7SHH

Bacterial cereblon homologue in complex with (R)-3-(4-methoxyphenyl)piperidine-2,6-dione

7SHH の概要

• エントリーDOI: 10.2210/pdb7shh/pdb
• 分子名称: Cereblon isoform 4, ZINC ION, (3R)-3-(4-methoxyphenyl)piperidine-2,6-dione, ... (4 entities in total)
• 機能のキーワード: cereblon, protac, targeted protein degradation, tbd, signaling protein
• 由来する生物種: Magnetospirillum gryphiswaldense
• タンパク質・核酸の鎖数: 3
• 化学式量合計: 41922.59

構造登録者

Nithianantham, S.,Fischer, M. (登録日: 2021-10-08, 公開日: 2022-04-13, 最終更新日: 2024-05-22)

主引用文献

Alcock, L.J.,Chang, Y.,Jarusiewicz, J.A.,Actis, M.,Nithianantham, S.,Mayasundari, A.,Min, J.,Maxwell, D.,Hunt, J.,Smart, B.,Yang, J.J.,Nishiguchi, G.,Fischer, M.,Mullighan, C.G.,Rankovic, Z.
Development of Potent and Selective Janus Kinase 2/3 Directing PG-PROTACs.
Acs Med.Chem.Lett., 13:475-482, 2022

PubMed Abstract: Aberrant activation of the JAK-STAT signaling pathway has been implicated in the pathogenesis of a range of hematological malignancies and autoimmune disorders. Here we describe the design, synthesis, and characterization of JAK2/3 PROTACs utilizing a phenyl glutarimide (PG) ligand as the cereblon (CRBN) recruiter. SJ10542 displayed high selectivity over GSPT1 and other members of the JAK family and potency in patient-derived ALL cells containing both JAK2 fusions and CRLF2 rearrangements.

PubMed: 35300081
DOI: 10.1021/acsmedchemlett.1c00650

実験手法

X-RAY DIFFRACTION (1.9 Å)