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Table 3 Chemosensitizers inhibiting Pgp, MRP and BCRP

From: ABC transporters as multidrug resistance mechanisms and the development of chemosensitizers for their reversal

Name Year Chemosensitizer
Pgp 2004 Benzyl-, phenethyl-, and alpha-naphthyl isothiocyanates [16], diallyl sulfide [17], PK11195 [18], small scFv recombinant Pgp antibody fragment [19]
2003 Amooranin [20], etrandrine, fangchinoline [21], ginsenoside Rg(3) [22], KR30031 [23], methylenedioxyethylamphetamine [24], protopanaxatriol ginsenosides [25], saquinavir [26], siRNA of mdr1 gene [27, 28], tRA 98006* [29]
2002 3,5-dibenzoyl-1,4-dihydropyridines[30], PKC412 [31], pyronaridine [32], sinensetin [33]
2001 Agosterol A [34], haloperidol and dihydrohaloperidol [35], SB203580 [36], tropane alkaloid esters [37], SNF4435C and D [38], tea polyphenol [39], trans-N,N'-bis(3,4-dimethoxybenzyl)-N-solanesyl-1,2-diaminocyclo hexane (N-5228) [40]
2000 Astemizole [41], atorvastatin [42], 7-O-benzoylpyripyropene A [43], 5-O-benzoylated taxinine k [44], clarithromycin and YM17K (3,4'-dideoxy mycaminosyl tylonolide hydrochloride) [45], cyclopamine and tomatidine[46], 3,5-diacetyl-1,4-dihydropyridines [47], 7, 8-dihydroxy-3-benzazepine [48], doxorubicin-gallium-transferrin conjugate [49], macrolide antibiotics (josamycin, tamolarizine) [50], nelfinavir [51] norverapamil [52], ontogen (ONT-093, formerly OC-144-093) [53], R101933 [54], taxuspine C, 2'-desacetoxyaustrospicatine and 2-desacetoxytaxinine [55], V-104 [56]
1999 D-alpha-tocopheryl polyethylene glycol 1000 succinate [57], anti-MDR1 ribozymes [58], AR-2 [59], carvedilol [60], erythromycin [61], ketoconazole [62], kopsiflorine [63], nomegestrol [64], PAK-200S [65], pluronic block copolymer [66], reversin [67], ritonarvir [68], rosemary extract [69], TTD [70], XR9576(2) [71]
1998 Ardeemins [72], AV200 [73], 5-O-benzoylated taxuspine C [74], bromocriptine [75], dipyridamole [76], droloxifene [77], imidazothiazole derivatives (N276-12, N276-14, N276-17) [78], oxalyl bis(N-phenyl)hydroxamic acid [79], tetrandine and fangchinoline [21], tiamulin [80], XR9051 [81]
1997 Biricodar (VX-710; Incel) [82, 83], cyproheptadine [84]
1996 CL 329,753 [85], indole-3-carbinol [86], itraconazole [87], LY335979 [88], medroxyprogesterone [89], mefloquine [90], mifepristone (RU-486) [91], reserpine [92]
1995 Azelastine and flezelastine [93], B9209-005 [94], dexniguldipine (B8509-035) [95], dexverapamil [96], epidermal growth factor (EGF), insulin-like growth factor I (IGF-I) [97], quercetin [98]
1994 MS-209 [99], pentoxifylline [100], Ro11-2933 (DMDP) [101], RU486 [102]
1993 Dilantin [103], GF120918[104], meperidine, pentazocine, and methadone [105], Pgp monoclonal antibodies and antisense oligonucleotide [106], tamoxifen and toremifene [107]
1992 Staurosporine and NA-382 [108]
1991 Biperidil [109], SDZ PSC 833[110]
1990 Cremophor EL [111]
1989 Cefoperazone, cetriaxone [112], phenothiazine [113], YM534 [114]
1987 Diltiazem[115], cyclosporine A [116]
1986 Aamiodarone [117]
1984 Quinidine [118]
1981 Verapamil [119],
MRP 2004 benzyl-, phenethyl-, and alpha-naphthyl isothiocyanates [16]
2003 tRA 98006 [29]
2001 Agosterol A [34]
2000 5-O-benzoylated taxinine k [44], 4-deacetoxyagosterol A [120], doxorubicin-gallium-transferrin conjugate [49], V-104 [56], pluronic block copolymer [66], quinoline-based drugs (chloroquine, quinine, quinidine, and primaquine) [121],
1999 dipyridamole [122], erythromycin and ofloxacin [123], mifepristone (RU-486) [124], MS-209 [125], rifampicin [126]
1998 Biricodar (VX-710; Incel) [83], imidazothiazole derivatives (N276-12, N276-14, N276-17) [78], NSAIDs (indomethacin, sulindac, tolmetin, acemetacin, zomepirac and mefenamic acid) [127], ONO-1078 [128], quercetin [98]
1997 Indomethacin [129], probenecid [130]
1996 Acrolein and chloroacetaldehyde [131], d,l-buthionine-(S,R)-sulfoximine [132], itraconazol [87], PAK-104P [133]
1995 Difloxacin [134], MK571 [135]
BCRP 2004 Chrysin and biochanin A [136], genistein and naligenin [137], Imatinib mesylate (Gleevec, STI571) [138]
2003 Estrone, diethylstilbestrol and TAG-139 [139], tRA 98006 [29]
2002 Ko143 [140]
1999 GF120918 [141]
1998 fumitremorgin C [142]
  1. * Boldface compounds indicate chemosensitizers inhibiting more than two transporters