Targeting Receptor-Mediated Transport for Delivery of Biologics Across the Blood-Brain Barrier

Structure and function of the blood–brain barrier

Abbott, N. J., Patabendige, A. A. K., Dolman, D. E. M., Yusof, S. R., & Begley, D. J. (2010) · Neurobiology of Disease · doi:10.1016/j.nbd.2009.07.030 · Cited by 5,185

Delivery of siRNA to the mouse brain by systemic injection of targeted exosomes

Alvarez-Erviti, L., Seow, Y., Yin, H., Betts, C., Lakhal, S., & Wood, M. J. A. (2011) · Nature Biotechnology · doi:10.1038/nbt.1807 · Cited by 4,930

The blood-brain barrier: Bottleneck in brain drug development

Pardridge, W. M. (2005) · NeuroRX · doi:10.1602/neurorx.2.1.3 · Cited by 2,798

Transvascular delivery of small interfering RNA to the central nervous system

Kumar, P., Wu, H., McBride, J. L., Jung, K.-E., Hee Kim, M., Davidson, B. L., Kyung Lee, S., Shankar, P., & Manjunath, N. (2007) · Nature · doi:10.1038/nature05901 · Cited by 1,246

Blood–brain barrier delivery

Pardridge, W. M. (2007) · Drug Discovery Today · doi:10.1016/j.drudis.2006.10.013 · Cited by 1,191

Targeted Drug Delivery via the Transferrin Receptor-Mediated Endocytosis Pathway

Qian, Z., Li, H., Sun, H., & Ho, K. (2002) · Pharmacological Reviews · doi:10.1124/pr.54.4.561 · Cited by 1,035

Quantitative targeted absolute proteomics of human blood-brain barrier transporters and receptors

Uchida, Y., Ohtsuki, S., Katsukura, Y., Ikeda, C., Suzuki, T., Kamiie, J., & Terasaki, T. (2011) · Journal of Neurochemistry · doi:10.1111/j.1471-4159.2011.07208.x · Cited by 881

Boosting Brain Uptake of a Therapeutic Antibody by Reducing Its Affinity for a Transcytosis Target

Yu, Y. J., Zhang, Y., Kenrick, M., Hoyte, K., Luk, W., Lu, Y., Atwal, J., Elliott, J. M., Prabhu, S., Watts, R. J., et al. (2011) · Science Translational Medicine · doi:10.1126/scitranslmed.3002230 · Cited by 794

The blood–brain barrier in health and disease

Daneman, R. (2012) · Annals of Neurology · doi:10.1002/ana.23648 · Cited by 794

CNS Delivery Via Adsorptive Transcytosis

Hervé, F., Ghinea, N., & Scherrmann, J.-M. (2008) · The AAPS Journal · doi:10.1208/s12248-008-9055-2 · Cited by 676

Increased Brain Penetration and Potency of a Therapeutic Antibody Using a Monovalent Molecular Shuttle

Niewoehner, J., Bohrmann, B., Collin, L., Urich, E., Sade, H., Maier, P., Rueger, P., Stracke, J. O., Lau, W., Tissot, A. C., et al. (2014) · Neuron · doi:10.1016/j.neuron.2013.10.061 · Cited by 622

Molecular Signatures of Tissue-Specific Microvascular Endothelial Cell Heterogeneity in Organ Maintenance and Regeneration

Nolan, D. J., Ginsberg, M. D., Israely, E., Palikuqi, B., Poulos, M. G., James, D., Ding, B., Schachterle, W., Liu, Y., Rosenwaks, Z., et al. (2013) · Developmental Cell · doi:10.1016/j.devcel.2013.06.017 · Cited by 603

The Mouse Blood-Brain Barrier Transcriptome: A New Resource for Understanding the Development and Function of Brain Endothelial Cells

Daneman, R., Zhou, L., Agalliu, D., Cahoy, J. D., Kaushal, A., & Barres, B. A. (2010) · PLoS ONE · doi:10.1371/journal.pone.0013741 · Cited by 577

