Rational design of water-dispersible and biocompatible nanoprobes with H2S-triggered NIR emission for cancer cell imaging

2020 ◽  
Vol 8 (28) ◽  
pp. 6013-6016
Author(s):  
Hengyan Liu ◽  
Ge Xu ◽  
Tianli Zhu ◽  
Rongchen Wang ◽  
Jiahui Tan ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cancer Cell ◽  
Small Molecule ◽  
Rational Design ◽  
Cell Imaging ◽  
Imaging Modality ◽  
Aqueous Solubility ◽  
Water Dispersible ◽  
Nir Emission ◽  
Small Molecule Probe

A nanoprobe with good aqueous solubility and biocompatibility by trapping an H2S-activatable small molecule probe in the interior of surface cross-linked micelles was fabricated for imaging of H2S-rich cancer cells in a dual-color imaging modality.

Supramolecular enhancement of aggregation-induced emission and its application in cancer cell imaging

2014 ◽  
Vol 2 (32) ◽  
pp. 6609-6617 ◽  
Author(s):  
Guocan Yu ◽  
Guping Tang ◽  
Feihe Huang
Keyword(s):  
Ternary System ◽  
Cancer Cells ◽  
Cancer Cell ◽  
Cell Imaging ◽  
Imaging Agent ◽  
Aggregation Induced Emission ◽  
Cancer Cell Imaging

A ternary system of two tetraphenylethene derivatives containing naphthalene and paraquat groups, respectively, and a pillar[6]arene is utilized as an imaging agent for cancer cells.

scholarly journals Targeting cancer cell metabolism with mitochondria-immobilized phosphorescent cyclometalated iridium(iii) complexes

2017 ◽  
Vol 8 (1) ◽  
pp. 631-640 ◽  
Author(s):  
Jian-Jun Cao ◽  
Cai-Ping Tan ◽  
Mu-He Chen ◽  
Na Wu ◽  
De-Yang Yao ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cancer Cell ◽  
Rational Design ◽  
Cell Metabolism ◽  
Mitochondrial Metabolism ◽  
Cancer Cell Metabolism

We report a rational design and mechanism studies of mitochondria-immobilized iridium(iii) complexes that can kill cancer cells by targeting mitochondrial metabolism.

scholarly journals Novel oligopeptide nanoprobe for targeted cancer cell imaging

RSC Advances ◽  
2018 ◽  
Vol 8 (54) ◽  
pp. 30887-30893 ◽  
Author(s):  
Wen-Qiang Ding ◽  
Si-Yong Qin ◽  
Yin-Jia Cheng ◽  
Yi-Han Ma ◽  
Ai-Qing Zhang
Keyword(s):  
Cancer Cells ◽  
Cancer Cell ◽  
Cell Imaging ◽  
Cancer Cell Imaging

Co-assembly of WFFW tetrapeptide and RGDWFFW heptapeptide generated the photostable and fluorescence-tunable nanoprobe, which could selectively image the cancer cells.

Highly efficient near-infrared organic dots based on novel AEE fluorogen for specific cancer cell imaging

RSC Advances ◽  
2015 ◽  
Vol 5 (46) ◽  
pp. 36837-36844 ◽  
Author(s):  
Yan Zhang ◽  
Kaiwen Chang ◽  
Bin Xu ◽  
Jinlong Chen ◽  
Lulin Yan ◽  
...  
Keyword(s):  
Quantum Efficiency ◽  
Cancer Cell ◽  
Small Molecule ◽  
Near Infrared ◽  
Cell Imaging ◽  
Amphiphilic Polymer ◽  
Cancer Cell Imaging ◽  
Highly Efficient ◽  
Specific Cancer ◽  
High Fluorescence

Near-infrared emissive organic dots with a high fluorescence quantum efficiency (AEE dots) are prepared by using an amphiphilic polymer PSMA and a novel small molecule fluorogen (DPPBPA).

scholarly journals A rational design of a cancer-specific and lysosome-targeted fluorescence nanoprobe for glutathione imaging in living cells

2020 ◽  
Vol 1 (6) ◽  
pp. 1739-1744
Author(s):  
Hong Wang ◽  
Peisheng Zhang ◽  
Chonghua Zhang ◽  
Shu Chen ◽  
Rongjin Zeng ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cancer Cell ◽  
Rational Design ◽  
Living Cells ◽  
Dual Targeting ◽  
Fluorescence Nanoprobe

A dual-targeting (both cancer cell- and lysosome-targeting) fluorescence nanoprobe was rational designed and synthesized for the efficient imaging of lysosomal GSH in cancer cells.

Orally administrative melk (maternal embryonic leucine zipper kinase)-targeting small molecule inhibitor suppresses the growth of various types of human cancer.

