Delivery of peptides and proteins through the blood-brain barrier

De Bault, 1980, Gamma-glutamyl transpeptidase in isolated brain endothelial cells: Induction by glial cells in vitro, Science, 207, 653, 10.1126/science.6101511 Cordon-Cardo, 1989, Multidrug-resistance gene (P-glycoprotein) is expressed by endothelial cells at blood-brain barrier sites, 86, 695 Mueckler, 1985, Sequence and structure of a human glucose transporter, Science, 229, 941, 10.1126/science.3839598 Birnbaum, 1986, Cloning and characterization of a cDNA encoding the rat brain glucose-transporter protein, 83, 5784 Pardridge, 1990, Brain-type glucose transporter (GLUT1) is selectively localized to the blood-brain barrier, 265, 18035 Pardridge, 1990, Comparison of in vitro and in vivo models of drug transcytosis through the blood-brain barrier, J. Pharmacol. Exp. Ther., 253, 884 Duvernoy, 1983, The vascularization of the human cerebellar cortex, Brain Res. Bull., 11, 419, 10.1016/0361-9230(83)90116-8 Brightman, 1977, Morphology of blood-brain interfaces, Exp. Eye Res., 25, 1, 10.1016/S0014-4835(77)80008-0 Weindl, 1973, Neuroendocrine aspects of circumventricular organs, 3 Crone, 1971, The blood-brain barrier-facts and questions, 52 Fishman, 1980 Davson, 1987, Secretion of the cerebrospinal fluid, 201 Shapiro, 1975, Methotrexate: distribution in cerebrospinal fluid after intravenous, ventricular and lumbar injections, N. Engl. J. Med., 293, 161, 10.1056/NEJM197507242930402 Blasberg, 1975, Intrathecal chemotherapy: brain tissue profiles after ventriculo-cisternal perfusion, J. Pharmacol. Exp. Ther., 195, 73 Harbaugh, 1989, Nerve growth factor as a potential treatment in Alzheimer's disease, Biomed. Pharmacother., 43, 483, 10.1016/0753-3322(89)90108-X Munsat, 1992, Intrathecal thyrotropin releasing hormone does not alter the progressive course of ALS, Neurology, 42, 1049, 10.1212/WNL.42.5.1049 Caroscio, 1986, A double-blind, placebo-controlled trial of TRH in amyotrophic lateral sclerosis, Neurology, 36, 141, 10.1212/WNL.36.2.141 Rieselbach, 1962, Subarachnoid distribution of drugs after lumbar injection, N. Engl. J. Med., 267, 1273, 10.1056/NEJM196212202672502 Oldendorf, 1970, Measurement of brain uptake of radiolabeled substances using a tritiated water internal standard, Brain Res., 24, 372, 10.1016/0006-8993(70)90123-X Pardridge, 1988, Recent advances in blood-brain barrier transport, Annu. Rev. Pharmacol. Toxicol., 28, 25, 10.1146/annurev.pa.28.040188.000325 Pardridge, 1984, Tracer kinetic model of blood-brain barrier transport of plasma protein-bound ligands, J. Clin. Invest., 74, 745, 10.1172/JCI111490 Zlokovic, 1986, Measurement of solute transport across the blood-brain barrier in the perfused guinea pig brain: method and application to N-methyl-α-aminoisobutyric acid, J. Neurochem., 46, 1444, 10.1111/j.1471-4159.1986.tb01760.x Zlokovic, 1987, Transport of leucineenkephalin across the blood-brain barrier in the perfused guinea pig brain, J. Neurochem., 49, 310, 10.1111/j.1471-4159.1987.tb03431.x Zlokovic, 1988, Slow penetration of thyrotropin-releasing hormone across the blood-brain barrier of an in situ perfused guinea pig brain, J. Neurochem., 51, 252, 10.1111/j.1471-4159.1988.tb04864.x Zlokovic, 1989, Kinetic analysis of leucineenkephalin cellular uptake at the luminal side of the blood-brain barrier of an in situ perfused guinea-pig brain, J. Neurochem., 53, 1333, 10.1111/j.1471-4159.1989.tb08522.x Takasato, 1984, An in situ brain