Differences in the Intracellular Localization of Methylated β-Cyclodextrins-Threaded Polyrotaxanes Lead to Different Cellular States

Today's cyclodextrin, ,

Today’s cyclodextrin is an essential paper on understanding differences in internalization and cellular location of various polyrotaxanes by Hokkaido University, Japan Science and Technology Agency (JST) and Tokyo Medical and Dental University

Activation of autophagy represents a potential therapeutic strategy for the treatment of diseases that are caused by the accumulation of defective proteins and the formation of abnormal organelles. Methylated β-cyclodextrins-threaded polyrotaxane (Me-PRX), a supramolecular structured polymer, induces autophagy by interacting with the endoplasmic reticulum. The same level of autophagy induction was achieved at one-twentieth the dosage for the mitochondria-targeted nanocarrier (Me-PRX) compared to the naked Me-PRX. The quantitative evaluation of the intracellular organelle localization of both naked Me-PRX and the MITO-Porter (Me-PRX) are reported here. Mitochondria, endoplasmic reticulum and lysosomes were selected as target organelles because they would be involved in autophagy induction. In addition, organelle injury and cell viability assays were performed. The results showed that the naked Me-PRX and the MITO-Porter (Me-PRX) were localized in different intracellular organelles, and organelle injury was different, depending on the route of administration, indicating that different organelles contribute to autophagy induction. These findings indicate that the organelle to which the autophagy-inducing molecules are delivered plays an important role in the level of induction of autophagy.

Biomolecules | Free Full-Text | Differences in the Intracellular Localization of Methylated β-Cyclodextrins-Threaded Polyrotaxanes Lead to Different Cellular States (mdpi.com)

Cyclodextrin supramolecular drug for targeted delivery of camptothecin as well as preparation method and application of cyclodextrin supramolecular drug

Egyéb kategória,

We believe that using cyclodextrin for targeted delivery of molecules is certainly one of the applications that will be in future’s research focus.

In this patent that we bring today as a good example, a camptothecin derivative and cyclodextrin polyrotaxane are subjected to a click chemical reaction under the catalysis of copper, and the cyclodextrin supramolecular drug for targeted delivery of camptothecin is obtained by using active folate termination. Cell experiments show that the compound has good targeting selectivity and anti-tumor effect, and also has the advantage of small toxic and side effects.

Espacenet – Cyclodextrin supramolecular drug for targeted delivery of camptothecin as well as preparation method and application of cyclodextrin supramolecular drug

Incorporation of Hydrophilic Macrocycles Into Drug-Linker Reagents Produces Antibody-Drug Conjugates With Enhanced in vivo Performance

Today's cyclodextrin, ,

Antibody-drug conjugates (ADCs) have begun to fulfill their promise as targeted cancer therapeutics with ten clinical approvals to date. Recently the role that linker-payload reagent design has on the properties of ADCs has been highlighted as an important consideration for developers. In this paper from Abzena, the effect of incorporating hydrophilic macrocycles like cyclodextrin into reagent structures on the in vitro and in vivo behavior of ADCs.

Nick Evans, Ruslan Grygorash, Nicolas Camper, Mark Frigerio, Matthew Bird et al

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In vivo assessment of tumor targeting potential of 68Ga-labelled randomly methylated beta-cyclodextrin (RAMEB) and 2-hydroxypropyl-β-cyclodextrin (HPβCD) using positron emission tomography

Today's cyclodextrin, , , , ,

This novel application is a fascinating combination of tumor targeting and diagnosis using of 68Ga-labelled cyclodextrin for positron emission tomography of PGE2-positive tumors.
University of Debrecen – Gabor Opposits, István Jószai, Istvan Kertesz, Zita Képes, Méhes Gábor, Ferenc Fenyvesi István Hajdu, György Trencsenyi

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Prostate-specific membrane antigen (PSMA) ligands comprising an amylase cleavable linker

carbohydrates, drug discovery, ,

Using sugars in a prodrug concept is a fascinating idea as these compounds can bring so much to the table like improve stability, PK, or help in targeting. In this patent from Heidelberg University oligosaccharide conjugated prostate-specific membrane antigens are described where the bonds are cleaved by amylase in the body.

See the patent on espacenet