![]() Biodistribution studies showed a higher in vivo accumulation in the tumor than in most healthy tissues.Ĭitation: Rana S, Nissen F, Marr A, Markert A, Altmann A, Mier W, et al. Stability experiments indicated the degradation site in the sequence of CaIX-P1-4-10. Binding of radiolabeled CaIX-P1-4-10 on CA IX positive cells could be inhibited by both the unlabeled and the native CaIX-P1 peptide but not by control peptides. Among various fragments and derivatives the ligand CaIX-P1-4-10 (NHVPLSPy) was found to possess increased binding potential in SKRC 52 cells, whereas no binding capacity for BxPC3 cells was observed. The results of our studies clearly identified amino acids that are important for target binding. Organ distribution and planar scintigraphy studies were performed in Balb/c nu/ nu mice carrying subcutaneously transplanted SKRC 52 tumors. Metabolic stability was investigated in cell culture medium and human serum. Derivatives with increased binding affinity were radiolabeled and in vitro studies were carried out on the CA IX positive human renal cell carcinoma cell line SKRC 52 and the CA IX negative human pancreatic carcinoma cell line BxPC3. Alanine scanning was performed for identification of the amino acids crucial for target binding. ![]() Various fragments of CaIX-P1 were synthesized on solid support using Fmoc chemistry. ![]()
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