Mechanically interlocked molecules present {opportunities|possibilities} to construct therapeutic drugs and diagnostic imaging agents but harnessing supramolecular chemistry {to make|to create|to produce} biologically active molecules in water {is a|is really a|is actually a|can be a|is often a|is usually a} challenge. {Here|Right here}, we describe a rotaxane-based {approach|method|strategy} {in the|within the|inside the} synthesis of radiolabelled proteins and peptides for molecular imaging of cancer-specific biomarkers in vivo. Host-guest chemistry with mono-functionalised beta-cyclodextrin, combined with curcurbit[6]uril catalysed cooperative capture synthesis, {produced|created|made|developed} radioactive gallium-68 or zirconium-89-labelled metallo[4]rotaxanes. Simultaneous, one-pot radiolabelling and photochemical conjugation to monoclonal antibodies {produced|created|made|developed} a viable radiotracer that was evaluated in vivo for quantitative positron emission tomography (PET) imaging of cancer biomarker expression. The rotaxane architecture {can be|may be|could be|might be|is often|is usually} {easily|effortlessly|very easily|simply|quickly|conveniently} tuned to accommodate {different|various|distinct|diverse|unique|distinctive} radioactive metal ion complexes, other proteins and peptide-based drugs, and fluorophores for optical detection. This {technology|technologies} {provides|offers|gives|supplies|delivers} a future platform to {explore|discover} {the use of|the usage of} mechanical bonding to optimise drug delivery, {control|manage|handle} metabolism and excretion profiles, and {enhance|improve|boost} the efficacy of tumour {specific|particular|certain|distinct|precise} agents. 1446022-58-7 Purity 5-Methoxy-2-methylbenzoic acid web PMID:23847952
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