Abstract
Cancer is one of the leading causes of death worldwide. The development of cancer-specific diagnostic agents and anticancer toxins would improve patient survival. The current and standard types of medical care for cancer patients, including surgery, radiotherapy, and chemotherapy, are not able to treat all cancers. A new treatment strategy utilizing tumor targeting peptides to selectively deliver drugs or applicable active agents to solid tumors is becoming a promising approach. In this review, we discuss the different tumor-homing peptides discovered through combinatorial library screening, as well as native active peptides. The different structure–function relationship data that have been used to improve the peptide’s activity and conjugation strategies are highlighted.
Highlights
Peptides are small molecules—often less than 40 amino acids in length—that are derived from natural or synthetic sources
We review here some of the recent advances in peptide-based delivery systems focusing on peptides for which the target protein is known and that target (i) brain tumors and BBB; (ii) tumor vasculature; (iii) cancer specific signatures involved in invasion and pre-metastatic niche formation; (iv) therapeutic peptides; and (v) cell and tumor penetrating peptides (Table 1)
Several native extracellular matrix (ECM) proteins, such as fibronectin [105,106,107,108,109], laminin [110], vitronectin [111], osteopontin [112], tenascin [113], collagens I, IV [114,115], and fibrinogen [116,117,118,119] interact with the integrin receptors including integrin αvβ3 through the RGD domain
Summary
Peptides are small molecules—often less than 40 amino acids in length—that are derived from natural or synthetic sources. In addition to integrins and other cell surface proteins, many intracellular proteins are often highly expressed on the surface of cancer cells and constitute molecular targets for phage displayed peptides [7,8,9,10] These peptides can act as carriers to deliver selectively and imaging agents, anticancer toxins, nanoparticles, and/or other applicable active agents to tumors. Due to several challenges associated with systemic therapy including non-specificity, low permeability and low retention, off-target toxicities, and in case of brain tumors, inability to cross the blood–brain–barrier (BBB), an efficient and viable strategy that would increase the delivery capacity of anticancer cargoes into the target site without compromising the drug’s efficacy would open many new avenues for targeted drug delivery PET imaging, SPECT imaging, chemotherapy, Chemotherapy, radiotherapy, Reference [8]
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