perfusion technique to study cerebrovascular transport in the rat, Am. J. Physiol., 247, H484 Fenstermacher, 1981, Methods for quantifying the transport of drugs across brain barrier systems, Pharmacol. Ther., 14, 217, 10.1016/0163-7258(81)90062-0 Patlak, 1983, Graphical evaluation of blood-to-brain transfer constants from multiple-time uptake data, J. Cereb. Blood Flow Metab., 3, 1, 10.1038/jcbfm.1983.1 Blasberg, 1983, Transport of α-aminoisobutyric acid across brain capillary and cellular membranes, J. Cereb. Blood Flow Metab., 3, 8, 10.1038/jcbfm.1983.2 Pardridge, 1990, β-endorphin chimeric peptides: transport through the blood-brain barrier in vivo and cleavage of disulfide linkage by brain, Endocrinology, 126, 977, 10.1210/endo-126-2-977 Churchill, 1987, Metabolism of opioid peptides by cerebral microvascular aminopeptidase M, Biochim. Biophys. Acta, 923, 35, 10.1016/0304-4165(87)90122-X Solhonne, 1987, Major localization of aminopeptidase M in rat brain microvessels, Neuroscience, 22, 225, 10.1016/0306-4522(87)90212-0 Zlokovic, 1985, Blood-brain barrier permeability to leucine-enkephalin, d-alanine2-d-leucine5-enkephalin and their N-terminal amino acid (tyrosine), Brain Res., 336, 125, 10.1016/0006-8993(85)90423-8 Deleted in proof. Triguero, 1990, Capillary depletion method for quantifying blood-brain barrier transcytosis of circulating peptides and plasma proteins, J. Neurochem., 54, 1882, 10.1111/j.1471-4159.1990.tb04886.x Duffy, 1987, Blood-brain barrier transcytosis of insulin in developing rabbits, Brain Res., 420, 32, 10.1016/0006-8993(87)90236-8 Broadwell, 1988, Transcytotic pathway for blood-borne protein through the blood-brain barrier, 85, 632 Joo, 1985, The blood-brain barrier in vitro: ten years of research on microvessels isolated from the brain, Neurochem. Int., 7, 1, 10.1016/0197-0186(85)90002-6 Lasbennes, 1983, Capacity for energy metabolism in microvessels isolated from rat brain, Neurochem. Res., 9, 1, 10.1007/BF00967654 Pardridge, 1991 van Houten, 1979, Insulin-binding sites in the rat brain: in vivo localization to the circumventricular organs by quantitative radioautography, Endocrinology, 105, 666, 10.1210/endo-105-3-666 Frank, 1981, A direct in vitro demonstration of insulin binding to isolated brain microvessels, Diabetes, 30, 757, 10.2337/diabetes.30.9.757 Pardridge, 1985, Human blood-brain barrier insulin receptor, J. Neurochem., 44, 1771, 10.1111/j.1471-4159.1985.tb07167.x Duffy, 1988, Human blood-brain barrier insulin-like growth factor receptor, Metabolism, 37, 136, 10.1016/S0026-0495(98)90007-5 Frank, 1986, Binding and internalization of insulin and insulin-like growth factors by isolated brain microvessels, Diabetes, 35, 654, 10.2337/diabetes.35.6.654 Speth, 1985, Angiotensin II receptor binding sites in brain microvessels, 82, 6340 Chabrier, 1987, Specific binding of atrial natriuretic factor in brain microvessels, 84, 2078 Okazaki, 1990, Atrial natriuretic peptide receptors in cerebral microvessels and choroid plexus of spontaneously hypertensive rats, Brain Res., 518, 292, 10.1016/0006-8993(90)90984-J Jefland, 1991, Brain and atrial natriuretic peptide bind to common receptors in brain capillary endothelial cells, Am. J. Physiol., 261, E183 Hashimoto, 1991, Action site of circulating interleukin-1 on the rabbit brain, Brain Res., 540, 217, 10.1016/0006-8993(91)90510-3 Banks, 1991, Human interleukin (IL) 1α, murine IL-1α and murine IL-1β are transported from blood to