Targeted prodrug design to optimize drug delivery

Physiology of the Gastrointestinal Tract

(2006) · Elsevier eBooks · doi:10.1016/b978-0-12-088394-3.x5000-4 · Cited by 4,597

In Vivo Gene Transfer with Retroviral Vector-Producer Cells for Treatment of Experimental Brain Tumors

Culver, K. W., Ram, Z., Wallbridge, S., Ishii, H., Oldfield, E. H., & Blaese, R. M. (1992) · Science · doi:10.1126/science.1317968 · Cited by 1,509

Handbook of Experimental Pharmacology

(1968) · Annals of Internal Medicine · doi:10.7326/0003-4819-68-1-269_2 · Cited by 727

Human Intestinal H+/Peptide Cotransporter

Liang, R., Fei, Y.-J., Prasad, P. D., Ramamoorthy, S., Han, H., Yang-Feng, T. L., Hediger, M. A., Ganapathy, V., & Leibach, F. H. (1995) · Journal of Biological Chemistry · doi:10.1074/jbc.270.12.6456 · Cited by 502

Transfer of the bacterial gene for cytosine deaminase to mammalian cells confers lethal sensitivity to 5-fluorocytosine: a negative selection system.

Mullen, C. A., Kilstrup, M., & Blaese, R. M. (1992) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.89.1.33 · Cited by 497

Chemical Aspects of Selective Toxicity

ALBERT, A. (1958) · Nature · doi:10.1038/182421a0 · Cited by 401

Carrier-Mediated Intestinal Transport of Drugs

Tsuji, A., & Tamai, I. (1996) · Pharmaceutical Research · doi:10.1023/a:1016086003070 · Cited by 392

Peptide Transporters in the Intestine and the Kidney

Leibach, F. H., & Ganapathy, V. (1996) · Annual Review of Nutrition · doi:10.1146/annurev.nu.16.070196.000531 · Cited by 315

Valacyclovir: A Substrate for the Intestinal and Renal Peptide Transporters PEPT1 and PEPT2

Ganapathy, M. E., Huang, W. Y., Wang, H., Ganapathy, V., & Leibach, F. H. (1998) · Biochemical and Biophysical Research Communications · doi:10.1006/bbrc.1998.8628 · Cited by 301

5′-Amino Acid Esters of Antiviral Nucleosides, Acyclovir, and AZT Are Absorbed by the Intestinal PEPT1 Peptide Transporter

Han, H.-K., de Vrueh, R. L. A., Rhie, J. K., Covitz, K.-M. Y., Smith, P. L., Lee, C.-P., Oh, D.-M., Sadee, W., & Amidon1, G. L. (1998) · Pharmaceutical Research · doi:10.1023/a:1011919319810 · Cited by 297

Antibody directed enzymes revive anti-cancer prodrugs concept

Bagshawe, K. (1987) · British Journal of Cancer · doi:10.1038/bjc.1987.237 · Cited by 280

Molecular cloning of PEPT 2, a new member of the H+/peptide cotransporter family, from human kidney

Liu, W., Liang, R., Ramamoorthy, S., Fei, Y.-J., Ganapathy, M. E., Hediger, M. A., Ganapathy, V., & Leibach, F. H. (1995) · Biochimica et Biophysica Acta (BBA) - Biomembranes · doi:10.1016/0005-2736(95)80036-f · Cited by 260

Cloning and characterization of a rat H+/peptide cotransporter mediating absorption of beta-lactam antibiotics in the intestine and kidney.

Saito, H., Okuda, M., Terada, T., Sasaki, S., & Inui, K. (1995) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)12227-1 · Cited by 242

Anti-tumor effects of antibody-alkaline phosphatase conjugates in combination with etoposide phosphate.

Senter, P. D., Saulnier, M. G., Schreiber, G. J., Hirschberg, D. L., Brown, J. P., Hellström, I., & Hellström, K. E. (1988) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.85.13.4842 · Cited by 236

Rationale for Design of Biologically Reversible Drug Derivatives: Prodrugs

Sinkula, A. A., & Yalkowsky, S. H. (1975) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.2600640203 · Cited by 223

The bioactivation of 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB1954)—I

Anlezark, G. M., Melton, R. G., Sherwood, R. F., Coles, B., Friedlos, F., & Knox, R. J. (1992) · Biochemical Pharmacology · doi:10.1016/0006-2952(92)90671-5 · Cited by 214

Direct Evidence for Peptide Transporter (PepT1)-Mediated Uptake of a Nonpeptide Prodrug, Valacyclovir

Balimane, P. V., Tamai, I., Guo, A., Nakanishi, T., Kitada, H., Leibach, F. H., Tsuji, A., & Sinko, P. J. (1998) · Biochemical and Biophysical Research Communications · doi:10.1006/bbrc.1998.9298 · Cited by 214

Prodrugs: Do They Have Advantages in Clinical Practice?

