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1.
J Org Chem ; 89(17): 11837-11863, 2024 Sep 06.
Artigo em Inglês | MEDLINE | ID: mdl-39173032

RESUMO

Radioactive iodines and astatine, possessing distinct exploitable nuclear properties, play indispensable roles in the realms of nuclear imaging and therapy. Their analogous chemical characteristics shape the design, preparation, and substrate range for tracers labeled with these radiohalogens through interconnected radiosynthetic chemistry. This perspective systematically explores the labeling methods by types of halogenating reagents─nucleophilic and electrophilic─underpinning the rational design of such compounds. It delves into the rapidly evolving synthetic strategies and reactions in radioiodination and radioastatination over the past decade, comparing their intrinsic relationships and highlighting variations. This comparative analysis illuminates potential radiosynthetic methods for exploration. Moreover, stability concerns related to compounds labeled with radioactive iodines and astatine are addressed, offering valuable insights for radiochemists and physicians alike.

2.
Sheng Wu Gong Cheng Xue Bao ; 40(4): 1225-1236, 2024 Apr 25.
Artigo em Chinês | MEDLINE | ID: mdl-38658159

RESUMO

Phospholipase A2 (PLA2) is widely distributed in animals, plants, and microorganisms, and it plays an important role in many physiological activities. In a previous study, we have identified a secretory PLA2 in Bombyx mori (BmsPLA2-1-1). In this study, we further identified four new sPLA2 genes (BmsPLA2-1-2, BmsPLA2-2, BmsPLA2-3, and BmsPLA2-4) in B. mori genome. All four genes exhibits the characteristic features of sPLA2, including the sPLA2 domain, metal binding sites, and highly conserved catalytic domain. This study completed the cloning, in vitro expression, and expression pattern analysis of the BmsPLA2-4 gene in B. mori. The full length of BmsPLA2-4 is 585 bp, and the recombinant protein obtained through prokaryotic expression has an estimated size of 25 kDa. qRT-PCR analysis revealed that the expression level of BmsPLA2-4 reached its peak on the first day of the fifth instar larval stage. Tissue expression profiling analysis showed that BmsPLA2-4 had the highest expression level in the midgut, followed by the epidermis and fat body. Western blotting analysis results were consistent with those of qRT-PCR. Furthermore, after infecting fifth instar 1-day-old larvae with Escherichia coli and Staphylococcus aureus, the expression level of the BmsPLA2-4 gene significantly increased in 24 h. The findings of this study provides a theoretical basis and valuable experimental data for future related research.


Assuntos
Bombyx , Fosfolipases A2 Secretórias , Bombyx/genética , Bombyx/enzimologia , Animais , Fosfolipases A2 Secretórias/genética , Fosfolipases A2 Secretórias/metabolismo , Proteínas Recombinantes/genética , Proteínas Recombinantes/biossíntese , Proteínas Recombinantes/metabolismo , Larva/genética , Clonagem Molecular , Staphylococcus aureus/genética , Staphylococcus aureus/enzimologia , Proteínas de Insetos/genética , Proteínas de Insetos/metabolismo , Proteínas de Insetos/biossíntese , Sequência de Aminoácidos , Perfilação da Expressão Gênica
4.
Cell Discov ; 9(1): 84, 2023 Aug 08.
Artigo em Inglês | MEDLINE | ID: mdl-37550284

RESUMO

Tumor development, involving both cell growth (mass accumulation) and cell proliferation, is a complex process governed by the interplay of multiple signaling pathways. TET2 mainly functions as a DNA dioxygenase, which modulates gene expression and biological functions via oxidation of 5mC in DNA, yet whether it plays a role in regulating cell growth remains unknown. Here we show that TET2 suppresses mTORC1 signaling, a major growth controller, to inhibit cell growth and promote autophagy. Mechanistically, TET2 functions as a 5mC "eraser" by mRNA oxidation, abolishes YBX1-HuR binding and promotes decay of urea cycle enzyme mRNAs, thus negatively regulating urea cycle and arginine production, which suppresses mTORC1 signaling. Therefore, TET2-deficient tumor cells are more sensitive to mTORC1 inhibition. Our results uncover a novel function for TET2 in suppressing mTORC1 signaling and inhibiting cell growth, linking TET2-mediated mRNA oxidation to cell metabolism and cell growth control. These findings demonstrate the potential of mTORC1 inhibition as a possible treatment for TET2-deficient tumors.

5.
Bioconjug Chem ; 34(1): 140-161, 2023 01 18.
Artigo em Inglês | MEDLINE | ID: mdl-36594786

RESUMO

18F-Labeling methods for the preparation of 18F-labeled molecular probes can be classified into electrophilic fluorination, nucleophilic fluorination, metal-F coordination, and 18F/19F isotope exchange. Isotope exchange-based 18F-labeling methods demonstrate mild conditions featuring water resistance and facile high-performance liquid chromatography-free purification in direct 18F-labeling of substrates. This paper systematically reviews isotope exchange-based 18F-labeling methods sorted by the adjacent atom bonding with F, i.e., carbon and noncarbon atoms (Si, B, P, S, Ga, Fe, etc.). The respective isotope exchange mechanism, radiolabeling condition, radiochemical yield, molar activity, and stability of the 18F-product are mainly discussed for each isotope exchange-based 18F-labeling method as well as the cutting-edge application of the corresponding 18F-labeled molecular probes.


Assuntos
Halogenação , Água , Sondas Moleculares , Marcação por Isótopo/métodos , Radioisótopos de Flúor/química , Compostos Radiofarmacêuticos/química
6.
Exp Ther Med ; 13(2): 515-518, 2017 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-28352324

RESUMO

The objective of the present study was to evaluate the combined application of measuring cystatin C (Cys-C) and hemoglobin A1c (HbA1c) levels for early renal injury in pediatric patients with type 2 diabetes. A total of 130 children with type 2 diabetes admitted to our hospital from May 2013 to July 2015 were selected. Patients were divided according to whether there was complication of renal injury. In group A (n=65), the patients had renal injury and in group B (n=65), the patients did not have renal injury. The levels of Cys-C and HbA1c in the two groups were examined. The results showed that the levels of Cys-C and HbA1c of patients in group A were significantly higher than those in group B (P<0.05), and the positive rate of the combined examination of Cys-C and HbA1c in group A was 92.3%, and was higher than that of the individual examinations of either Cys-C or HbA1c (P<0.05). The Spearman's correlation coefficient analysis was applied to group B and showed that Cys-C was positively correlated with HbA1c (r=0.842, P<0.05). From analysis of the receiver operating characteristic curves, the combined examination of Cys-C and HbA1c surpassed the individual examinations of Cys-C or HbA1c in sensitivity and specificity (P<0.05). In conclusion, the positive detection rate of early renal injury was significantly increased by the combined examination of Cys-C and HbA1c in pediatric patients with type 2 diabetes, which is beneficial for early identification and diagnosis of this diseases and is worthy of clinical application.

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