brain in the mouse by a shared saturable mechanism, J. Pharmacol. Exp. Ther., 259, 988 Jefferies, 1984, Transferrin receptor on endothelium of brain capillaries, Nature, 312, 162, 10.1038/312162a0 Fishman, 1987, Receptor-mediated transcytosis of transferrin across the blood-brain barrier, J. Neurosci. Res., 18, 299, 10.1002/jnr.490180206 Taylor, 1990, Developmental changes in transferrin and iron uptake by the brain in the rat, Dev. Brain Res., 55, 35, 10.1016/0165-3806(90)90103-6 Grasso, 1987, Transglutaminase activity in bovine calf testicular membranes: evidence for a possible role in the interaction of follicle-stimulating hormone with its receptor, Endocrinology, 121, 459, 10.1210/endo-121-2-459 Gex-Fabry, 1984, Receptor-mediated endocytosis: a model and its implications for experimental analysis, Am. J. Physiol., 247, R768 Verner, 1988, Protein translocation across membranes, Science, 241, 1307, 10.1126/science.2842866 Lund, 1990, Quantitative analysis of the endocytic system involved in hormone-induced receptor internalization, J. Biol. Chem., 265, 15713, 10.1016/S0021-9258(18)55456-9 Clarke, 1985, Recycling of the asialoglycoprotein receptor in isolated rat hepatocytes, J. Biol. Chem., 260, 128, 10.1016/S0021-9258(18)89703-4 Solenski, 1985, Insulin binding and vesicular ingestion in capillary endothelium, J. Cell. Physiol., 124, 87, 10.1002/jcp.1041240115 Willingham, 1984, Morphologic characterization of the pathway of transferrin endocytosis and recycling in human KB cells, 81, 175 Ahnert-Hilger, 1985, Minimal requirements for exocytosis, J. Biol. Chem., 260, 12730, 10.1016/S0021-9258(17)38936-6 McAbee, 1987, ATP depletion causes a reversible redistribution and inactivation of a subpopulation of galactosyl receptors in isolated rat hepatocytes, J. Biol. Chem., 260, 128 Vilmart-Seuwen, 1986, ATP keeps exocytosis sites in a primed state but is not required for membrane fusion: an analysis with Paramecium cells in vivo and in vitro, J. Cell. Biol., 103, 1279, 10.1083/jcb.103.4.1279 Almers, 1990, Exocytosis, Annu. Rev. Physiol., 52, 607, 10.1146/annurev.ph.52.030190.003135 Pardridge, 1985, Blood-brain barrier protein phosphorylation and dephosphorylation, J. Neurochem., 45, 1141, 10.1111/j.1471-4159.1985.tb05534.x Gonatas, 1984, Endosomes and Golgi vesicles in adsorptive and fluid phase endocytosis, J. Cell Biol., 99, 1379, 10.1083/jcb.99.4.1379 Nevo, 1955, Interaction of basic polyamino acids with the red blood cell, Biochim. Biophys. Acta, 17, 536, 10.1016/0006-3002(55)90416-9 Skutelsky, 1976, Redistribution of surface anionic sites on the luminal front of blood vessel endothelium after interaction with polycationic ligand, J. Cell. Biol., 71, 232, 10.1083/jcb.71.1.232 Vorbrodt, 1989, Ultracytochemical characterization of anionic sites in the wall of brain capillaries, J. Neurocytol, 18, 359, 10.1007/BF01190839 Basu, 1976, Degradation of cationized low density lipoprotein and regulation of cholesterol metabolism in homozygous familial hypercholesterolemia fibroblasts, 73, 3178 Shen, 1978, Conjugation of poly-l-lysine to albumin and horseradish peroxidase: a novel method of enhancing the cellular uptake of proteins, 75, 1872 Griffin, 1982, Study of protein characteristics that influence entry into the cerebrospinal fluid of normal mice and mice with encephalitis, J. Clin. Invest., 70, 289, 10.1172/JCI110616 Terasaki, 1989, Absorptive-mediated endocytosis of a dynorphin-like analgesic peptide, E-2078, into