Organization of vesicular trafficking in epithelia

Rodriguez-Boulan, E., Kreitzer, G., & Müsch, A. (2005) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm1593 · Cited by 574

Involvement of the low‐density lipoprotein receptor‐related protein in the transcytosis of the brain delivery vector Angiopep‐2

Demeule, M., Currie, J., Bertrand, Y., Ché, C., Nguyen, T., Régina, A., Gabathuler, R., Castaigne, J., & Béliveau, R. (2008) · Journal of Neurochemistry · doi:10.1111/j.1471-4159.2008.05492.x · Cited by 557

Exosomes for targeted siRNA delivery across biological barriers

Andaloussi, S. E., Lakhal‐Littleton, S., Mäger, I., & Wood, M. J. A. (2012) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2012.08.008 · Cited by 555

Exosomes as intercellular signalosomes and pharmacological effectors

Record, M., Subra, C., Silvente‐Poirot, S., & Poirot, M. (2011) · Biochemical Pharmacology · doi:10.1016/j.bcp.2011.02.011 · Cited by 550

Blood–Brain Barrier Transport of Therapeutics via Receptor-Mediation

Jones, A. R., & Shusta, E. V. (2007) · Pharmaceutical Research · doi:10.1007/s11095-007-9379-0 · Cited by 549

ABC Transporters and the Blood-Brain Barrier

Begley, D. J. (2004) · Current Pharmaceutical Design · doi:10.2174/1381612043384844 · Cited by 548

Transcytosis and brain uptake of transferrin-containing nanoparticles by tuning avidity to transferrin receptor

Wiley, D. T., Webster, P. C., Gale, A., & Davis, M. E. (2013) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1307152110 · Cited by 535

Delivery of peptides and proteins through the blood–brain barrier

Bickel, U., Yoshikawa, T., & Pardridge, W. M. (2001) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(00)00139-3 · Cited by 490

A New Function for the LDL Receptor: Transcytosis of LDL across the Blood–Brain Barrier

Dehouck, B., Fenart, L., Dehouck, M.-P., Pierce, A., Torpier, G., & Cecchelli, R. (1997) · The Journal of Cell Biology · doi:10.1083/jcb.138.4.877 · Cited by 490

Contribution of Carrier-Mediated Transport Systems to the Blood–Brain Barrier as a Supporting and Protecting Interface for the Brain; Importance for CNS Drug Discovery and Development

Ohtsuki, S., & Terasaki, T. (2007) · Pharmaceutical Research · doi:10.1007/s11095-007-9374-5 · Cited by 476

Identification and Design of Peptides as a New Drug Delivery System for the Brain

Demeule, M., Régina, A., Ché, C., Poirier, J., Nguyen, T., Gabathuler, R., Castaigne, J., & Béliveau, R. (2007) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.107.131318 · Cited by 476

The intracellular trafficking pathway of transferrin

Mayle, K. M., Le, A. M., & Kamei, D. T. (2012) · Biochimica et Biophysica Acta (BBA) - General Subjects · doi:10.1016/j.bbagen.2011.09.009 · Cited by 466

Gantenerumab: A Novel Human Anti-Aβ Antibody Demonstrates Sustained Cerebral Amyloid-β Binding and Elicits Cell-Mediated Removal of Human Amyloid-β

Bohrmann, B., Baumann, K., Benz, J., Gerber, F., Huber, W., Knoflach, F., Messer, J., Oroszlan, K., Rauchenberger, R., Richter, W. F., et al. (2012) · Journal of Alzheimer's Disease · doi:10.3233/jad-2011-110977 · Cited by 448

Albumin nanoparticles targeted with Apo E enter the CNS by transcytosis and are delivered to neurones

Zensi, A., Begley, D., Pontikis, C., Legros, C., Mihoreanu, L., Wagner, S., Büchel, C., von Briesen, H., & Kreuter, J. (2009) · Journal of Controlled Release · doi:10.1016/j.jconrel.2009.03.002 · Cited by 438

Anti-transferrin receptor antibody and antibody-drug conjugates cross the blood-brain barrier.

