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[In]In-RM2: a high potential agent for SPECT imaging of GRPR-expressing tumors.
Phys Eng Sci Med
January 2025
Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Tehran, 14155-1339, Iran.
Gastrin-releasing peptide receptors (GRPRs) overexpressed in many cancers are known as promising biomarkers to target tumors such as prostate, breast, and lung cancers. As the early diagnosis of the cancers can serve for better treatment of the patients, [In]In-DOTA-Pip-D-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2 ([In]In-RM2) was prepared using an in-house developed Sn/In generator. 0.
View Article and Find Full Text PDFAntimicrobial peptide LyeTx I mn∆K labeled with Ga is a potential PET radiopharmaceutical for molecular imaging of infections.
Nucl Med Biol
December 2024
Hospital Israelita Albert Einstein, São Paulo, Brazil.
Background: Antimicrobial peptides have been radiolabeled and investigated as molecular diagnostic probes due to their propensity to accumulate in infectious sites rather than aseptic inflammatory lesions. LyeTx I is a cationic peptide from the venom of Lycosa erythrognatha, exhibiting significant antimicrobial activity. LyeTx I mn∆K is a shortened derivative of LyeTx I, with an optimized balance between antimicrobial and hemolytic activities.
View Article and Find Full Text PDFRadiosynthesis and identification of a molecular probe I-FAPI targeting cancer-associated fibroblasts.
Front Oncol
August 2024
Department of Nuclear Medicine, General Hospital of Ningxia Medical University, Yinchuan, Ningxia, China.
Purpose: Fibroblast activation protein (FAP) is highly expressed in the mesenchyme of most malignant epithelial tumors, while its expression is low in normal tissues. FAP inhibitors (FAPIs) bind specifically to FAP and are used for tumor-targeted diagnosis and therapy. The aim of this study was to radiosynthesize a novel molecular probe I-FAPI and evaluate its targeting and biological characteristics.
View Article and Find Full Text PDFExploring separation mechanisms and lipophilicity in hydrophilic interaction chromatography conditions by thin-layer chromatography of anesthetics and adjuvant drugs as polar model compounds.
J Sep Sci
June 2024
Department of Analytical Chemistry, University of Belgrade-Faculty of Chemistry, Belgrade, Serbia.
The chromatographic behavior of the selected compounds was studied under conditions of hydrophilic interaction liquid chromatography (HILIC). The effect of mobile phase composition on the retention in different chromatographic systems was systematically examined using high-performance thin-layer chromatography. The sorbents of different polarity and adsorption characteristics were selected and mixtures of water and organic solvents of various compositions, from pure water to pure organic solvent were used as mobile phases.
View Article and Find Full Text PDFEvaluation of the Lipophilicity of Angularly Condensed Diquino- and Quinonaphthothiazines as Potential Candidates for New Drugs.
Molecules
April 2024
Department of Analytical Chemistry, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia in Katowice, 41-200 Sosnowiec, Poland.
Article Synopsis
- Lipophilicity is key for predicting how compounds are absorbed, distributed, and transported in biological systems, influencing their ADME profile.
- The study compared various computational methods and experimental chromatography to estimate the lipophilicity of 21 newly synthesized compounds.
- Results indicated that while in silico ADME profiling offers initial design insights, the correlation between lipophilicity and other molecular descriptors was generally weak, but the compounds complied with drug design rules, suggesting potential for therapeutic use.
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