Department of Life Sciences, University of Modena and Reggio Emilia , Via Campi 183, 41125 Modena, Italy.
J Med Chem. 2014 Dec 26;57(24):10551-6. doi: 10.1021/jm501397h. Epub 2014 Dec 3.
Information on the cellular internalization and stability of the ovarian cancer cell growth inhibitor peptide, LSCQLYQR (LR), is vital for lead optimization. Ad-hoc-synthesized LR/fluorescent-probe conjugates were used to monitor the internalization of the peptide. Mass spectrometry was used to identify adducts resulting from the thiol reactivity of the cysteine residue in LR. A mechanistic model is proposed to explain the observed change in intracellular peptide amount over time. Structural modifications can be foreseen to improve the peptide stability.
对于先导优化，了解卵巢癌细胞生长抑制剂肽 LSCQLYQR（LR）的细胞内化和稳定性信息至关重要。专门合成的 LR/荧光探针缀合物用于监测肽的内化。质谱用于鉴定 LR 中半胱氨酸残基的巯基反应生成的加合物。提出了一个机制模型来解释观察到的细胞内肽含量随时间的变化。可以预见结构修饰可以提高肽的稳定性。
