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Brain Cancer Receptors and Targeting Strategies

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Targeted Intracellular Drug Delivery by Receptor Mediated Endocytosis

Part of the book series: AAPS Advances in the Pharmaceutical Sciences Series ((AAPS,volume 39))

Abstract

Brain cancer is regarded as the most widespread cancer of the central nervous system. The complexity of the glial cell tumor renders the survival and prognosis of glioma difficult, even after conventional chemotherapy, radiotherapy, and surgery treatments. The major concern is the formidable blood–brain barrier (BBB) that guards the entry of all exogenous moieties into the brain. This chapter addresses in brief the various approaches to bypass the BBB. Among different strategies, receptor-oriented drug delivery takes advantage of receptors on the BBB to traverse into the brain and if appropriately designed can enter the cancer cells through receptors overexpressed on their surface. This chapter will also summarize the various receptors, their physiology, ligands for the receptor, and drug-delivery strategies that could improve brain cancer therapy.

Rijo John and Heero Vaswani are equally contributed to this work.

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Abbreviations

ADC:

Antibody–drug conjugate

ADMIDAS:

Adjacent to MIDAS

AP1:

CRKRLDRNC peptide

Apo B:

Apolipoprotein B

Apo E:

Apolipoprotein E

AQP4:

Aquaporin-4

BBB:

Blood-brain barrier

BSA:

Bovine serum albumin

CNS:

Central nervous system

DHA:

Docosahexaenoic acid

DNA:

Deoxyribonucleic acid

DOX:

Doxorubicin

EGF:

Epidermal growth factor

EGFR:

Epithelial growth factor receptor

EPR:

Enhanced permeability and retention

GBM:

Glioblastoma

IC50:

Half-maximal inhibitory concentration

IL:

Interleukin

IL-13Rα2:

Interleukin-13 receptor subunit alpha-2

IL-2Rγc:

Interleukin-2 receptor common gamma chain

Kd:

Dissociation constant

LDH:

Lactate dehydrogenase

LDL:

Low-density lipoprotein

LDLR:

Low-density lipoprotein receptor

Lf:

Lactoferrin

LfR:

Lactoferrin receptor

LRP:

Low-density lipoprotein receptor-related protein

MIDAS:

Metal ion-dependent adhesion Site

mPEG:

Methoxy polyethylene glycol

MTT:

(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide

NPs:

Nanoparticles

PE:

Paired end

PEG:

Polyethylene glycol

PI3 kinase:

Phosphoinositide-3-kinase

PLA:

Poly lactic acid

PTX:

Paclitaxel

RAP:

Receptor-associated protein

RGD:

Arginine–glycine–aspartic acid

RNA:

Ribonucleic acid

STAT 6:

Signal transducer and activator of transcription 6

Tf:

Transferrin

TPGS:

D-ɑ-tocopheryl polyethylene glycol succinate

VLDLR:

Very low-density lipoprotein receptor

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    Authors and Affiliations

    1. Department of Pharmaceutical Sciences &Technology, Institute of Chemical Technology, Matunga, Mumbai, India

      Rijo John & Heero Vaswani

    2. Department of Pharmaceutical Sciences, Insitute of Chemical Technology, Deemed University, Elite Status and Centre of Excellence, Government of Maharashtra, Mumbai, India

      Prajakta Dandekar & Padma V. Devarajan

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    1. Rijo John
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    3. Prajakta Dandekar
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    4. Padma V. Devarajan
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    Correspondence to Padma V. Devarajan .

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    1. Department of Pharmaceutical Sciences, Insitute of Chemical Technology Deemed University, Elite Status and Centre of Excellence Government of Maharashtra, Mumbai, India

      Padma V. Devarajan

    2. Department of Pharmaceutical Sciences, Insitute of Chemical Technology Deemed University, Elite Status and Centre of Excellence Government of Maharashtra, Mumbai, India

      Prajakta Dandekar

    3. Piramal Enterprises Limited, Pharmaceutical R&D, Mumbai, India

      Anisha A. D'Souza

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    John, R., Vaswani, H., Dandekar, P., Devarajan, P.V. (2019). Brain Cancer Receptors and Targeting Strategies. In: Devarajan, P., Dandekar, P., D'Souza, A. (eds) Targeted Intracellular Drug Delivery by Receptor Mediated Endocytosis. AAPS Advances in the Pharmaceutical Sciences Series, vol 39. Springer, Cham. https://doi.org/10.1007/978-3-030-29168-6_2

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