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25 Results Found

  • Article
  • Open Access
15 Citations
3,972 Views
16 Pages

Cantharidin and Its Analogue Norcantharidin Inhibit Metastasis—Inducing Genes S100A4 and MACC1

  • Paul Curtis Schöpe,
  • Viktoria Zinnow,
  • Muhammad Ahtisham Ishfaq,
  • Janice Smith,
  • Pia Herrmann,
  • Robert H. Shoemaker,
  • Wolfgang Walther and
  • Ulrike Stein

Colorectal cancer (CRC) is the third most prevalent and second deadliest cancer worldwide. In addition, metastasis directly causes up to 90% of all CRC deaths, highlighting the metastatic burden of the disease. Biomarkers such as S100A4 and MACC1 aid...

  • Article
  • Open Access
4 Citations
1,631 Views
19 Pages

Evaluation of a Norcantharidin Nanoemulsion Efficacy for Treating B16F1-Induced Melanoma in a Syngeneic Murine Model

  • Gabriel Martínez-Razo,
  • Patrícia C. Pires,
  • Angélica Avilez-Colin,
  • María Lilia Domínguez-López,
  • Francisco Veiga,
  • Eliezer Conde-Vázquez,
  • Ana Cláudia Paiva-Santos and
  • Armando Vega-López

30 January 2025

Melanoma, a lethal type of cancer originating from melanocytes, is the leading cause of death among skin cancers. While surgical excision of the lesions is the primary treatment for melanoma, not all cases are candidates for surgical procedures. New...

  • Review
  • Open Access
12 Citations
3,281 Views
23 Pages

10 November 2022

Cantharidin (CTD) is the main active ingredient isolated from Mylabris, and norcantharidin (NCTD) is a demethylated derivative of CTD, which has similar antitumor activity to CTD and lower toxicity than CTD. However, the clinical use of NCTD is limit...

  • Article
  • Open Access
24 Citations
6,030 Views
10 Pages

Facile Chemical Access to Biologically Active Norcantharidin Derivatives from Biomass

  • Konstantin I. Galkin,
  • Fedor A. Kucherov,
  • Oleg N. Markov,
  • Ksenia S. Egorova,
  • Alexandra V. Posvyatenko and
  • Valentine P. Ananikov

12 December 2017

Reductive amination of 2,5-diformylfuran (DFF) was used to implement the transition from bio-derived 5-hydroxymethylfurfural (HMF) to pharmaceuticals. The synthesized bis(aminomethyl)furans were utilized as building blocks for the construction of new...

  • Article
  • Open Access
12 Citations
2,915 Views
18 Pages

Norcantharidin Nanoemulsion Development, Characterization, and In Vitro Antiproliferation Effect on B16F1 Melanoma Cells

  • Gabriel Martínez-Razo,
  • Patrícia C. Pires,
  • María Lilia Domínguez-López,
  • Francisco Veiga,
  • Armando Vega-López and
  • Ana Cláudia Paiva-Santos

28 March 2023

Melanoma is a highly lethal type of cancer that has had an increase in incidence in the last decades. Nevertheless, current therapies lack effectiveness and have highly disabling side effects, which calls for new therapeutic strategies. Norcantharidi...

  • Article
  • Open Access
11 Citations
3,826 Views
11 Pages

Norcantharidin Suppresses YD-15 Cell Invasion Through Inhibition of FAK/Paxillin and F-Actin Reorganization

  • Kyoung-Ok Hong,
  • Chi-Hyun Ahn,
  • In-Hyoung Yang,
  • Jung-Min Han,
  • Ji-Ae Shin,
  • Sung-Dae Cho and
  • Seong Doo Hong

Norcantharidin (NCTD), a demethylated derivative of cantharidin, has been reported to exhibit activity against various types of cancers. However, the anti-invasive effects of NCTD and its molecular mechanism in human mucoepidermoid carcinoma (MEC) re...

  • Article
  • Open Access
30 Citations
3,548 Views
16 Pages

Norcantharidin Induces Immunogenic Cell Death of Bladder Cancer Cells through Promoting Autophagy in Acidic Culture

  • Lili Xu,
  • Bijia Su,
  • Lijun Mo,
  • Chenye Zhao,
  • Zhenlin Zhao,
  • Hongwei Li,
  • Zhiming Hu and
  • Jinlong Li

The acidic tumor microenvironment stands as a major obstacle to the efficient elimination of tumor cells. Norcantharidin (NCTD) is a powerful antitumor agent with multiple bioactivities. However, the effect of NCTD under acidic conditions is still un...

  • Article
  • Open Access
1,215 Views
29 Pages

Melanoma is a highly aggressive skin cancer with limited therapeutic response. Targeting intracellular signaling pathways and promoting tumor cell differentiation are promising therapeutic strategies. Pentoxifylline (PTX) and norcantharidin (NCTD) ha...

