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Treatment of tumors expressing mutant p53

机译:表达突变型p53的肿瘤的治疗

摘要

PDGFRb inhibitors and the use of such inhibitors to treat mutant p53-expressing tumors are described. The present disclosure encompasses the discovery that mutant p53-induced upregulation of the platelet-derived growth factor receptor b (PDGFRb) contributes to invasion and/or metastasis of tumors expressing mutant p53. Specifically, the present disclosure encompasses the discovery that mutant p53 can disrupt a p73/NF-Y complex (which can repress PDGFRB transcription), leading to transcription of PDGFRb. The present disclosure therefore provides, at least in part, PDGFRb modulators (e.g., activators or inhibitors) for use in medicine, and specifically in diagnosis, treatment and/or prevention (e.g., delay of onset) of certain disorders, e.g., cancer.
机译:描述了PDGFRb抑制剂及其在治疗表达突变型p53的肿瘤中的用途。本公开涵盖了以下发现:突变体p53诱导的血小板衍生的生长因子受体b(PDGFRb)的上调有助于表达突变体p53的肿瘤的侵袭和/或转移。具体地,本公开内容涵盖突变体p53可以破坏p73 / NF-Y复合物(其可以抑制PDGFRB转录),导致PDGFRb转录的发现。因此,本公开至少部分提供了PDGFRb调节剂(例如,活化剂或抑制剂),其用于医学中,并且具体地用于某些疾病例如癌症的诊断,治疗和/或预防(例如,发作延迟)。

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