P2.19 Aaptamine, Demethyloxyaaptamine, and Isoaaptamine: A Proteomic-Based Screening of Protein Targets in Cisplatin-Resistant Tumor Cells

Dyshlovoy, Sergey A.; Naeth, Ina; Venz, Simone; Fedorov, Sergey N.; Shubina, Larisa K.; Stonik, Valentin A.; Balabanov, Stefan; Honecker, Friedemann

doi:10.1016/s0923-7534(20)31342-9

Cited by 3 publications

(1 citation statement)

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“…11 Based on biochemical activity, Aaptamine can increase cofilin-1 concentration. 12 Cofilin-1 detach F-actin filament by using the actindepolymerizing factor (ADF), then it inhibits actin-myosin movement. 13 Increase of Cofilin-1 expression also inhibit Matrix Metalloprotein (MMP) activity, especially MMP-1, MMP-3, MMP-9.…”

Section: Discussionmentioning

confidence: 99%

Anti-migration Effect of Aaptos suberitoides Fraction in HCT-116 Colorectal Cancer Cell Line

Daffa

Bashari

Ariyanto

et al. 2021

AMJ

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Background: Colorectal cancer is the second leading cause of mortality and the most prevalent cancer worldwide. Most patients, who come with late-stage, have ineffective treatments and some side effects in chemotherapy. Aaptos suberitoides has potential anti-cancer effects due to its bioactive compounds such as aptamine. This study aimed to evaluate the migration inhibition effect of Aaptos suberitoides fraction in HCT-116 cell line.Methods: This study was an experimental study. Aaptos suberitoides specimen was taken in Tinjil Island and fractionated with ethyl acetate. HCT-116 cell line was added with Aaptos suberitoides fraction and cellular migration activity was observed in 48 hours of which the scratch assay was performed. The gap closure area was determined with ImageJ software.Results: The data showed that a low concentration of Aaptos suberitoides fraction inhibited migration activity in HCT-116 cell line as follow; 1 and 5 mg/L Aaptos suberitoides fraction inhibit 3-4 % cancer cell migration in 24 hours, and 10-11% inhibition in 48 hours, respectively. However, 10 mg/L fraction concentration only inhibited 7-14% of the migration effect.Conclusion: Aaptos suberitoides fraction suggests insignificant migration inhibition in colorectal cancer cells and only inhibits less than 15 % HCT-116 cell line.

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Section: Discussionmentioning

confidence: 99%

Anti-migration Effect of Aaptos suberitoides Fraction in HCT-116 Colorectal Cancer Cell Line

Daffa

Bashari

Ariyanto

et al. 2021

AMJ

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Synthese und Pharmakologie von Proteasom‐Inhibitoren

et al. 2013

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Schon kurz nach der Entdeckung des Proteasoms war klar, dass Proteasom‐Inhibitoren in der Lage sein sollten, Proteine zu stabilisieren, die zur Apoptose von Tumorzellen führen sollten. Die entscheidenden Fragen dabei war, ob es prinzipiell überhaupt möglich ist, das Proteasom zu inhibieren, ohne untragbare Nebenwirkungen hervorzurufen, und wie man zu solchen Inhibitoren gelangen könnte. Glücklicherweise stellt “Mutter Natur” eine ganze Bandbreite von verschiedenen Naturstoffen zur Verfügung, die selektiv und spezifisch das Proteasom inhibieren. Die chemische Synthese dieser Naturstoffe hat schließlich den Zugang zu deren Analoga und optimierten Wirkstoffen ermöglicht, von denen zwei bereits als Medikament zur Behandlung von Krebserkrankungen zugelassen sind. Trotz dieser Erfolge werden noch weitere Naturstoffe als Leitstrukturen bearbeitet, und wir werden deren biologisches Potenzial sowie die damit verbundenen Herausforderungen auf dem Gebiet der Synthese im Folgenden besprechen.

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Synthesis and Pharmacology of Proteasome Inhibitors

et al. 2013

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Shortly after the discovery of the proteasome it was proposed that inhibitors could stabilize proteins which ultimately would trigger apoptosis in tumor cells. The essential questions were whether small molecules would be able to inhibit the proteasome without generating prohibitive side effects and how one would derive these compounds. Fortunately, "Mother Nature" has generated a wide variety of natural products that provide distinct selectivities and specificities. The chemical synthesis of these natural products finally provided access to analogues and optimized drugs of which two different classes have been approved for the treatment of malignancies. Despite these achievements, additional lead structures derived from nature are under investigation and will be discussed with regard to their biological potential and chemical challenges.

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P2.19 Aaptamine, Demethyloxyaaptamine, and Isoaaptamine: A Proteomic-Based Screening of Protein Targets in Cisplatin-Resistant Tumor Cells

Cited by 3 publications

References 0 publications

Anti-migration Effect of Aaptos suberitoides Fraction in HCT-116 Colorectal Cancer Cell Line

Anti-migration Effect of Aaptos suberitoides Fraction in HCT-116 Colorectal Cancer Cell Line

Synthese und Pharmakologie von Proteasom‐Inhibitoren

Synthesis and Pharmacology of Proteasome Inhibitors

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