title: Development of target protein-selective degradation inducer for protein knockdown.
abstract: Our previous technique for inducing selective degradation of target proteins with ester-type SNIPER (Specific and Nongenetic Inhibitor-of-apoptosis-proteins (IAPs)-dependent Protein ERaser) degrades both the target proteins and IAPs. Here, we designed a small-molecular amide-type SNIPER to overcome this issue. As proof of concept, we synthesized and biologically evaluated an amide-type SNIPER which induces selective degradation of cellular retinoic acid binding protein II (CRABP-II), but not IAPs. Such small-molecular, amide-type SNIPERs that induce target protein-selective degradation without affecting IAPs should be effective tools to study the biological roles of target proteins in living cells.
authors.affiliation: Institute of Molecular and Cellular Biosciences, The University of Tokyo, Yayoi, Bunkyo-ku, Japan.
authors.forename: Yukihiro
authors.initials: Y
authors.lastname: Itoh
authors.forename: Minoru
authors.initials: M
authors.lastname: Ishikawa
authors.forename: Risa
authors.initials: R
authors.lastname: Kitaguchi
authors.forename: Shinichi
authors.initials: S
authors.lastname: Sato
authors.forename: Mikihiko
authors.initials: M
authors.lastname: Naito
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Hashimoto
mesh_terms: D000577:Amides / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D045744:Cell Line, Tumor; D006801:Humans; D051034:Inhibitor of Apoptosis Proteins / Q000378:metabolism*; D009447:Neuroblastoma / Q000378:metabolism; D018168:Receptors, Retinoic Acid / Q000378:metabolism*; D054852:Small Molecule Libraries / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000577:Amides; D051034:Inhibitor of Apoptosis Proteins; D018168:Receptors, Retinoic Acid; D054852:Small Molecule Libraries; C082928:retinoic acid binding protein II, cellular