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Transferrin and Transferrin Receptor Function in Brain Barrier Systems

Moos, T., & Morgan, E. H. (2000) · Cellular and Molecular Neurobiology · doi:10.1023/a:1006948027674 · Cited by 405

LDL receptor-related protein, a multifunctional ApoE receptor, binds secreted β-amyloid precursor protein and mediates its degradation

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Human blood-brain barrier leptin receptor. Binding and endocytosis in isolated human brain microvessels.

Golden, P. L., Maccagnan, T. J., & Pardridge, W. M. (1997) · Journal of Clinical Investigation · doi:10.1172/jci119125 · Cited by 372

Antitumour activity of ANG1005, a conjugate between paclitaxel and the new brain delivery vector Angiopep‐2

Régina, A., Demeule, M., Ché, C., Lavallée, I., Poirier, J., Gabathuler, R., Béliveau, R., & Castaigne, J. (2008) · British Journal of Pharmacology · doi:10.1038/bjp.2008.260 · Cited by 370

Blood-brain barrier transcytosis of insulin in developing rabbits

Duffy, K. R., & Pardridge, W. M. (1987) · Brain Research · doi:10.1016/0006-8993(87)90236-8 · Cited by 358

Selective transport of an anti-transferrin receptor antibody through the blood-brain barrier in vivo.

Pardridge, W. M., Buciak, J. L., & Friden, P. M. (1991) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)20567-5 · Cited by 358

Transferrin receptor (TfR) trafficking determines brain uptake of TfR antibody affinity variants

Bien‐Ly, N., Yu, Y. J., Bumbaca, D., Elstrott, J., Boswell, C. A., Zhang, Y., Luk, W., Lu, Y., Dennis, M. S., Weimer, R. M., et al. (2014) · The Journal of Experimental Medicine · doi:10.1084/jem.20131660 · Cited by 356

Gene delivery targeted to the brain using an Angiopep-conjugated polyethyleneglycol-modified polyamidoamine dendrimer

Ke, W., Shao, K., Huang, R., Han, L., Liu, Y., Li, J., Kuang, Y., Ye, L., Lou, J., & Jiang, C. (2009) · Biomaterials · doi:10.1016/j.biomaterials.2009.08.049 · Cited by 343

Restoring Blood-Brain Barrier P-Glycoprotein Reduces Brain Amyloid-β in a Mouse Model of Alzheimer’s Disease

Hartz, A. M. S., Miller, D. S., & Bauer, B. (2010) · Molecular Pharmacology · doi:10.1124/mol.109.061754 · Cited by 329

Absorptive-mediated endocytosis of cationized albumin and a beta-endorphin-cationized albumin chimeric peptide by isolated brain capillaries. Model system of blood-brain barrier transport.

Kumagai, A. K., Eisenberg, J., & Pardridge, W. M. (1987) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)48160-4 · Cited by 325

Human Insulin Receptor Monoclonal Antibody Undergoes High Affinity Binding to Human Brain Capillaries in Vitro and Rapid Transcytosis Through the Blood–Brain Barrier in Vivo in the Primate

Pardridge, W. M., Kang, Y., Buciak, J. L., & Yang, J. (1995) · Pharmaceutical Research · doi:10.1023/a:1016244500596 · Cited by 324

Transport of Insulin Across the Blood-Brain Barrier: Saturability at Euglycemic Doses of Insulin

Banks, W. A., Jaspan, J. B., Huang, W., & Kastin, A. J. (1997) · Peptides · doi:10.1016/s0196-9781(97)00231-3 · Cited by 318

A novel endocytic pathway induced by clustering endothelial ICAM-1 or PECAM-1

Muro, S., Wiewrodt, R. G., Thomas, A., Koniaris, L. S., Albelda, S. Μ., Muzykantov, V. R., & Koval, M. H. (2003) · Journal of Cell Science · doi:10.1242/jcs.00367 · Cited by 302

Targeting Rat Anti-Mouse Transferrin Receptor Monoclonal Antibodies through Blood-Brain Barrier in Mouse

