Development of BCR-ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand

• Published in: Bioorganic & medicinal chemistry letters Vol. 26; no. 20; pp. 4865 - 4869
• Main Authors: Demizu, Yosuke, Shibata, Norihito, Hattori, Takayuki, Ohoka, Nobumichi, Motoi, Hiromi, Misawa, Takashi, Shoda, Takuji, Naito, Mikihiko, Kurihara, Masaaki
• Format: Journal Article
• Language: English
• Published: OXFORD Elsevier Ltd 15.10.2016; Elsevier
• Subjects: BCR-ABL; Bestatin; Chemistry; Chemistry, Medicinal; Chemistry, Organic; E3 ubiquitin ligase; Fusion Proteins, bcr-abl - metabolism; Humans; Imatinib; Imatinib Mesylate - metabolism; Inhibitor of Apoptosis Proteins - metabolism; K562 Cells; Life Sciences & Biomedicine; Ligands; Pharmacology & Pharmacy; Physical Sciences; Protein Binding; Protein knockdown; Proteolysis; Science & Technology; Protein knockdown; Imatinib; E3 ubiquitin ligase; Bestatin; BCR-ABL; DESIGN; HYBRID MOLECULES; TYROSINE KINASE; ALPHA; CHRONIC MYELOID-LEUKEMIA; CELL-DEATH; SMALL-MOLECULE PROTACS; UBIQUITINATION; PHILADELPHIA-CHROMOSOME

[Display omitted] The manipulation of protein stability with small molecules has great potential as a technique for aiding the development of clinical therapies, including treatments for cancer. In this study, BCR-ABL protein degradation inducers called SNIPER(ABL) (Specific and Non-genetic inhibito...