The mechanisms that control intracellular penetration of the HIV protease inhibitors

被引:36
作者
Hoggard, PG [1 ]
Owen, A [1 ]
机构
[1] Univ Liverpool, Dept Pharmacol & Therapeut, Liverpool L69 3GE, Merseyside, England
关键词
P-glycoprotein; lipophilicity; physiochemical; transport; efflux;
D O I
10.1093/jac/dkg137
中图分类号
R51 [传染病];
学科分类号
100401 ;
摘要
The PIs are a class of drugs whose members show different physiochemical properties. Because of these properties, the PIs have differential accumulations within cells. As the concentration of free drug at its site of action determines its activity, any mechanism that alters this concentration will alter response. It is therefore essential that these mechanisms are investigated further.
引用
收藏
页码:493 / 496
页数:4
相关论文
共 19 条
[1]   α1-acid glycoprotein levels in human immunodeficiency virus-infected subjects on antiretroviral regimens [J].
Boffito, M ;
Sciole, K ;
Raiteri, R ;
Bonora, S ;
Hoggard, PG ;
Back, DJ ;
Di Perri, G .
DRUG METABOLISM AND DISPOSITION, 2002, 30 (07) :859-860
[2]   Kinetic analysis of calcein and calcein -: Acetoxymethylester efflux mediated by the multidrug resistance protein and P-glycoprotein [J].
Essodaïgui, M ;
Broxterman, HJ ;
Garnier-Suillerot, A .
BIOCHEMISTRY, 1998, 37 (08) :2243-2250
[3]   Response to antiretroviral treatment in HIV-1-infected individuals with allelic variants of the multidrug resistance transporter 1: a pharmacogenetics study [J].
Fellay, J ;
Marzolini, C ;
Meaden, ER ;
Back, DJ ;
Buclin, T ;
Chave, JP ;
Decosterd, LA ;
Furrer, H ;
Opravil, M ;
Pantaleo, G ;
Retelska, D ;
Ruiz, L ;
Schinkel, AH ;
Vernazza, P ;
Eap, CB ;
Telenti, A .
LANCET, 2002, 359 (9300) :30-36
[4]  
FORD J, 2003, IN PRESS J IMMUNOLOG
[5]  
Frijters CMG, 1999, J LIPID RES, V40, P1950
[6]  
HOGGARD PG, 2002, 6 INT C DRUG THER HI
[7]  
Huang LY, 2001, DRUG METAB DISPOS, V29, P754
[8]   Multidrug resistance protein 2 (MRP2) transports HIV protease inhibitors, and transport can be enhanced by other drugs [J].
Huisman, MT ;
Smit, JW ;
Crommentuyn, KML ;
Zelcer, N ;
Wiltshire, HR ;
Beijnen, JH ;
Schinkel, AH .
AIDS, 2002, 16 (17) :2295-2301
[9]   Effect of α1-acid glycoprotein on the intracellular accumulation of the HIV protease inhibitors saquinavir, ritonavir and indinavir in vitro [J].
Jones, K ;
Hoggard, PG ;
Khoo, S ;
Maher, B ;
Back, DJ .
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 2001, 51 (01) :99-102
[10]   Differences in the intracellular accumulation of HIV protease inhibitors in vitro and the effect of active transport [J].
Jones, K ;
Hoggard, PG ;
Sales, SD ;
Khoo, S ;
Davey, R ;
Back, DJ .
AIDS, 2001, 15 (06) :675-681