2013 ◽  
Vol 31 (15_suppl) ◽  
pp. e13569-e13569
Author(s):  
Suyoun Chung ◽  
Hanae Suzuki ◽  
Takashi Miyamoto ◽  
Naofumi Takamatsu ◽  
Ayako Tatsuguchi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Cancer Cell ◽  
Small Molecule ◽  
Breast Cancer Cells ◽  
Leucine Zipper ◽  
Human Cancer ◽  
Tumor Initiating Cells ◽  
Mammosphere Formation ◽  
Intravenous And Oral Administration

e13569 Background: We previously reported MELK (maternal embryonic leucine zipper kinase) as a novel therapeutic target for breast cancer. MELK was also highly upregulated in multiple types of cancer including prostate, pancreas and lung cancers, and plays indispensable roles in cancer cell survival, particularly in the maintenance of tumor-initiating cells. In this study, we attempted to identify novel substrates of MELK and develop the small-molecule MELK inhibitor. Methods: To elucidate the MELK signaling pathway in breast cancer cells, we screened MELK substrates by 2D-PAGE and mass spectrometric analysis, and characterized two of them for their roles in mammary carcinogenesis. Furthermore, we conducted a high-throughput screening of a compound library followed by structure-activity relationship studies. We investigated the growth suppressive effect of a MELK inhibitor OTSSP167 using xenograft models in mice and a mammosphere-formation assay. Results: We identified two novel MELK substrates, DBNL and PSMA1, which plays critical roles in invasiveness of cancer cells and maintenance of mammary tumor-initiating cells. We successfully obtained a highly potent MELK inhibitor OTSSP167 with IC50 of 0.41 nM. OTSSP167 inhibited the phosphorylation of these two substrates by MELK as well as mammosphere formation of breast cancer cells, and exhibited strong tumor-growth suppressive effects on xenografts of human breast, lung, prostate, and pancreas cancer cell lines in mice by both intravenous and oral administration. Conclusions: Orally administrative MELK inhibitor OTSSP167 is a promising compound to treat various types of human cancer. This compound can inhibit the phosphorylation of MELK substrates and also suppresses the formation of cancer stem cells in breast cancer cells, providing a novel strategy to cure cancer.

scholarly journals Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers

2016 ◽  
Vol 113 (7) ◽  
pp. 1778-1783 ◽  
Author(s):  
Edouard Mullarky ◽  
Natasha C. Lucki ◽  
Reza Beheshti Zavareh ◽  
Justin L. Anglin ◽  
Ana P. Gomes ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Small Molecule ◽  
Cancer Cell Lines ◽  
Small Molecule Inhibitor ◽  
Genetic Ablation ◽  
Molecule Inhibitor ◽  
Phosphoglycerate Dehydrogenase ◽  
Serine Biosynthesis

Cancer cells reprogram their metabolism to promote growth and proliferation. The genetic evidence pointing to the importance of the amino acid serine in tumorigenesis is striking. The gene encoding the enzyme 3-phosphoglycerate dehydrogenase (PHGDH), which catalyzes the first committed step of serine biosynthesis, is overexpressed in tumors and cancer cell lines via focal amplification and nuclear factor erythroid-2-related factor 2 (NRF2)-mediated up-regulation. PHGDH-overexpressing cells are exquisitely sensitive to genetic ablation of the pathway. Here, we report the discovery of a selective small molecule inhibitor of PHGDH, CBR-5884, identified by screening a library of 800,000 drug-like compounds. CBR-5884 inhibited de novo serine synthesis in cancer cells and was selectively toxic to cancer cell lines with high serine biosynthetic activity. Biochemical characterization of the inhibitor revealed that it was a noncompetitive inhibitor that showed a time-dependent onset of inhibition and disrupted the oligomerization state of PHGDH. The identification of a small molecule inhibitor of PHGDH not only enables thorough preclinical evaluation of PHGDH as a target in cancers, but also provides a tool with which to study serine metabolism.

scholarly journals Piperidone Analogue of Curcumin-loaded HPβ-cyclodextrin liposomes as delivery system for human cancer therapy

2017 ◽  
Vol 1 (3) ◽  
Author(s):  
S. Alhabardi, A. Aboussekhra, A. Alshamsan, A. Alomrani
Keyword(s):  
Breast Cancer ◽  
Colon Cancer ◽  
Particle Size ◽  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Delivery System ◽  
Annexin V ◽  
Aqueous Solubility ◽  
Anti Cancer

