TMC120 displayed potent cytotoxic effect on human cervical carcinoma through enhancing the polymerization of microtubules

Shi, Lili; Yu, Li; Zhong, Desheng; Gu, Chunping; Lv, Longyun; Zeng, Xianmin; Yao, Xingang; Li, Lin; Liu, Shuwen

doi:10.1097/qad.0000000000001808

Cited by 2 publications

(2 citation statements)

References 32 publications

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“… 12 Studies have shown that TMC120 displayed potent cytotoxic effect on human cervical carcinoma through enhancing the polymerization of microtubules, thus can be used as a potential chemoprophylactic and therapeutic agent for cervical cancers in the similar manner as paclitaxel and TMC120 is also suitable for preventing HIV infection and cervical cancer in women. 13 The sensitivity of primary tumor cell from patients with cervical cancer to eight chemotherapeutic combinations were as follows: gemcitabine < docetaxel < topotecan + cisplatin < cisplatin + cyclophosphamide + doxorubicin < gemcitabine + cisplatin < taxol < taxol + carboplatin < taxol + cisplatin. 14 However, most existing anticancer drugs have strong side effects making them unable to reach tumor tissues effectively, which requires the development of effective anticancer drugs that can be specifically or selectively delivered to tumor tissues.…”

Section: Introductionmentioning

confidence: 99%

A study on screening and antitumor effect of CD55-specific ligand peptide in cervical cancer cells

Li¹,

Yin²,

Ji³

et al. 2018

DDDT

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BackgroundTo improve the targeting ability of antitumor drugs, we identified the antigens with high expression on the surface of tumor cells associated with tumor escape, such as the complement regulatory protein CD55 molecule, which is also known as the decay accelerating factor. In this study, phage display technology was used to screen and identify CD55-specific ligand peptide (CD55sp) bound to CD55 molecule on the surface of cervical cancer HeLa cells. We then explored the role of this peptide in inhibiting the growth of cervical cancer cells in vitro. Our characterization of CD55sp will provide implication for tumor target therapy.MethodsThe phage bound to the surface of HeLa cells were isolated by phage display technology. Positive phage clones were identified by ELISA. Phage was then amplified and determined by agarose gel electrophoresis after monoclonal DNA extraction. DNA sequencing and bioinformatical analysis were conducted to obtain specific ligand peptides. Flow cytometry and immunofluorescence were used to measure the expression of CD55 molecule on the surface of tumor and normal cells. Subsequently, the effects of CD55sp on the proliferation and apoptosis of HeLa and SiHa cells were determined by Cell Counting Kit-8 (CCK-8), flow cytometry, and TUNEL assay, respectively. The morphology of apoptotic cells was examined by electron microscope. The distribution of Cleaved caspase-3 was detected by immunofluorescence. The expression of bcl-2 and Cleaved caspase-3 were determined by Western blot.ResultsThe results showed that the peptide (QVNGLGERSQQM) can bind to the CD55 molecule on the surface of cervical cancer HeLa and SiHa cells as a ligand peptide. It can also effectively inhibit the proliferation of cervical cancer cells and induce cell apoptosis.ConclusionThis study demonstrates that CD55sp screened by phage display technology plays a strong antitumor role.

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Section: Introductionmentioning

confidence: 99%

A study on screening and antitumor effect of CD55-specific ligand peptide in cervical cancer cells

Li¹,

Yin²,

Ji³

et al. 2018

DDDT

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“…Enediynes, containing pentafluorophenylsulfoxide, have antiproliferative activity against human cancer cells which is associated with their ability to compromise the MT network (Borie et al, 2018). TMC120 is a potential anticancer drug candidate that enhances MT polymerization, followed by mitotic arrest, and abnormal mitotic spindles (Shi et al, 2018). SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor with antitumor efficiency.…”

Section: Mt In Cancermentioning

confidence: 99%

Microtubules: From understanding their dynamics to using them as potential therapeutic targets

Ilan

2018

Journal Cellular Physiology

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Microtubules (MT) and actin microfilaments are dynamic cytoskeleton components involved in a range of intracellular processes. MTs play a role in cell division, beating of cilia and flagella, and intracellular transport. Over the past decades, much knowledge has been gained regarding MT function and structure, and its role in underlying disease progression. This makes MT potential therapeutic targets for various disorders. Disturbances in MT and their associated proteins are the underlying cause of diseases such as Alzheimer’s disease, cancer, and several genetic diseases. Some of the advances in the field of MT research, as well as the potenti G beta gamma, is needed al uses of MT‐targeting agents in various conditions have been reviewed here.

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TMC120 displayed potent cytotoxic effect on human cervical carcinoma through enhancing the polymerization of microtubules

Abstract: TMC120 is a potential chemoprophylactic and therapeutic agent for cervical cancers in a manner similar to paclitaxel, and could be suitable for helping healthy women to prevent HIV infection and cervical cancer.

Cited by 2 publications

References 32 publications

A study on screening and antitumor effect of CD55-specific ligand peptide in cervical cancer cells

A study on screening and antitumor effect of CD55-specific ligand peptide in cervical cancer cells

Microtubules: From understanding their dynamics to using them as potential therapeutic targets

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