Optimizing the ''Drug-Like'' Properties of Leads in Drug by Ronald T. Borchardt, Edward H. Kerns, Michael J. Hageman, PDF

Pharmacology

By Ronald T. Borchardt, Edward H. Kerns, Michael J. Hageman, Dhrien R. Thakker, James L. Stevens

ISBN-10: 0387340564

ISBN-13: 9780387340562

ISBN-10: 0387449612

ISBN-13: 9780387449616

This publication arises from a workshop prepared by means of the yankee organization of Pharmaceutical Scientists entitled "Optimizing the Drug-Like houses of Leads in Drug Discovery," which happened in Parsippany, NJ in September 2004. The workshop concerned with the optimization of the drug-like houses of leads in drug discovery. the amount outlines recommendations and methodologies designed to lead pharmaceutical and biotechnology businesses in the course of the drug discovery and improvement strategy.

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Sparreboom A, van Asperen J, Mayer U, Schinkel AH, Smit JW, Meijer DK, Borst P, Nooijen WJ, Beijnen JH, and van Tellingen O. Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine. Proc Natl Acad Sci U S A 1997; 94:2031-2035. Speeg KV, Maldonado AL, Liaci J, and Muirhead D. Effect of cyclosporine on colchicine secretion by a liver canalicular transporter studied in vivo. Hepatology 1992; 15:899-903. Thiebaut F, Tsuruo T, Hamada H, Gottesman MM, Pastan I, and Willingham MC.

Sonveaux N, Vigano C, Shapiro AB, Ling V, and Ruysschaert JM. Ligandmediated tertiary structure changes of reconstituted P-glycoprotein. A tryptophan fluorescence quenching analysis. J Biol Chem 1999; 274:1764917654. Sparreboom A, van Asperen J, Mayer U, Schinkel AH, Smit JW, Meijer DK, Borst P, Nooijen WJ, Beijnen JH, and van Tellingen O. Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine. Proc Natl Acad Sci U S A 1997; 94:2031-2035.

Ann Rev Pharmacol Toxicol 2001; 41:535-567 Lin JH and Yamazaki M. Role of P-glycoprotein in Pharmacokinetics: Clinical Implications. Clin Pharmacokinet 2003; 42:59-98 Lee K and Thakker DR. Saturable Transport of H2-Antagonists Ranitidine and Famotidine across Caco-2 Cell Monolayers. J Pharm Sci; 1999:88:680-687 Liu X, Brouwer, KL, Gan LS, Brouwer KR, Stieger B, Meier PJ, Audus KL, and LeCluyse EL. Partial Maintenance of Taurocholate Uptake by Adult Rat Hepatocytes Cultured in a Collagen Sandwich Configuration.

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Optimizing the ''Drug-Like'' Properties of Leads in Drug Discovery by Ronald T. Borchardt, Edward H. Kerns, Michael J. Hageman, Dhrien R. Thakker, James L. Stevens


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