the blood-brain barrier, J. Pharmacol. Exp. Ther., 251, 351 Terasaki, 1991, In vivo transport of a dynorphin-like analgesic peptide, E-2078, through the blood-brain barrier: an application of brain microdialysis, Pharm. Res., 8, 815, 10.1023/A:1015882924470 Shimura, 1991, Transport mechanism of a new behaviorally highly potent adrenocorticotropic hormone (ACTH) analog, ebiratide, through the blood brain barrier, J. Pharmacol. Exp. Ther., 258, 459 Peters, 1985, Serum albumin, Adv. Protein Chem., 17, 161, 10.1016/S0065-3233(08)60065-0 Lambert, 1983, The pathogenicity of cationized albumin in the dog, 307 Kumagai, 1987, Absorptive-mediated endocytosis of cationized albumin and a β-endorphin-cationized albumin chimeric peptide by isolated brain capillaries, 262, 15214 Pardridge, 1990, Evaluation of cationized rat albumin as a potential blood-brain barrier drug transport vector, J. Pharmacol. Exp. Ther., 255, 893 Bergmann, 1984, Plasma clearance, tissue distribution and catabolism of cationized albumins with increasing isoelectric points in the rat, Clin. Sci., 67, 35, 10.1042/cs0670035 Pardridge, 1989, Transport of histone through the blood-brain barrier, J. Pharmacol. Exp. Ther., 251, 821 Hardebo, 1985, Endothelial negative surface charge areas and blood-brain barrier function, Acta Physiol. Scand., 125, 495, 10.1111/j.1748-1716.1985.tb07746.x Nagy, 1983, Charge-related alterations of the cerebral endothelium, Lab. Invest., 49, 662 Strausbaugh, 1987, Intracarotid infusions of protamine sulfate disrupt the blood-brain barrier of rabbits, Brain Res., 409, 221, 10.1016/0006-8993(87)90705-0 Vehaskari, 1984, The effects of polycations on vascular permeability in the rat, J. Clin. Invest., 73, 1053, 10.1172/JCI111290 Adler, 1983, Electrical charge, 71, 487 Huang, 1984, In situ formation of immune complexes in the choroid plexus of rats by sequential injection of a cationized antigen and unaltered antibodies, J. Neuropathol. Exp. Neurol., 43, 489, 10.1097/00005072-198409000-00004 Nell, 1988, Frequency and specificity of protamine antibodies in diabetic and control subjects, Diabetes, 37, 172, 10.2337/diabetes.37.2.172 Muckerheide, 1987, Cationization of protein antigens, J. Immunol., 138, 833 Triguero, 1989, Blood-brain barrier transport of cationized immunoglobulin G, 86, 4761 Pardridge, 1985, Absence of albumin receptor on brain capillaries in vivo or in vitro, Am J. Physiol., 249, E264 Triguero, 1991, Cationization of immunoglobulin G results in enhanced organ uptake of the protein following intravenous administration in rats and primate, J. Pharmacol. Exp. Ther., 258, 186 Bergmann, 1983, Binding of cationized albumin to red cells, 29 Gauthier, 1982, Effect of cationized antibodies in preformed immune complexes on deposition and persistence in renal glomeruli, J. Exp. Med., 156, 766, 10.1084/jem.156.3.766 Fujii, 1990, Structural heterogeneity of sugar chains in immunoglobulin G, J. Biol. Chem., 265, 6009, 10.1016/S0021-9258(19)39283-X Rodwell, 1986, Site-specific covalent modification of monoclonal antibodies: in vitro and in vivo evaluations, 83, 2632 Morrison, 1988, Production and characterization of genetically engineered antibody molecules, Clin. Chem., 34, 1668, 10.1093/clinchem/34.9.1668 Morrison, 1984, Chimeric human antibody molecules: mouse antigen-binding domains with human constant region domains, 81, 6851 Mathieson, 1990, Monoclonal-antibody therapy in systemic vasculitis, N. Engl. J. Med., 323, 250, 