Cancer is a broad term used to describe different types of tumors affecting various parts of the human body. The resistance to multiple therapeutic agents, toxicity to healthy tissues, and lack of effective therapies obligate scientists to keep looking for new agents. Curcumin (diferuloylmethane) is a natural product. It has been reported that curcumin has anti-inflammatory, anti-diabetic, and anti-cancer effects. However, clinical use of curcumin is limited due to its poor aqueous solubility. Recently, a curcumin analogue, 5-Bis (4-hydroxy-3-methoxybenzylidene)-N-methyl-4-piperidone of curcumin (PAC), was synthesized to overcome this limitation. This compound showed significantly higher anticancer activity on breast cancer cell lines and colon cancer cell lines as compared to native curcumin. However, aqueous solubility of this new chemical compound limited its use and application. Liposomes were found to be the most promising system to use to overcome aqueous solubility and delivery limitations. Liposomes are a self-assembly of phospholipid molecules. They are biodegradable, biocompatible, and nontoxic carrier systems. These features make liposomes an ideal carrier system for anticancer agents. In this study liposomes were utilized to overcome PAC limitations. This project was designed to develop liposomal delivery system for PAC for cancer treatment and evaluate the anti-cancer properties of this system. Liposomal PAC formulae were prepared by the film hydration method and were optimized by adding hydroxypropyl-beta-cyclodextrin (HPβCD) and characterized in term of particle size, entrapment efficiency, release profile and cytotoxic activity. Liposomes with an average size below 150 nm and zwitterionic charge were obtained. Indeed, no major differences were seen in particle size and surface charge. However, HPβCD inclusion gave satisfied incorporation capacity reaching 68.1%. In addition, HPβCD inclusion in the liposomes resulted in increased in vitro release rate compared to conventional liposomes. On colon cancer cells, Annexin V/PI- Flow Cytometery cytotoxicity results revealed that the PAC-loaded HPβ-cyclodextrin liposomes trigger apoptosis by 75% in response (10 µM), whereas it was only 43% in response to the same concentration of PAC conventional liposomes, which confirmed their potential anti-cancer activity. On breast cancer cells, Annexin V/PI- Flow Cytometery cytotoxicity results showed that while PAC conventional liposomes have only minor cytotoxic effect (22-25%), PAC-loaded HPβCD liposomes induced 53% and 70% apoptosis in response to 5 µM and 10 µM, respectively. The cytotoxicity of PAC-loaded HPβ-cyclodextrin liposomes was more pronounced than PAC conventional liposomes in both cells, suggesting the benefits of using HPβ-cyclodextrin. Therefore, PAC-loaded HPβ-cyclodextrin liposomes indicate significant potential as delivery vehicles for the treatment of cancers.

scholarly journals A novel small molecule LLL12B inhibits STAT3 signaling and sensitizes ovarian cancer cell to paclitaxel and cisplatin

2020 ◽  
Author(s):  
Ruijie Zhang ◽  
Xiaozhi Yang ◽  
Dana M. Roque ◽  
Chenglong Li ◽  
Jiayuh Lin
Keyword(s):  
Ovarian Cancer ◽  
Cell Viability ◽  
Cancer Cells ◽  
Cancer Cell ◽  
Small Molecule ◽  
Ovarian Cancer Cells ◽  
Human Ovarian Cancer ◽  
Inhibitory Effects ◽  
Stat3 Signaling ◽  
Stat3 Phosphorylation

AbstractOvarian cancer is the fifth most common cause of cancer deaths among American women. Platinum and taxane combination chemotherapy represents the first-line approach for ovarian cancer, but treatment success is often limited by chemoresistance. Therefore, it is necessary to find new drugs to sensitize ovarian cancer cells to chemotherapy. Persistent activation of Signal Transducer and Activator of Transcription 3 (STAT3) signaling plays an important role in oncogenesis. Using a novel approach called advanced multiple ligand simultaneous docking (AMLSD), we developed a novel nonpeptide small molecule, LLL12B, which targets the STAT3 pathway. In this study, LLL12B inhibited STAT3 phosphorylation (tyrosine 705) and the expression of its downstream targets, which are associated with cancer cell proliferation and survival. We showed that LLL12B also inhibits cell viability, migration, and proliferation in human ovarian cancer cells. LLL12B combined with either paclitaxel or with cisplatin demonstrated synergistic inhibitory effects relative to monotherapy in inhibiting cell viability and LLL12B-paclitaxel or LLL12B-cisplatin combination exhibited greater inhibitory effects than cisplatin- paclitaxel combination in ovarian cancer cells. Furthermore, LLL12B-paclitaxel or LLL12B-cisplatin combination showed more significant in inhibiting cell migration and growth than monotherapy in ovarian cancer cells. In summary, our results support the novel small molecule LLL12B as a potent STAT3 inhibitor in human ovarian cancer cellsand suggest that LLL12B in combination with the current front-line chemotherapeutic drugs cisplatin and paclitaxel may represent a promising approach for ovarian cancer therapy.

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