Enhanced tumor retention of NTSR1-targeted agents by employing a hydrophilic cysteine cathepsin inhibitor.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.05.068
Abstract: We explored the approach of using an analog of E-64, a well-known and hydrophilic cysteine cathepsin (CC) inhibitor, as a potent cysteine cathepsin-trapping agent (CCTA) to improve the tumor retention of low-molecular-weight, receptor-targeted radiopharmaceuticals. The… read more here.
Keywords: cysteine cathepsin; retention; ntsr1 targeted; tumor retention ... See more keywords
Examination of Charge Modifications of an Endolysosomal Trapping Inhibitor in an Antagonistic NTSR1-Targeted Construct for Colon Cancer.
Sign Up to like & getrecommendations! Published in 2022 at "Bioconjugate chemistry"
DOI: 10.1021/acs.bioconjchem.2c00214
Abstract: Many low-molecular weight targeted radiotherapeutics (TRTs) are capable of rapidly achieving exceptional tumor to non-target ratios shortly after administration. However, the low tumor residence time of many TRTs limits therapeutic dose delivery and has become… read more here.
Keywords: antagonistic ntsr1; charge; colon cancer; endolysosomal trapping ... See more keywords