Lee, H., Engelhardt, B., Lesley, J., Bickel, U., & Pardridge, W. M. (2000) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)35388-1 · Cited by 287

A Hybrid Vector for Ligand-Directed Tumor Targeting and Molecular Imaging

Hajitou, A., Trepel, M., Lilley, C. E., Soghomonyan, S., Alauddin, M. M., Marini, F. C., Restel, B. H., Ozawa, M. G., Moya, C. A., Rangel, R., et al. (2006) · Cell · doi:10.1016/j.cell.2006.02.042 · Cited by 283

Addressing Safety Liabilities of TfR Bispecific Antibodies That Cross the Blood-Brain Barrier

Couch, J. A., Yu, Y. J., Zhang, Y., Tarrant, J. M., Fuji, R. N., Meilandt, W. J., Solanoy, H. O., Tong, R. K., Hoyte, K., Luk, W., et al. (2013) · Science Translational Medicine · doi:10.1126/scitranslmed.3005338 · Cited by 278

Physiology of Blood–Brain Interfaces in Relation to Brain Disposition of Small Compounds and Macromolecules

Strazielle, N., & Ghersi‐Egea, J. (2013) · Molecular Pharmaceutics · doi:10.1021/mp300518e · Cited by 277

A Therapeutic Antibody Targeting BACE1 Inhibits Amyloid-β Production in Vivo

Atwal, J. K., Chen, Y., Chiu, C., Mortensen, D. L., Meilandt, W. J., Liu, Y., Heise, C. E., Hoyte, K., Luk, W., Lu, Y., et al. (2011) · Science Translational Medicine · doi:10.1126/scitranslmed.3002254 · Cited by 274

Uptake Mechanism of ApoE-Modified Nanoparticles on Brain Capillary Endothelial Cells as a Blood-Brain Barrier Model

Wagner, S., Zensi, A., Wien, S., Tschickardt, S., Maier, W., Vogel, T., Worek, F., Pietrzik, C. U., Kreuter, J., & von Briesen, H. (2012) · PLoS ONE · doi:10.1371/journal.pone.0032568 · Cited by 265

Selection of phage‐displayed llama single‐domain antibodies that transmigrate across human blood‐brain barrier endothelium

Muruganandam, A., Tanha, J., Narang, S. A., & Stanimirovic, D. B. (2001) · The FASEB Journal · doi:10.1096/fj.01-0343fje · Cited by 261

Targeted delivery of proteins across the blood–brain barrier

Spencer, B. J., & Verma, I. M. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0702170104 · Cited by 249

Identification of the low density lipoprotein receptor-binding site in apolipoprotein B100 and the modulation of its binding activity by the carboxyl terminus in familial defective apo-B100.

Borén, J., Lee, I., Zhu, W., Arnold, K. S., Taylor, S., & Innerarity, T. L. (1998) · Journal of Clinical Investigation · doi:10.1172/jci1847 · Cited by 233

Uptake of ANG1005, A Novel Paclitaxel Derivative, Through the Blood-Brain Barrier into Brain and Experimental Brain Metastases of Breast Cancer

Thomas, F. C., Taskar, K. S., Rudraraju, V., Goda, S., Thorsheim, H. R., Gaasch, J. A., Mittapalli, R. K., Palmieri, D., Steeg, P. S., Lockman, P. R., et al. (2009) · Pharmaceutical Research · doi:10.1007/s11095-009-9964-5 · Cited by 227

High transcytosis of melanotransferrin (P97) across the blood–brain barrier

Demeule, M., Poirier, J., Jodoin, J., Bertrand, Y., Desrosiers, R. R., Dagenais, C., Nguyen, T., Lanthier, J., Gabathuler, R., Kennard, M. L., et al. (2002) · Journal of Neurochemistry · doi:10.1046/j.1471-4159.2002.01201.x · Cited by 223

The blood–brain barrier transmigrating single domain antibody: mechanisms of transport and antigenic epitopes in human brain endothelial cells