10.1056/NEJM199007263230407 Abuchowski, 1977, Alteration of immunological properties of bovine serum albumin by covalent attachment of polyethylene glycol, J. Biol. Chem., 252, 3578, 10.1016/S0021-9258(17)40291-2 Abuchowski, 1977, Effect of covalent attachment of polyethylene glycol on immunogenicity and circulating life of bovine liver catalase, J. Biol. Chem., 252, 3582, 10.1016/S0021-9258(17)40292-4 Pool, 1990, “Hairy enzymes” stay in blood, Science, 248, 305, 10.1126/science.2326644 Giddings, 1985, Evaluation of rat insulin messenger RNA in pancreatic and extrapancreatic tissues, Diabetologia, 28, 343, 10.1007/BF00283141 Baskin, 1983, Regional concentrations of insulin in rat brain, Endocrinology, 112, 898, 10.1210/endo-112-3-898 Frank, 1985, Enhanced insulin binding to blood-brain barrier in vivo and to brain microvessels in vitro in newborn rabbits, Diabetes, 34, 728, 10.2337/diabetes.34.8.728 Havrankova, 1979, Concentrations of insulin and of insulin receptors in the brain are independent of peripheral insulin levels, 64, 636 Frank, 1986, Insulin binding to the blood-brain barrier in the streptozotocin diabetic rat, J. Neurochem., 47, 405, 10.1111/j.1471-4159.1986.tb04516.x Dahms, 1989, Mannose-6-phosphate receptors and lysosomal enzyme targeting, J. Biol. Chem., 264, 12115, 10.1016/S0021-9258(18)63825-6 Rosenfeld, 1987, Demonstration and structural comparison of receptors for insulin-like growth factor-I and -II (IGF-I and -II) in brain and blood-brain barrier, Biochem. Biophys. Res. Commun., 149, 159, 10.1016/0006-291X(87)91618-4 Braulke, 1990, Insulin-like growth factors I and II stimulate endocytosis but do not affect sorting of lysosomal enzymes in human fibroblasts, J. Biol. Chem., 265, 6650, 10.1016/S0021-9258(19)39199-9 Kovacina, 1989, Interactions of recombinant and platelet transforming growth factor-beta 1 precursor with the insulin-like growth factor II/mannose 6-phosphate receptor, Biochem. Biophys. Res. Commun., 160, 393, 10.1016/0006-291X(89)91669-0 Werther, 1990, Localization of insulin-like growth factor-I mRNA in rat brain by in situ hybridization-relationship to IGF-I receptors, Molec. Endocrinol., 4, 773, 10.1210/mend-4-5-773 Haselbacher, 1985, Insulin-like growth factor II (IGF II) in human brain: regional distribution of IGF II and of higher molecular mass forms, 82, 2153 Ocrant, 1990, Characterization of insulin-like growth factor binding proteins produced in the rat central nervous system, Endocrinology, 127, 1260, 10.1210/endo-127-3-1260 Cascieri, 1988, Serum half-life and biological activity of mutants of human insulin-like growth factor I which do not bind to serum binding proteins, Endocrinology, 123, 373, 10.1210/endo-123-1-373 Clemmons, 1990, Discrete alterations of the insulin-like growth factor I molecule which alter its affinity for insulin-like growth factor-binding proteins result in changes in bioactivity, J. Biol. Chem., 265, 12210, 10.1016/S0021-9258(19)38332-2 De Vroede, 1985, Hybrid molecules containing the B-domain of insulin-like growth factor I are recognized by carrier proteins of the growth factor, 82, 3010 Huebers, 1987, The physiology of transferrin and transferrin receptors, Physiol. Rev., 67, 520, 10.1152/physrev.1987.67.2.520 Jing, 1990, Nonacylated human transferrin receptors are rapidly internalized and mediate iron uptake, J. Biol. Chem., 265, 11555, 10.1016/S0021-9258(19)38433-9 Alvarez, 1990, Inhibition of the receptor-mediated endocytosis of diferric