  • Article
  • Open Access
17 Citations
3,833 Views
13 Pages

Contribution of p38 MAPK Pathway to Norcantharidin-Induced Programmed Cell Death in Human Oral Squamous Cell Carcinoma

  • Chi-Hyun Ahn,
  • Kyoung-Ok Hong,
  • Bohwan Jin,
  • WonWoo Lee,
  • Yun Chan Jung,
  • Hakmo Lee,
  • Ji-Ae Shin,
  • Sung-Dae Cho and
  • Seong Doo Hong

Norcantharidin (NCTD), a demethylated analog of cantharidin isolated from blister beetles, has been used as a promising anticancer agent; however, the underlying function of NCTD against human oral squamous cell carcinoma (OSCC) has not been fully un...

  • Article
  • Open Access
4 Citations
2,245 Views
21 Pages

Exploring the Anti-Colorectal Cancer Mechanism of Norcantharidin Through TRAF5/NF-κB Pathway Regulation and Folate-Targeted Liposomal Delivery

  • Fanqin Zhang,
  • Xiaodong Chen,
  • Chuanqi Qiao,
  • Siyun Yang,
  • Yiyan Zhai,
  • Jingyuan Zhang,
  • Keyan Chai,
  • Haojia Wang,
  • Jiying Zhou and
  • Jiarui Wu
  • + 1 author

9 February 2025

Colorectal cancer is one of the most common malignant tumors worldwide, significantly impacting human health. Cantharidin (CTD), an active compound derived from the Spanish fly, exhibits antitumor properties. Its derivative, norcantharidin (NCTD), is...

  • Article
  • Open Access
10 Citations
6,352 Views
17 Pages

2 December 2015

Based on the structure of naturally produced cantharidin, different arylamine groups were linked to the norcantharidin scaffold to provide thirty six compounds. Their structures were confirmed by melting point, 1H-NMR, 13C-NMR and HRMS-ESI studies. T...

  • Brief Report
  • Open Access
2 Citations
1,710 Views
9 Pages

Pentoxifylline and Norcantharidin Modify p62 Expression in 2D and 3D Cultures of B16F1 Cells

  • José Luis González-Quiroz,
  • Juan Moisés Ocampo-Godínez,
  • Victoria Noemi Hernández-González,
  • Ruth Angélica Lezama,
  • Elba Reyes-Maldonado,
  • Armando Vega-López and
  • María Lilia Domínguez-López

Three-dimensional cell cultures have improved the evaluation of drugs for cancer therapy, due to their high similarity to solid tumors. In melanoma, autophagy appears to show a dual role depending on the progression of the disease. p62 protein has be...

  • Article
  • Open Access
5 Citations
3,183 Views
21 Pages

Norcantharidin (NCTD), a cantharidin derivative, induces ROS generation and is widely used to treat CRC. In this study, we clarified the role and mechanism of action of norcantharidin in increasing CRC sensitivity to radiotherapy. We treated the CRC...

  • Short Note
  • Open Access
1 Citations
922 Views
5 Pages

3-([4-(Acetylamino)phenyl]methoxy-1-carbonyl)-7-oxabicyclo[2.2.1]heptane-2-carboxylic Acid

  • Kathryn N. Mayeaux,
  • Bailey N. Baxter,
  • Hannah K. Lawley,
  • Caleb N. Lopansri,
  • Mary Helene Marmande,
  • Lucy A. Orr and
  • David C. Forbes

30 August 2025

Overexpression of protein phosphatase 5 (PP5) is linked to tumor cell growth, making it a candidate for small-molecule drug therapy. Since the PP2A domain has been selectively inhibited using functionalized scaffolds that maximize contacts, a similar...

  • Article
  • Open Access
5 Citations
2,061 Views
18 Pages

15 November 2023

Objective: The objective of this study was to examine the preparation process of DSPE-PEG-C60/NCTD micelles and assess the impact of fullerenol (C60)-modified micelles on the nephrotoxicity and antitumor activity of NCTD. Method: The micelles contain...

  • Short Note
  • Open Access
74 Views
5 Pages

Methyl 2-(Chloromethoxy-1-carbonyl)-7-oxabicyclo[2.2.1]heptane-3-carboxylate

  • Hannah K. Lawley,
  • Bailey N. Baxter,
  • Caleb N. Lopansri,
  • Mary Helene Marmande,
  • Kathryn N. Mayeaux,
  • Lucy A. Orr and
  • David C. Forbes

13 January 2026

Overexpression of protein phosphatase 5 (PP5) is implicated in tumor cell growth, establishing PP5 as a compelling target for small-molecule anticancer therapy. Building on prior success in achieving selectivity within the PP2A domain through scaffol...