Abulrob, A., Sprong, H., Henegouwen, P. M. P. V. B. E., & Stanimirovic, D. B. (2005) · Journal of Neurochemistry · doi:10.1111/j.1471-4159.2005.03463.x · Cited by 223

Humanization of anti‐human insulin receptor antibody for drug targeting across the human blood–brain barrier

Boado, R. J., Zhang, Y., Zhang, Y., & Pardridge, W. M. (2006) · Biotechnology and Bioengineering · doi:10.1002/bit.21120 · Cited by 213

Cellular Elements of the Blood-Brain Barrier

Correale, J. D., & Villa, A. M. (2009) · Neurochemical Research · doi:10.1007/s11064-009-0081-y · Cited by 210

A Nanomedicine Transports a Peptide Caspase-3 Inhibitor across the Blood–Brain Barrier and Provides Neuroprotection

Karataş, H., Aktaş, Y., Özdemir, Y., Bodur, E., Yemişçi, M., Caban-Toktas, S., Vural, A., Pınarbaşlı, O., Çapan, Y., Fernández-Megía, E., et al. (2009) · Journal of Neuroscience · doi:10.1523/jneurosci.4246-09.2009 · Cited by 191

Phase I Study of GRN1005 in Recurrent Malignant Glioma

Drappatz, J., Brenner, A., Wong, E. T., Eichler, A., Schiff, D., Groves, M. D., Mikkelsen, T., Rosenfeld, S., Sarantopoulos, J., Meyers, C. A., et al. (2013) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-12-2481 · Cited by 190

Gene therapy progress and prospects: Hydrodynamic gene delivery

Herweijer, H., & Wolff, J. A. (2006) · Gene Therapy · doi:10.1038/sj.gt.3302891 · Cited by 189

Cell penetrating peptide tethered bi-ligand liposomes for delivery to brain in vivo: Biodistribution and transfection

Sharma, G., Modgil, A., Layek, B., Arora, K., Sun, C., Law, B., & Singh, J. (2013) · Journal of Controlled Release · doi:10.1016/j.jconrel.2013.01.016 · Cited by 183

Tissue-Type Plasminogen Activator Crosses the Intact Blood-Brain Barrier by Low-Density Lipoprotein Receptor–Related Protein-Mediated Transcytosis

Benchenane, K., Bérézowski, V., Ali, C., Fernández‐Monreal, M., López‐Atalaya, J. P., Brillault, J., Chuquet, J., Nouvelot, A., MacKenzie, E. T., Bu, G., et al. (2005) · Circulation · doi:10.1161/01.cir.0000163542.48611.a2 · Cited by 178

Receptor-mediated transcytosis of transferrin through blood-brain barrier endothelial cells

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Mechanisms of TfR-mediated transcytosis and sorting in epithelial cells and applications toward drug delivery

Widera, A., Norouziyan, F., & Shen, W. (2003) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2003.07.004 · Cited by 173

Restricted transport of anti‐transferrin receptor antibody (OX26) through the blood–brain barrier in the rat

Moos, T., & Morgan, E. H. (2001) · Journal of Neurochemistry · doi:10.1046/j.1471-4159.2001.00541.x · Cited by 169

Large Neutral Amino Acid Transporter Enables Brain Drug Delivery via Prodrugs

Gynther, M., Laine, K., Ropponen, J., Leppänen, J., Mannila, A., Nevalainen, T., Savolainen, J., Järvinen, T., & Rautio, J. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm701175d · Cited by 169

Re-Engineering Biopharmaceuticals for Delivery to Brain with Molecular Trojan Horses

Pardridge, W. M. (2008) · Bioconjugate Chemistry · doi:10.1021/bc800148t · Cited by 168

Safety, Pharmacokinetics, and Activity of GRN1005, a Novel Conjugate of Angiopep-2, a Peptide Facilitating Brain Penetration, and Paclitaxel, in Patients with Advanced Solid Tumors

