Bathing in carbs: Lai-Xi Wang and his group from the University of Maryland reported the synthesis of cyclodextrin-based multivalent glycan ligands for human galectin-3. The GalNAc (Tn antigen) containing heptavalent ligand showed the highest affinity for human Gal-3 among the synthetic ligands tested, with an EC50 of 1.4 μM in binding to human Gal-3.
Great read on pore-forming lectin SaroL-1 punching holes in cancer cells by targeting the tumor-related glycosphingolipid Gb3 presented by a well-known team led by Anne Imberty (Grenoble University), Winfried Römer (Université de Fribourg – Universität Freiburg) and Frederique Lisacek (University of Geneva)
Fascinating!
Great paper on the relations of Gal-3 levels and Aβ deposits and tau aggregates in #brain tissue in #alzheimersdisease published by a great collaboration of the University of Seville, ENS-PSL, EHESS, Université Paris Cité, Lund University, and the University of Gothenburg.
#neurodegenerativediseases #alzheimers #brainhealth #carbohydrates #glycotime
Cyclodextrin derivatives were demonstrated to be endowed with intrinsic antiviral action against several viruses (herpes, HIV, RSV, influenza, covid19, etc.). In this great work from Rachele Francese, Francesco Trotta, Claudio Cecone, Matteo Constantino, Gjylije Hoti, Pierangiola Bracco, and David Lembo from the University of Turin, four water-soluble hyper-branched beta cyclodextrin anionic polymer were screened against herpes simplex virus (HSV-2), respiratory syncytial virus (RSV), rotavirus (HRoV), and influenza virus (FluVA). The results suggest that the polymer virucidal activity against RSV can be exploited to produce new antiviral materials to counteract the virus dissemination through the air or direct contact.
This week seems to be all about cyclodextrin.
Chris Kevil’s group (Gopi Krishna Kolluru et al.) from Louisiana State University discovered the Sugammadex (among other prodrugs) could serve as an H2S donor and support the treatment of covid patients. Amazing work!
Great paper from The University of Kansas by Mark P. Farrell and their team on lectin drug conjugates targeting N-glycans.
Read more: https://chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/cbic.202200266
Yet another novel use proposed for sugammadex and SBE-cyclodextrin: as antidotes against chlorpromazine-induced acute toxicity. An excellent paper by Eszter Nyúl, Rita Klaudia Csepregi, Gábor Benkovics PhD, Lajos Szente, and Poór Miklós from the University of Pécs.
For more details, follow this link.
An interesting idea proposed by Knut M. Wittkowski for the novel use of alpha-#cyclodextrin:
The effect of alpha-cyclodextrin on post-prandial glucose excursions, a systematic meta-analysis
For more details, click here
Using cyclodextrins, especially 2-hydroxypropyl-beta-CD for the treatment of atherosclerosis has a hype, there are several companies and research groups chasing this holy grail. Fresh from the oven is the patent application from Beren Therapeutics explaining methods of treating familial hypercholesterolemia via different mechanisms of action.