Stella, V. J., Charman, W. N., & Naringrekar, V. H. (1985) · Drugs · doi:10.2165/00003495-198529050-00002 · Cited by 199

Physiology of the Gastrointestinal Tract.

DeLor, C. J. (1969) · Archives of Internal Medicine · doi:10.1001/archinte.1969.00300170121031 · Cited by 189

A colon-specific drug-delivery system based on drug glycosides and the glycosidases of colonic bacteria

Friend, D. R., & Chang, G. W. (1984) · Journal of Medicinal Chemistry · doi:10.1021/jm00369a005 · Cited by 172

Molecular cloning and tissue distribution of rat peptide transporter PEPT2

Saito, H., Terada, T., Okuda, M., Sasaki, S., & Inui, K.-I. (1996) · Biochimica et Biophysica Acta (BBA) - Biomembranes · doi:10.1016/0005-2736(96)00024-7 · Cited by 162

Peptides and Related Drugs: A Review of Their Absorption, Metabolism, and Excretion

Humphrey, M., & Ringrose, P. S. (1986) · Drug Metabolism Reviews · doi:10.3109/03602538608998293 · Cited by 153

Design of prodrugs

Bundgaard, H. (1985) · Elsevier eBooks · Cited by 145

Structural Specificity of Mucosal-Cell Transport and Metabolism of Peptide Drugs: Implication for Oral Peptide Drug Delivery

Bai, J. P. F., & Amidon, G. L. (1992) · Pharmaceutical Research · doi:10.1023/a:1015885823793 · Cited by 145

Cure of Mice bearing Advanced Plasma Cell Tumours with Aniline Mustard : the Relationship between Glucuronidase Activity and Tumour Sensitivity

Connors, T. A., & Whisson, M. E. (1966) · Nature · doi:10.1038/210866b0 · Cited by 142

2,4-Dinitro-5-ethyleneiminobenzamide (CB 1954): A potent and selective inhibitor of the growth of the Walker carcinoma 256

Cobb, L., Connors, T. A., Elson, L. A., Khan, A. H., Mitchley, B. C. V., Ross, W. C. J., & Whisson, M. E. (1969) · Biochemical Pharmacology · doi:10.1016/0006-2952(69)90267-6 · Cited by 133

Thymidine kinase-mediated killing of rat brain tumors

Barba, D., Hardin, J., Ray, J., & Gage, F. H. (1993) · Journal of neurosurgery · doi:10.3171/jns.1993.79.5.0729 · Cited by 132

The First Bagshawe lecture: Towards generating cytotoxic agents at cancer sites

Bagshawe, K. D. (1989) · British Journal of Cancer · doi:10.1038/bjc.1989.270 · Cited by 131

gamma-Glutamyl dopa: a kidney-specific dopamine precursor.

Wilk, S., Mizoguchi, H., & Orłowski, M. (1978) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)31317-0 · Cited by 118

Passive and Carrier-Mediated Intestinal Absorption Components of Two Angiotensin Converting Enzyme (ACE) Inhibitor Prodrugs in Rats: Enalapril and Fosinopril

Friedman, D. I., & Amidon, G. L. (1989) · Pharmaceutical Research · doi:10.1023/a:1015978420797 · Cited by 116

H+ gradient-dependent and carrier-mediated transport of cefixime, a new cephalosporin antibiotic, across brush-border membrane vesicles from rat small intestine.

Tsuji, A., Terasaki, T., Tamai, I., & Hirooka, H. (1987) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-5347(25)00304-0 · Cited by 110

Cellular Uptake Mechanism of Amino Acid Ester Prodrugs in Caco-2/hPEPT1 Cells Overexpressing a Human Peptide Transporter

Han, H.-K., Oh, D.-M., & Amidon, G. L. (1998) · Pharmaceutical Research · doi:10.1023/a:1011945420235 · Cited by 96

Use of the Peptide Carrier System to Improve the Intestinal Absorption of L-α-Methyldopa: Carrier Kinetics, Intestinal Permeabilities, and In Vitro Hydrolysis of Dipeptidyl Derivatives of L-α-Methyldopa

Hu, M., Subramanian, P. K., Mosberg, H. I., & Amidon, G. L. (1989) · Pharmaceutical Research · doi:10.1023/a:1015855820488 · Cited by 91

Transport of l-Valine-Acyclovir Via the Oligopeptide Transporter In The Human Intestinal Cell Line, Caco-2

de Vrueh, R. L. A., Smith, P. L., & Lee, C. (1998) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)37707-9 · Cited by 91

Membrane Transporters as Drug Targets

Meijer, D. K. F., & Müller, M. (1999) · Cited by 86

Carrier-mediated intestinal absorption of valacyclovir, the L-valyl ester prodrug of acyclovir. 1. Interactions with peptides, organic anions and organic cations in rats

Sinko, P. J., & Balimane, P. V. (1998) · Biopharmaceutics & Drug Disposition · Cited by 84

Interaction of renin inhibitors with the intestinal uptake system for oligopeptides and β-lactam antibiotics