Kurzrock, R., Gabrail, N., Chandhasin, C., Moulder, S., Smith, C., Brenner, A., Sankhala, K., Mita, A., Elian, K., Bouchard, D., et al. (2012) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-11-0566 · Cited by 168

Potential role of the low-density lipoprotein receptor family as mediators of cellular drug uptake

Chung, N., & Wasan, K. M. (2004) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2003.12.003 · Cited by 165

Systemic combinatorial peptide selection yields a non-canonical iron-mimicry mechanism for targeting tumors in a mouse model of human glioblastoma

Staquicini, F. I., Ozawa, M. G., Moya, C. A., Driessen, W. H. P., Barbu, E. M., Nishimori, H., Soghomonyan, S., Flores, L. G., Liang, X., Paolillo, V., et al. (2010) · Journal of Clinical Investigation · doi:10.1172/jci44798 · Cited by 163

Targeting Anti—Transferrin Receptor Antibody (OX26) and OX26-Conjugated Liposomes to Brain Capillary Endothelial Cells Using In Situ Perfusion

Gosk, S., Vermehren, C., Storm, G., & Moos, T. (2004) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1097/01.wcb.0000135592.28823.47 · Cited by 163

Efficient transfer of receptor-associated protein (RAP) across the blood-brain barrier

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Engineering a lysosomal enzyme with a derivative of receptor-binding domain of apoE enables delivery across the blood–brain barrier

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Iron and transferrrin uptake by brain and cerebrospinal fluid in the rat

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Transcytosis of Protein through the Mammalian Cerebral Epithelium and Endothelium

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Engineering and expression of a chimeric transferrin receptor monoclonal antibody for blood–brain barrier delivery in the mouse

Boado, R. J., Zhang, Y., Wang, Y., & Pardridge, W. M. (2008) · Biotechnology and Bioengineering · doi:10.1002/bit.22135 · Cited by 146

Genetic engineering of a lysosomal enzyme fusion protein for targeted delivery across the human blood‐brain barrier

Boado, R. J., Zhang, Y., Zhang, Y., Xia, C., Wang, Y., & Pardridge, W. M. (2007) · Biotechnology and Bioengineering · doi:10.1002/bit.21602 · Cited by 142

Fusion Antibody for Alzheimer's Disease with Bidirectional Transport Across the Blood−Brain Barrier and Aβ Fibril Disaggregation

Boado, R. J., Zhang, Y., Zhang, Y., Xia, C., & Pardridge, W. M. (2007) · Bioconjugate Chemistry · doi:10.1021/bc060349x · Cited by 135

ABC Transporters in the CNS – An Inventory

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Conjugation of a brain-penetrant peptide with neurotensin provides antinociceptive properties

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Differing regulation and function of ICAM-1 and class II antigens on renal tubular cells

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Pharmacokinetics and Brain Uptake of a Genetically Engineered Bifunctional Fusion Antibody Targeting the Mouse Transferrin Receptor

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Physiological Pathway for Low-Density Lipoproteins across the Blood-Brain Barrier: Transcytosis through Brain Capillary Endothelial Cells In Vitro

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A highly secreted sulphamidase engineered to cross the blood‐brain barrier corrects brain lesions of mice with mucopolysaccharidoses type IIIA

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Transduction of Liver Cells by Lentiviral Vectors: Analysis in Living Animals by Fluorescence Imaging

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Selective targeting of a TNFR decoy receptor pharmaceutical to the primate brain as a receptor-specific IgG fusion protein

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Design and construction of targeted AAVP vectors for mammalian cell transduction

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Glycoprotein 330/Low Density Lipoprotein Receptor-related Protein-2 Mediates Endocytosis of Low Density Lipoproteins via Interaction with Apolipoprotein B100

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GDNF fusion protein for targeted‐drug delivery across the human blood–brain barrier

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Drug Targeting of Erythropoietin Across the Primate Blood-Brain Barrier with an IgG Molecular Trojan Horse

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Rabies virus binding to an acetylcholine receptor α‐subunit peptide

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Polyamine Modification Increases the Permeability of Proteins at the Blood‐Nerve and Blood‐Brain Barriers

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