Abstract
Paclitaxel (PTX) has been used for cancer treatment for decades and has become one of the most successful chemotherapeutics in the clinic and financially. However, serious problems with its use still exist, owing to its poor solubility and non-selective toxicity. With respect to these issues, recent advances have addressed the water solubility and tumor specificity related to PTX application. Many measures have been proposed to remedy these limitations by enhancing tumor recognition via ligand-receptor-mediated targeting as well as other associated strategies. In this review, we investigated various kinds of ligands that have emerged as PTX tumor-targeting tools. In particular, this article highlights small molecule-, protein-, and aptamer-functionalized conjugates and nanoparticles (NPs), providing a promising approach for PTX-based individualized treatment prospects.
Highlights
Paclitaxel (PTX) is a natural terpenoid bearing a tricyclic skeleton
Antibody-drug conjugates (ADCs) perfectly combine monoclonal antibodies with an effective cytotoxic payload, making full use of the specific binding ability to the target of the former and overcoming defects such as the low efficacy of the former and the large side effects of the latter
One of the earliest studies on antibody–PTX conjugates was by Guillemard and Saragovi (2001), who found that several PTX–antibody conjugates have high aqueous solubility, excellent tumor target selectivity, and high therapeutic efficacy, affording more cytotoxicity than free PTX or a mixture of free PTX and the free antibody in vitro
Summary
Paclitaxel (PTX) is a natural terpenoid bearing a tricyclic skeleton. It is an alkaline power taxine after isolation from the leaves of the European yew, formerly performed by German scientist Lucas in 1865. Due to the high affinity of ligands to their targets, small molecule-drug conjugates (SMDCs) have successfully enhanced the specificity of the cytotoxic payload toward tumors.
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