An article Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein WOS:000505633400021 published article about E3 UBIQUITIN LIGASE; 2 SH2 DOMAIN; SIGNAL TRANSDUCER; PEPTIDOMIMETIC INHIBITORS; SMALL MOLECULES; DESIGN; DEGRADATION; ACTIVATOR; OPTIMIZATION; VALIDATION in [Zhou, Haibin; Bai, Longchuan; Xu, Renqi; Zhao, Yujun; Chen, Jianyong; McEachern, Donna; Yang, Chao-Yie; Liu, Zhaomin; Wang, Mi; Liu, Liu; Yi, Han; Wang, Shaomeng] Univ Michigan, Rogel Canc Ctr, Ann Arbor, MI 48109 USA; [Zhou, Haibin; Bai, Longchuan; Xu, Renqi; Zhao, Yujun; Chen, Jianyong; McEachern, Donna; Yang, Chao-Yie; Liu, Zhaomin; Wang, Mi; Liu, Liu; Yi, Han; Wang, Shaomeng] Univ Michigan, Dept Internal Med, Ann Arbor, MI 48109 USA; [Wang, Shaomeng] Univ Michigan, Dept Pharmacol, Med Sch, Ann Arbor, MI 48109 USA; [Wang, Shaomeng] Univ Michigan, Coll Pharm, Med Chem, 428 Church St, Ann Arbor, MI 48109 USA; [Chinnaswamy, Krishnapriya; Meagher, Jennifer L.; Stuckey, Jeanne A.] Univ Michigan, Life Sci Inst, Ann Arbor, MI 48109 USA; [Wen, Bo; Dai, Lipeng; Kumar, Praveen; Sun, Duxin] Univ Michigan, Coll Pharm, Dept Pharmaceut Sci, 428 Church St, Ann Arbor, MI 48109 USA in 2019.0, Cited 43.0. Computed Properties of C13H13N. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9
Signal transducer and activator of transcription 3 (STAT3) is a transcription factor and an attractive therapeutic target for cancer and other human diseases. Despite 20 years of persistent research efforts, targeting STAT3 has been very challenging. We report herein the structure-based discovery of potent small-molecule STAT3 degraders based upon the proteolysis targeting chimera (PROTAC) concept. We first designed SI-109 as a potent, small-molecule inhibitor of the STAT3 SH2 domain. Employing ligands for cereblon/cullin 4A E3 ligase and SI-109, we obtained a series of potent PROTAC STAT3 degraders, exemplified by SD-36. SD-36 induces rapid STAT3 degradation at low nanomolar concentrations in cells and fails to degrade other STAT proteins. SD-36 achieves nanomolar cell growth inhibitory activity in leukemia and lymphoma cell lines with high levels of phosphorylated STAT3. A single dose of SD-36 results in complete STAT3 protein degradation in xenograft tumor tissue and normal mouse tissues. SD-36 achieves complete and long-lasting tumor regression in the Molm-16 xenograft tumor model at well-tolerated dose-schedules. SD-36 is a potent, selective, and efficacious STAT3 degrader.
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