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An organotrifluoroborate for broadly applicable one-step 18F-labeling.
TLDR
A new zwitterionic organotrifluoroborate is appended to three radiosynthons that afford undergo facile bioconjugation to several clinically relevant peptides and one enzyme inhibitor, which shows in vivo stability and tumor uptake.
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Characterization of the structure and membrane interaction of the antimicrobial peptides aurein 2.2 and 2.3 from Australian southern bell frogs.
TLDR
The data presented here suggest that all three peptides studied interact with phosphatidylcholine membranes in a manner which is similar to aurein 2.2 and citropin 1.1, as reported in the literature, with no correlation to the reported activity.
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Parameters Affecting the Chiral Nematic Phase of Nanocrystalline Cellulose Films
Nanocrystalline cellulose (NCC) is extracted from woody biomass using acid hydrolysis. It has unique strength and distinctive optical/conductive/magnetic properties. When a suspension of NCC is…
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Preclinical Evaluation of a High-Affinity 18F-Trifluoroborate Octreotate Derivative for Somatostatin Receptor Imaging
TLDR
18F-AMBF3-TATE was radiolabeled in high yield and at high specific activity, did not require high-performance liquid chromatography purification, exhibited unexpectedly high binding affinity to somatostatin receptor subtype 2, and showed excellent pharmacokinetic properties in vivo, with high tumor uptake and high contrast ratios.
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Trimeric Radiofluorinated Sulfonamide Derivatives to Achieve In Vivo Selectivity for Carbonic Anhydrase IX–Targeted PET Imaging
TLDR
The data suggest that trimerization of an otherwise nonspecific CA inhibitor greatly enhances the selectivity for CA-IX in vivo and represents a promising strategy for creating multivalent enzyme inhibitors for selectively imaging extracellular enzyme activity by PET.
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Synthetic fusion peptides of tick-borne encephalitis virus as models for membrane fusion.
TLDR
The data suggest that TFPtr is the most fusogenic at acidic pH and that the mutation from L107 to T reduces activity, and that this reduction in activity may be related to the fact that the mutations disrupt trimer stability.
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Irreversible denaturation of proteins through aluminum-induced formation of backbone ring structures.
A combination of ab initio calculations, circular dichroism, nuclear magnetic resonance, and X-ray photoelectron spectroscopy has shown that aluminum ions can induce the formation of backbone ring…
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Effects of Linker Modification on Tumor-to-Kidney Contrast of 68Ga-Labeled PSMA-Targeted Imaging Probes.
TLDR
The data indicate that substitution of 2-Nal in PSMA-617 with other lipophilic amino acid can modulate PSMA binding affinity and their pharmacokinetics in vivo.
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Preclinical Melanoma Imaging with 68Ga-Labeled α-Melanocyte-Stimulating Hormone Derivatives Using PET
TLDR
The introduction of a cationic Pip linker to Nle-CycMSHhex, CCZ01048, not only improved tumor uptake, but also generated high tumor-to-normal tissue contrast with PET imaging in a preclinical melanoma model, suggesting it is a promising candidate for PET imaging of melanoma and potentially as a theranostic agent for radionuclide therapy of melanomas when labeled with α or β emitters.
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Nitroimidazole-Containing H2dedpa and H2CHXdedpa Derivatives as Potential PET Imaging Agents of Hypoxia with (68)Ga.
TLDR
Nitroimidazole (NI) derivatives of H2dedpa and H2CHXdedpa to investigate specific targeting of hypoxic tumor cells are investigated, given that NI can be reduced and retained exclusively in hypoxic cells.
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