Commentary: Nonspecific protein binding versus membrane partitioning: It is not just semantics

Drug Metabolism and Disposition

Volumn 40, Issue 9, 2012, Pages 1649-1652

  Nagar, Swati ^a   Korzekwa, Ken ^a  

^a TEMPLE UNIVERSITY SCHOOL OF PHARMACY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

DRUG; PROTEIN;

CELL ASSAY; DRUG CONCENTRATION; DRUG DISTRIBUTION; IN VITRO STUDY; IN VIVO STUDY; MEMBRANE BIOLOGY; MEMBRANE PARTITIONING; MEMBRANE PERMEABILITY; NOTE; PRIORITY JOURNAL; PROTEIN BINDING;

ANIMALS; BIOLOGICAL TRANSPORT; CELL MEMBRANE; CELL MEMBRANE PERMEABILITY; DRUG DISCOVERY; ENDOPLASMIC RETICULUM; HUMANS; KINETICS; MEMBRANE PROTEINS; METABOLIC CLEARANCE RATE; MICROSOMES; MODELS, BIOLOGICAL; PHARMACEUTICAL PREPARATIONS; PROTEIN BINDING;

EID: 84865192206     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.112.046599     Document Type: Note

References (36)

1. Abraham MH and Austin RP (2012) The effect of ionized species on microsomal binding. Eur J Med Chem 47:202-205.
2. Agarwal S, Hartz AM, Elmquist WF, and Bauer B (2011) Breast cancer resistance protein and P-glycoprotein in brain cancer: two gatekeepers team up. Curr Pharm Des 17:2793-2802.
3. Alberts B, Johnson A, Lewis J, Raff M, Roberts K, and Walter P (2002) Intracellular compartments and protein sorting, in Molecular Biology of the Cell, pp 659-710, Garland Science, New York.
4. Austin RP, Barton P, Cockroft SL, Wenlock MC, and Riley RJ (2002) The influence of nonspecific microsomal binding on apparent intrinsic clearance, and its prediction from physicochemical properties. Drug Metab Dispos 30:1497-1503. (Pubitemid 35397059)
5. Axelrod J (1955a) The enzymatic conversion of codeine to morphine. J Pharmacol Exp Ther 115:259-267.
6. Axelrod J (1955b) The enzymatic deamination of amphetamine (benzedrine). J Biol Chem 214:753-763.
7. Bickel MH and Steele JW (1974) Binding of basic and acidic drugs to rat tissue subcellular fractions. Chem Biol Interact 8:151-162.
8. Brodie BB, Axelrod J, Cooper JR, Gaudette L, La Du BN, Mitoma C, and Udenfriend S (1955) Detoxication of drugs and other foreign compounds by liver microsomes. Science 121:603-604.
9. Cojocaru V, Winn PJ, and Wade RC (2007) The ins and outs of cytochrome P450s. Biochim Biophys Acta 1770:390-401. (Pubitemid 46136742)
10. De Duve C and Beaufay H (1981) A short history of tissue fractionation. J Cell Biol 91:293s-299s. (Pubitemid 12177874)
11. Ernster L, Siekevitz P, and Palade GE (1962) Enzyme-structure relationships in the endoplasmic reticulum of rat liver: a morphological and biochemical study. J Cell Biol 15:541-562.
12. Fan J, Maeng HJ, and Pang KS (2010) Interplay of transporters and enzymes in the Caco-2 cell monolayer: I. effect of altered apical secretion. Biopharm Drug Dispos 31:215-227.
13. Francesco CD and Bickel MH (1977) Membrane lipids as intracellular binders of chlorpromazine and related drugs. Chem Biol Interact 16:335-346.
14. Gao H, Yao L, Mathieu HW, Zhang Y, Maurer TS, Troutman MD, Scott DO, Ruggeri RB, and Lin J (2008) In silico modeling of nonspecific binding to human liver microsomes. Drug Metab Dispos 36:2130-2135.
15. Giacomini KM, Huang SM, Tweedie DJ, Benet LZ, Brouwer KL, Chu X, Dahlin A, Evers R, Fischer V, Hillgren KM, et al. (2010) Membrane transporters in drug development. Nat Rev Drug Discov 9:215-236.
16. Gottesman MM, Hrycyna CA, Schoenlein PV, Germann UA, and Pastan I (1995) Genetic analysis of the multidrug transporter. Annu Rev Genet 29:607-649. (Pubitemid 26005354)
17. Gottesman MM, Pastan I, Ambudkar SV (1996) P-glycoprotein and multidrug resistance. Curr Opin Genet Dev 6:610-617. (Pubitemid 26372158)
18. Hallifax D and Houston JB (2006) Binding of drugs to hepatic microsomes: comment and assessment of current prediction methodology with recommendation for improvement. Drug Metab Dispos 34:724-726; author reply 727.
