Reversal of resistance in multidrug resistance protein (MRP1)- overexpressing cells by LY329146

Bioorganic and Medicinal Chemistry Letters

Volumn 9, Issue 23, 1999, Pages 3381-3386

  Norman, Bryan H ^a   Dantzig, Anne H ^a   Kroin, Julian S ^a   Law, Kevin L ^a   Tabas, Linda B ^a   Shepard, Robert L ^a   Palkowitz, Alan D ^a   Hauser, Kenneth L ^a   Winter, Mark A ^a   Sluka, James P ^a   Starling, James J ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BENZOTHIOPHENE DERIVATIVE; DOXORUBICIN; LY 329146; MULTIDRUG RESISTANCE PROTEIN; RALOXIFENE; UNCLASSIFIED DRUG; VINCRISTINE;

ARTICLE; DRUG BINDING; DRUG MECHANISM; DRUG POTENCY; DRUG STRUCTURE; GENE OVEREXPRESSION; HUMAN; HUMAN CELL; STRUCTURE ANALYSIS;

EID: 0033530845     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(99)00610-1     Document Type: Article

References (24)

1. Cole, S. P. C.; Bhardwaj, G.; Gerlach, J. H.; Mackie, J. E.; Grant, C. E.; Almquist, K.C.; Stewart, A. J.; Kurz, E. U.; Duncan, A. M. V.; Deeley, R. G. Science 1992, 258, 1650.
2. Cole, S. P. C.; Sparks, K. E.; Fraser, K.; Loe, D. W.; Grant, C. E.; Wilson, G. M.; Deeley, R. G. Cancer Res. 1994, 54, 5902.
3. Jedlitschky, G.; Leier, I.; Buchholz, U.; Center, M.; Keppler, D. Cancer Res. 1994, 54, 4833.
4. Jedlitschky, G., Leier, I.; Buchholz, U.; Barnouin, K.; Kurz, G.; Keppler, D. Cancer Res. 1996, 56, 988.
5. Loe, D. W.; Almquist, K. C.; Deeley, R. G.; Cole, S. P. C. J. Biol. Chem. 1996, 271, 9675.
6. Loe, D. W.; Almquist, K. C.; Deeley, R. G.; Cole, S. P. C. J. Biol. Chem. 1996, 271, 9683.
7. Leier, I.; Jedlitschky, G.; Buchholz, U.; Cole, S. P. C.; Deeley, R. G.; Keppler., D. Biol. Chem. 1994, 269, 27807.
8. For a recent review of MRP1 inhibitors, see Norman, B. H. Drugs Fut. 1998, 23, 1001.
9. Gekeler, V.; Ise, W.; Sanders, K. H.; Ulrich, W.; Beck, J. Biochem. Biophys. Res. Commun. 1995, 208, 345.
10. Experimental procedures for all assays have been described previously. See Ref. 2 for cellular chemo-sensitivity and reversal studies. See Ref. 3 for inhibition of membrane transport studies. See Ref. 19 for equilibrium binding displacement studies. Additionally, it should be pointed out that experiments were typically performed in duplicate, therefore appropriate statistical analysis is not possible. The use of standards in these experiments, however, indicates that the numbers are accurate to within 20%.
11. Kauffman, R. F.; Bryant, H. U. Drug News Perspect. 1995, 8, 531.
12. Jones, C. D.; Jevniker, M. G.; Pike, A. J.; Peters, M. K.; Black, L. J.; Thompson, A. R.; Falcone, J. F.; Clemens, J. A. J. Med. Chem. 1984, 27, 1057.
13. Delmas, P. D.; Bjarnason, N. H.; Mitlak, B. H.; Ravoux, A.; Shah, A. S.; Huster, W. J.; Draper, M.; Christiansen, C. N. Engl. J. Med. 1997, 337, 1641.
14. Glasebrook, A. L.; Phillips, D. L.; Sluka, J. P. J. Bone Miner. Res. 1993, 8 (Suppl. 1), S268.
15. Grese, T. A.; Cho, S.; Finley, D. R.; Godfrey, A. G.; Jones, C. D.; Luger, C. W.; Martin, M. J.; Matsumoto, K.; Pennington, L. D.; Winter, M. A.; Adrian, M. D.; Cole, H. W.; Magee, D. E.; Phillips, D. L.; Rowley, E. R.; Short, L. L.; Glasebrook, A. L.; Bryant, H. U. J. Med. Chem. 1997, 40, 146.
16. LY117018 and LY329146 were prepared using chemistry outlined in Ref. 14.
17. Grese, T. A., J. P. Sluka, J. P.; H. U. Bryant, H. U.; G. J. Cullinan, G. J.; A. L. Glasebrook, A. L.;C. D. Jones, C. D.; Matsumoto, K.; Palkowitz, A. D.; Sato, M.; Termine, J. D.; Winter, M. A.; Yang, N. N.; Dodge, J. A. Proc. Natl. Acad. Sci USA 1997, 94, 14105.
18. Norman, B. H.; Dantzig, A.; Hauser, K.; Kroin, J.; Law, K; Palkowitz, A.; Shepard, R.; Sluka, J.; Starling, J.; Tabas, L.; Winter, M. Proc. Am. Assoc. Cancer Res. 1997, 38, 2949.
19. Dantzig, A. H.; Shepard, R. L.; Cao, J.; Law, K. L.; Ehlhardt, W. J.; Baughman, T, M.; Bumol, T. F.; Starling, J. J. Cancer Res. 1996, 56, 4171.
20. Grant, C. E.; Valdimarsson, G.; Hipfner, D. R.; Almquist, K. C.; Cole, S. P. C.; Deeley, R. G. Cancer Res. 1994, 54, 357.
21. Germann, U. A.; Ford, P. J.; Shlyakhter, D.; Mason, V. S.; Harding, M. W. Anti-cancer Drugs 1997, 8, 141.
22. Keppler, D.; Konig, J. FASEB J. 1997, 11, 509.
23. i = 0.6 μM (see ref. 7).
24. The overlay was calculated using a least squares technique using Insight-II (version 95.0.4, Molecular Simulations Inc., San Diego) from the x-ray crystal structures of raloxifene and estradiol.