ABSTRACT
This paper aimed to investigate the release efficiency of peptide at carbon terminal triggered by tetrazine bioorthogonal click-to-release reaction, and further explored the potential application of this reaction in functional modification and mild cleavage in solid-phase peptide synthesis. Thirteen peptide derivatives modified by trans-cyclooctene (TCO) were designed and synthesized, which were reacted with tetrazine to release the peptides. The results showed that the release rates of peptide were 90.0% to 97.7% in one hour. The strategy has good compatibility with the functional side-groups and the length of peptides, which expands the applications scope of tetrazine bioorthogonal click-to-release reaction. At the same time, a novel bifunctional trans-cyclooctene molecule was designed and synthesized. The active peptide GIRLRG was modified by fluorophore on the solid-phase resin, and released through tetrazine click-to-release reaction under mild condition, providing a new strategy for the solid-phase modification and release strategy of the peptide.
ABSTRACT
Prostate cancer is the most common malignancy in the urinary system of males. The remarkable biological and clinical heterogeneity of prostate cancer poses challenges to the initial diagnosis, differential diagnosis, treatment, and prognosis of the disease. Positron emission tomography/computed tomography (PET/CT) is an ideal imaging tool for noninvasive interrogation of underlying tumor biology. Recently, there are a variety of molecular imaging paths and radiopharmaceuticals for the diagnosis and treatment of prostate cancer. This article reviews the current state and prospects of the application of PET in the diagnosis of prostate cancer.