19. Hansch C (1969) Quantitative approach to biochemical structure-activity relationships. Acc Chem Res 2:232-239.
20. Hennessy M and Spiers JP (2007) A primer on the mechanics of P-glycoprotein the multidrug transporter. Pharmacol Res 55:1-15. (Pubitemid 46108588)
21. Janmey PA and Kinnunen PK (2006) Biophysical properties of lipids and dynamic membranes. Trends Cell Biol 16:538-546. (Pubitemid 44468385)
22. Kilford PJ, Gertz M, Houston JB, and Galetin A (2008) Hepatocellular binding of drugs: correction for unbound fraction in hepatocyte incubations using microsomal binding or drug lipophilicity data. Drug Metab Dispos 36:1194-1197. (Pubitemid 351929330)
23. Korzekwa KR, Nagar S, Tucker J, Weiskircher EA, Bhoopathy S, and Hidalgo IJ (2012) Models to predict unbound intracellular drug concentrations in the presence of transporters. Drug Metab Dispos 40:865-876.
24. Lam JL, Okochi H, Huang Y, and Benet LZ (2006) In vitro and in vivo correlation of hepatic transporter effects on erythromycin metabolism: characterizing the importance of transporterenzyme interplay. Drug Metab Dispos 34:1336-1344. (Pubitemid 44079874)
25. Margolis JM and Obach RS (2003) Impact of nonspecific binding to microsomes and phospholipid on the inhibition of cytochrome P4502D6: implications for relating in vitro inhibition data to in vivo drug interactions. Drug Metab Dispos 31:606-611. (Pubitemid 36444170)
26. Minder R, Weder HJ, and Bickel MH (1970) Experimental errors resulting from uptake of lipophilic drugs by soft plastic materials. Biochem Pharmacol 19:2179-2180.
27. Murphy PJ (2008) The evolution of drug metabolism research, in Handbook of Drug Metabolism (Pearson PG and Weinkers LC eds) pp 1-15, Informa HealthCare, New York, NY.
28. Obach RS (1997) Nonspecific binding to microsomes: impact on scale-up of in vitro intrinsic clearance to hepatic clearance as assessed through examination of warfarin, imipramine, and propranolol. Drug Metab Dispos 25:1359-1369.
29. Obach RS (1999) Prediction of human clearance of twenty-nine drugs from hepatic microsomal intrinsic clearance data: an examination of in vitro half-life approach and nonspecific binding to microsomes. Drug Metab Dispos 27:1350-1359.
30. Osterberg T, Svensson M, and Lundahl P (2001) Chromatographic retention of drug molecules on immobilised liposomes prepared from egg phospholipids and from chemically pure phospholipids. Eur J Pharm Sci 12:427-439. (Pubitemid 32166741)
31. Palmgrén JJ, Mönkkönen J, Korjamo T, Hassinen A, and Auriola S (2006) Drug adsorption to plastic containers and retention of drugs in cultured cells under in vitro conditions. Eur J Pharm Biopharm 64:369-378. (Pubitemid 44585210)
32. Riley RJ, McGinnity DF, and Austin RP (2005) A unified model for predicting human hepatic, metabolic clearance from in vitro intrinsic clearance data in hepatocytes and microsomes. Drug Metab Dispos 33:1304-1311. (Pubitemid 41196973)
33. Rowland M and Tozer TN (2010) Membranes and distribution, in Clinical Pharmacokinetics and Pharmacodynamics: Concepts and Applications, pp 73-110, Wolters Kluwer Health/Lippincott William & Wilkins, Philadelphia, PA.
34. Römer J and Bickel MH (1979) Interactions of chlorpromazine and imipramine with artificial membranes investigated by equilibrium dialysis, dual-wavelength photometry, and fluorimetry. Biochem Pharmacol 28:799-805. (Pubitemid 9161476)
35. Smith DA, Allerton C, Kalgutkar AS, Waterbeemd H, Walker DK, Mannhold R, Kubinyi H, and Folkers G (2012) Physicochemistry, in Pharmacokinetics and Metabolism in Drug Design, pp 1-18, John Wiley & Sons, Weinheim, Germany.
36. Tran TH, Von Moltke LL, Venkatakrishnan K, Granda BW, Gibbs MA, Obach RS, Harmatz JS, and Greenblatt DJ (2002) Microsomal protein concentration modifies the apparent inhibitory potency of CYP3A inhibitors. Drug Metab Dispos 30:1441-1445. (Pubitemid 35397052)