Tykvart, Jan; Schimer, Jiri; Barinkova, Jitka; Pachl, Petr; Postova-Slavetinska, Lenka; Majer, Pavel; Konvalinka, Jan; Sacha, Pavel published the artcile< Rational design of urea-based glutamate carboxypeptidase II (GCPII) inhibitors as versatile tools for specific drug targeting and delivery>, SDS of cas: 22717-55-1, the main research area is glutamate carboxypeptidase II inhibitor prostate cancer targeting; GCPII; PSMA; Specific drug targeting; Structure-aided drug design.
Glutamate carboxypeptidase II (GCPII), also known as prostate specific membrane antigen (PSMA), is an established prostate cancer marker and is considered a promising target for specific anticancer drug delivery. Low-mol.-weight inhibitors of GCPII are advantageous specific ligands for this purpose. However, they must be modified with a linker to enable connection of the ligand with an imaging mol., anticancer drug, and/or nanocarrier. Here, we describe a structure-activity relationship (SAR) study of GCPII inhibitors with linkers suitable for imaging and drug delivery. Structure-assisted inhibitor design and targeting of a specific GCPII exosite resulted in a 7-fold improvement in Ki value compared to the parent structure. X-ray structural anal. of the inhibitor series led to the identification of several inhibitor binding modes. We also optimized the length of the inhibitor linker for effective attachment to a biotin-binding mol. and showed that the optimized inhibitor could be used to target nanoparticles to cells expressing GCPII.
Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 22717-55-1 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO3, SDS of cas: 22717-55-1.
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