical detection for alpha-1-acid glycoprotein. Anal. Chem. 1982, 56, 2318-2322. 

Triazolam 0.25-0.50 mg qhs Flepatic 100% 100% 100% Protein binding correlates with alpha-1 acid glycoprotein concentration NC NC No data... 

Brinkman-Van der Linden, C.M., Havenaar, E.C., Van Ommen, C.R., Van Kamp, G.J., Gooren, L.J. and Van Dijk, W. (1996) Oral estrogen treatment induces a decrease in expression of sialyl Lewis x on alpha 1-acid glycoprotein in females and male-to-female transsexuals. Glycobiology, 6,407 142. 

Otagiri M, Maruyama T, Imai T, et al. A comparative study of the interaction of warfarin with human alpha 1-acid glycoprotein and human albumin. J Pharm Pharmacol 1987 39(6) 416-20. 

Vanoss CJ, Gillman CF, Bronson PM, et al. Opsonic properties of human-serum alpha-1 acid glycoprotein. Immunol Commun 1974 3 329-335. 

Alpha-1-acid glycoproteins (220,221), bovine serum albumin (222-224), pepsin, and cellobiohydrolase I (223) have been used as chiral selectors. In general, enantiomeric separation increases with increased protein concentration however, this results in a sensitivity loss due to high background signal. The use of a partial filling technique for the capillary injection to overcome this limitation has been reported (220,221). 

A commercial CE system and a micropacked capillary was used to separate N—, O—, and S-containing heterocyclic compounds. Migration time reproducibility, linearity, and detector response was found to be comparable to HPLC. A study of the heterocyclic compound s elution order followed that predicted by the octanol-water partition coefficients (354). While chiral CEC provides improved resolution and higher efficiencies, additional work is needed since chiral CEC capillaries are not available commercially. The separation principles and chiral recognition mechanism for the separation of enantiomers have been reviewed (355). Furthermore, a comprehensive collection of drug applications and other compounds of interest has been reported (356). Direct enantiomeric separations by CEC were studied using a capillary packed with alpha-1-acid glycoprotein chiral stationary phase (357). Chiral resolution was achieved for enantiomers of benzoin, hexobarbital, pentobarbital, fosfamide, disopyramide, methoprolol, oxprenolol, and propanolol. The effects of pH, electrolyte concentration, and con-... 

H Shiono, A Shibukawa, Y Kuroda, T Nakagawa. Effect of sialic acid residues of human alpha 1-acid glycoprotein on stereoselectivity in basic drug-protein binding. Chirality 9 291-296, 1997. 

Eap, C.B., Cuendet, C., and Baumann, P. Orosomucoid (alpha-1 acid glycoprotein) phenotyping by use of immobilized pH gradients with 8 M urea and immunoblotting. A new variant encountered in a population study. Human Genetics 1988 80 183-185. 

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