Kramer, W., Girbig, F., Gutjahr, U., Kleemann, H., Leipe, I., Urbach, H., & Wagner, A. (1990) · Biochimica et Biophysica Acta (BBA) - Biomembranes · doi:10.1016/0005-2736(90)90043-n · Cited by 79

Facilitated brain uptake of 4-chlorokynurenine and conversion to 7-chlorokynurenic acid

Hokari, M., Wu, H., Schwarcz, R. M., & Smith, Q. R. (1996) · Neuroreport · doi:10.1097/00001756-199612200-00004 · Cited by 77

Intestinal active absorption of sugar-conjugated compounds by glucose transport system: implication of improvement of poorly absorbable drugs

Mizuma, T., Ohta, K., Hayashi, M., & Awazu, S. (1992) · Biochemical Pharmacology · doi:10.1016/0006-2952(92)90649-4 · Cited by 75

Mechanism of L-α-Methyldopa Transport Through a Monolayer of Polarized Human Intestinal Epithelial Cells (Caco-2)

Hu, M., & Borchardt, R. T. (1990) · Pharmaceutical Research · doi:10.1023/a:1015906409585 · Cited by 72

Improving intestinal absorption of water-insoluble compounds: A membrane metabolism strategy

Amidon, G. L., Leesman, G. D., & Elliott, R. L. (1980) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.2600691203 · Cited by 70

Genetic delivery of enzymes for cancer therapy.

Deonarain, M. P., Spooner, R. A., & Aa, E. (1995) · PubMed · Cited by 67

Drug Transport and Targeting

Oh, D.-M., Han, H.-K., & Amidon, G. L. (2002) · Pharmaceutical biotechnology · doi:10.1007/0-306-46812-3_3 · Cited by 59

A micro‐electrode study of oligopeptide absorption by the small intestinal epithelium of Necturus maculosus.

Boyd, C. A. R., & Ward, M. R. (1982) · The Journal of Physiology · doi:10.1113/jphysiol.1982.sp014121 · Cited by 53

Intestinal brush-border transport of the oral cephalosporin antibiotic, cefdinir, mediated by dipeptide and monocarboxylic acid transport systems in rabbits

Tsuji, A., Tamai, I., Nakanishi, M., Terasaki, T., & Hamano, S. (1993) · Journal of Pharmacy and Pharmacology · doi:10.1111/j.2042-7158.1993.tb05645.x · Cited by 50

Structural Requirements for the Intestinal Mucosal-Cell Peptide Transporter: The Need for N-Terminal α-Amino Group

Bai, P., Subramanian, P. K., Mosberg, H. I., & Amidon, G. L. (1991) · Pharmaceutical Research · doi:10.1023/a:1015848522228 · Cited by 45

Comparative study of active absorption by the intestine and disposition of anomers of sugar-conjugated compounds

Mizuma, T., Ohta, K., Hayashi, M., & Awazu, S. (1993) · Biochemical Pharmacology · doi:10.1016/0006-2952(93)90053-y · Cited by 44

Antibody-Directed Enzyme Prodrug Therapy (ADEPT)

Bagshawe, K. D. (1993) · Advances in pharmacology · doi:10.1016/s1054-3589(08)60935-7 · Cited by 30

Chemical Approaches to Improve the Oral Bioavailability of Peptidergic Molecules

Samanen, J. M., Wilson, G., Smith, P. L., Lee, C., Bondinell, W. E., Ku, T. W., Rhodes, G. R., & Nichols, A. J. (1996) · Journal of Pharmacy and Pharmacology · doi:10.1111/j.2042-7158.1996.tb07111.x · Cited by 27

Gastrointestinal Transport of Peptide and Protein Drugs and Prodrugs

Bai, J., Stewart, B. H., & Amidon, G. L. (1994) · Handbook of experimental pharmacology · doi:10.1007/978-3-642-78680-8_6 · Cited by 7

Prodrugs: design and clinical applications

Rautio, J., Kumpulainen, H., Heimbach, T., Oliyai, R., Oh, D., Järvinen, T., & Savolainen, J. (2008) · Nature Reviews Drug Discovery · doi:10.1038/nrd2468 · Cited by 1,630

Is the oral route possible for peptide and protein drug delivery?

Morishita, M., & Peppas, N. A. (2006) · Drug Discovery Today · doi:10.1016/j.drudis.2006.08.005 · Cited by 515

Getting into the Brain: Approaches to Enhance Brain Drug Delivery

Patel, M. M., Goyal, B. R., Bhadada, S. V., Bhatt, J. S., & Amin, A. F. (2009) · CNS Drugs · doi:10.2165/0023210-200923010-00003 · Cited by 461

Enzymes involved in the bioconversion of ester-based prodrugs

Liederer, B. M., & Borchardt, R. T. (2006) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.20542 · Cited by 377

Self-assembling prodrugs

Cheetham, A. G., Chakroun, R. W., Ma, W., & Cui, H. (2017) · Chem. Soc. Rev. · doi:10.1039/c7cs00521k · Cited by 367