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Introduction
Published in Malgorzata Lekka, Cellular Analysis by Atomic Force Microscopy, 2017
Based on single-cell deformability measurements, it has been found that cell structure is closely related to specific mechanical properties, which, in turn, depend on the organization of cell cytoskeleton. The role of cytoskeletal components (mainly actin filaments and microtubules) in cellular deformability has been shown by applying so-called cytoskeletal drugs that influence the structure and formation of each particular component [13, 14, and 15]. For example, cytochalasin D increases the cellular deformability while nocodazol leads to cell stiffening. A summary of cytoskeletal drugs influence on cellular deformability is presented in Table 1.1. Depending on the type of the compounds, disrupting or stabilizing particular cytoskeletal elements, the influence on cellular deformability manifests either in higher or in lower deformability (cells become softer or more rigid, respectively). However, it should be underlined that the effect is dependent on the applied concentration and time of action.
An overview of the recent progress in Middle East Respiratory Syndrome Coronavirus (MERS-CoV) drug discovery
Published in Expert Opinion on Drug Discovery, 2023
A cell-based enzyme-linked immunosorbent assay (ELISA) has been used to screen and evaluate many FDA-approved drugs for their ability to target MERS-CoV. The drugs include neurotransmitter blockers, DNA synthesis/repair inhibitors, lipid and sterol metabolism antagonists, estrogen receptor antagonists, protein-processing blockers, ion transport blockers, cytoskeletal drugs (particularly tubulin), kinase-signaling blockers, and apoptosis inhibitors [22]. Despite not having a clear connection to CoVs, two groups of pharmaceuticals – antiparasitics and antibiotics – showed effectiveness against MERS-CoV infection. Specifically, nocodazole acted on the cytoskeleton to halt spindle development. It is an antimitotic drug originally developed to fight cancer, but studies have shown that it is also highly effective against MERS-CoV [22,130]. Two of nine ion channel blockers tested, monensin and salinomycin sodium, had inhibitory effects against MERS-CoV. There is experimental evidence that MERS-CoV is vulnerable to ionophore activities [131]. The EC50 and CC50 values for monensin were 3.2 and greater than 20 µM, respectively [131]. Thus, it was effective against MERS-CoV at low concentrations and had little toxicity.
Simultaneous estimation of paclitaxel and erlotinib in plasma by liquid chromatography/(+) electrospray tandem mass spectrometry: application in formulation development and pharmacokinetics
Published in Drug Development and Industrial Pharmacy, 2022
Tahir Khuroo, Umme Atifa, Arshad Khuroo, Mohd Aamir Mirza, Asgar Ali, Zeenat Iqbal
Paclitaxel (PAC) is one of several cytoskeletal drugs that target tubulin. Paclitaxel-treated cells have defects in mitotic spindle assembly, chromosome segregation, and cell division. Unlike other tubulin-targeting drugs such as colchicines that inhibit microtubule assembly, paclitaxel stabilizes the microtubule and protects it from disassembly. Chromosomes are thus unable to achieve a metaphase spindle configuration. This blocks the progression of mitosis and prolonged activation of the mitotic checkpoint triggers apoptosis or reversion to the G-phase of the cell cycle without cell division [1]. Among the clinically-validated nanomedicines, only nanoparticle albumin-bound Paclitaxel (Pac) has become officially part of the first-line treatment of cancer [2,3].