transferrin is associated with the covalent modification of the transferrin receptor with palmitic acid, J. Biol. Chem., 265, 16644, 10.1016/S0021-9258(17)46270-3 Pardridge, 1987, Human blood-brain barrier transferrin receptor, Metabolism, 36, 892, 10.1016/0026-0495(87)90099-0 Seligman, 1983, Structure and function of the transferrin receptor, Prog. Hematol., 13, 131 Friden, 1991, Antitransferrin receptor antibody and antibody-drug conjugates cross the blood-brain barrier, 88, 4771 Pardridge, 1991, Selective transport of an anti-transferrin receptor antibody through the blood-brain barrier in vivo, J. Pharmacol. Exp. Ther., 259, 66 Letvin, 1986, In vivo administration of lymphocyte-specific monoclonal antibodies in nonhuman primates, 77, 977 Worrell, 1986, Fate of an antibody-ricin A chain conjugate administered to normal rats, Biochem. Pharmacol., 35, 417, 10.1016/0006-2952(86)90214-5 Pardridge, 1993, Localization of blood-brain barrier-specific antibodies with immunogold-silver enhancement methodology, J. Histotechnol., 10.1179/his.1993.16.3.249 Broadwell, 1989, Transcytosis of macromolecules through the blood-brain barrier: a cell biological perspective and critical appraisal, Acta Neuropathol., 79, 117, 10.1007/BF00294368 Pardridge, 1992, Transport of recombinant CD4 through the rat blood brain barrier, J. Pharmacol. Exp. Ther., 261, 1175 Pardridge, 1987, Chimeric peptides as a vehicle for peptide pharmaceutical delivery through the blood-brain barrier, Biochem. Biophys. Res. Commun., 146, 307, 10.1016/0006-291X(87)90726-1 Yoshikawa, 1992, Biotin delivery to brain with a covalent conjugate of avidin and a monoclonal antibody to the transferrin receptor, J. Pharmacol. Exp. Ther., 263, 897 Pardridge, 1993, Drug delivery of antisense oligonucleotides or peptides to tissues in vivo using an avidin-biotin system, Drug Targeting Delivery, 10.3109/10717549309031340 Green, 1990, Avidin and streptavidin, Methods Enzymol., 184, 51, 10.1016/0076-6879(90)84259-J Pardridge, 1991, Enhanced cellular uptake of biotinylated antisense oligonucleotide or peptide mediated by avidin, a cationic protein, FEBS Lett., 288, 30, 10.1016/0014-5793(91)80996-G Riddles, 1979, Ellman's reagent: 5,5′-dithiobis(2-nitrobenzoic acid) - a reexamination, Anal. Biochem., 94, 75, 10.1016/0003-2697(79)90792-9 Bewley, 1983, Evidence for tertiary structure in aqueous solutions of human β-endorphin as shown by difference absorption spectroscopy, Biochemistry, 22, 2671, 10.1021/bi00280a013 Yaksh, 1987, Cortical vasodilatation produced by vasoactive intestinal polypeptide (VIP) and by physiological stimuli in the cat, J. Cereb. Blood Flow Metab., 7, 315, 10.1038/jcbfm.1987.69 McCulloch, 1980, Cerebral circulatory and metabolic effects of vasoactive intestinal polypeptide, Am. J. Physiol., 238, H449 Bickel, 1993, Pharmacologic effects in vivo in brain by vector-mediated delivery of peptides, 90, 2618 Andersson, 1991, The preparation of biotinyl-ε-aminocaproylated forms of the vasoactive intestinal polypeptide (VIP) as probes for the VIP receptor, FEBS Lett., 282, 35, 10.1016/0014-5793(91)80439-A Huffman, 1986, Effects of vasoactive intestinal peptide on thyroid blood flow and circulating thyroid hormone levels in the rat, Endocrinology, 118, 550, 10.1210/endo-118-2-550 Bickel, 1992, Site protected, cationized monoclonal antibody against beta amyloid as a potential diagnostic imaging technique for Alzheimer's disease, Soc. Neurosci. Abstr., 18, 764