  • Article
  • Open Access
3 Citations
2,201 Views
19 Pages

Tumor-Infiltrating iNKT Cells Activated through c-Kit/Sca-1 Are Induced by Pentoxifylline, Norcantharidin, and Their Mixtures for Killing Murine Melanoma Cells

  • Maximiliano V. M. Correa-Lara,
  • Israel Lara-Vega,
  • Minerva Nájera-Martínez,
  • María Lilia Domínguez-López,
  • Elba Reyes-Maldonado and
  • Armando Vega-López

16 October 2023

The involvement of NK and other cytotoxic cells is considered the first defense line against cancer. However, a significant lack of information prevails on the possible roles played by factors considered characteristic of primitive cells, such as c-k...

  • Short Note
  • Open Access
1 Citations
2,073 Views
6 Pages

2-Furanylmethyl N-(2-propenyl)carbamate

  • Noah C. Baker,
  • Abby L. Mock,
  • Ivy B. Nguyen,
  • Savan D. Patel and
  • David C. Forbes

1 December 2022

The overexpression of protein phosphatase 5 (PP5) has been correlated to tumor cell reproduction, making it a candidate for small molecule drug therapy. Prior work has focused on functionalized and decorated scaffolds that maximize contacts within an...

  • Article
  • Open Access
7 Citations
2,422 Views
13 Pages

Norcantharidin Enhances the Antitumor Effect of 5-Fluorouracil by Inducing Apoptosis of Cervical Cancer Cells: Network Pharmacology, Molecular Docking, and Experimental Validation

  • Yong Huang,
  • Xin-Wei Wan,
  • Yu-Tong Du,
  • Yue Feng,
  • Lin-Sen Yang,
  • Yong-Bin Liu,
  • Tian Chen,
  • Zhuan Zhu,
  • Yi-Ting Xu and
  • Cheng-Cheng Wang

The high recurrence rate of cervical cancer is a leading cause of cancer deaths in women. 5-Fluorouracil (5-FU) is an antitumor drug used to treat many types of cancer, but its diminishing effectiveness and side effects limit its use. Norcantharidin...

  • Article
  • Open Access
9 Citations
2,606 Views
12 Pages

Inhibition of MZF1/c-MYC Axis by Cantharidin Impairs Cell Proliferation in Glioblastoma

  • Chie-Hong Wang,
  • Hsuan-Cheng Wu,
  • Chen-Wei Hsu,
  • Yun-Wei Chang,
  • Chiung-Yuan Ko,
  • Tsung-I Hsu,
  • Jian-Ying Chuang,
  • Tsui-Hwa Tseng and
  • Shao-Ming Wang

25 November 2022

Myeloid zinc finger 1 (MZF1), also known as zinc finger protein 42, is a zinc finger transcription factor, belonging to the Krüppel-like family that has been implicated in several types of malignancies, including glioblastoma multiforme (GBM). M...

  • Review
  • Open Access
16 Citations
6,229 Views
24 Pages

Norbornene and Related Structures as Scaffolds in the Search for New Cancer Treatments

  • Gorka Calvo-Martín,
  • Daniel Plano,
  • Nuria Martínez-Sáez,
  • Carlos Aydillo,
  • Esther Moreno,
  • Socorro Espuelas and
  • Carmen Sanmartín

25 November 2022

The norbornene scaffold has arisen as a promising structure in medicinal chemistry due to its possible therapeutic application in cancer treatment. The development of norbornene-based derivatives as potential chemotherapeutic agents is attracting sig...

  • Article
  • Open Access
28 Citations
8,151 Views
16 Pages

20 December 2012

Cantharidin is a natural compound of novel structure with ideal insecticidal activity. However, the relationship of structure to insecticidal activity of cantharidin and its derivatives has not been ever clarified. To explore what determines the inse...

  • Article
  • Open Access
9 Citations
2,813 Views
13 Pages

8 October 2020

The American cockroach, Periplaneta americana (L.), is a notorious urban pest. It has developed insecticidal resistance to commonly used insecticides. Cantharidin (CTD) is a defensive toxin derived from blister beetles. It has been verified to have i...

  • Article
  • Open Access
4 Citations
6,346 Views
13 Pages

16 December 2013

Protein phosphatase 5 (PP5) is a unique member of serine/threonine phosphatases which has been recognized in regulation of diverse cellular processes. A cDNA fragment encoding PP5 (EcPP5) was cloned and characterized from the cantharidin-producing b...

  • Review
  • Open Access
7 Citations
3,108 Views
23 Pages

Dissecting the Puzzling Roles of FAM46C: A Multifaceted Pan-Cancer Tumour Suppressor with Increasing Clinical Relevance

  • Giancarlo Lai,
  • Federica De Grossi,
  • Ilaria Catusi,
  • Elisa Pesce and
  • Nicola Manfrini

27 April 2024

FAM46C is a well-established tumour suppressor with a role that is not completely defined or universally accepted. Although FAM46C expression is down-modulated in several tumours, significant mutations in the FAM46C gene are only found in multiple my...