Boron clusters as broadband membrane carriers

Article

关键词: CELL-PENETRATING PEPTIDES;    ANTIBODY DELIVERY;    RICH PEPTIDES;    TRANSPORT;    POLYARGININE;    RECOGNITION;    CALIXARENES;    TECHNOLOGY;    ACTIVATORS;    INTERACTS;   

DOI  :  10.1038/s41586-022-04413-w

来源: SCIE

【 摘 要 】

The membrane translocation of hydrophilic substances constitutes a challenge for their application astherapeutic compounds and labelling probes(1-4) . To remedy this, charged amphiphilic molecules have been classically used as carriers(3,5). However, such amphiphilic carriers may cause aggregation and non-specific membrane lysis(6,7). Here we show that globular dodecaborate clusters, and prominently B12Br122-, can function as anionic inorganic membrane carriers for a broad range of hydrophilic cargo molecules (with molecular mass of146-4,500 Da). We show that cationic and neutral peptides, amino acids, neurotransmitters, vitamins, antibiotics and drugs can be carried across liposomal membranes. Mechanistic transport studies reveal that the carrier activity is related to the superchaotropic nature of these cluster anions(8-)(12). We demonstrate that B12Br122-- affects cytosolic uptake of different small bioactive molecules, including the antineoplastic monomethyl auristatin F, the proteolysis targeting chimera dBET1 and the phalloidin toxin, which has been successfully delivered in living cells for cytoskeleton labelling. We anticipate the broad and distinct delivery spectrum of our superchaotropic carriers to be the starting point of conceptually distinct cell-biological, neurobiological, physiological and pharmaceutical studies.

【 授权许可】

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