近日,中山大学肿瘤防治中心张星教授团队在国际权威期刊《ESMO Open》上发表了题为"A first-in-human phase I study of a novel MDM2/p53 inhibitor alrizomadlin in advanced solid tumors"的研究论文。该研究首次评估了新型MDM2-p53抑制...
[13] Mrinal M. Gounder et al. A First-in-Human Phase I Study of Milademetan, an MDM2 Inhibitor, in Patients With Advanced Liposarcoma, Solid Tumors, or Lymphomas. JCO . 2022, 41, 1714-1724(2023). [14] Abdul Razak AR...
前言 近日,中山大学肿瘤防治中心张星教授团队在国际权威期刊《ESMO Open》上发表了题为"A first-in-human phase I study of a novel MDM2/p53 inhibitor alrizomadlin in advanced solid tumors"的研究论文。该研究首次评估了新型MDM2-p53抑制剂alrizomadlin(APG-115)在晚期实体瘤患者中的安全性、药代动力学、...
通过对这一系列多肽进行活性测试，测得其中SAH-p53-8活性最好，荧光极化实验测得其与MDM2有55nM的结合活性（图三）。在细胞活性上，SAH-p53-8对SJSA-1 cells有8uM的抑制活性。图三：A.烯烃复分解策略完成环肽的合成；B.对设计的多肽进行筛选和优化 随后Loren D. Walensky在2010年于Cancer Cell上【4】对SAH-p...
"APG-115在此次ASCO年会上展示的核心要点如下：Newly updated activity results of alrizomadlin (APG-115), a novel MDM2/p53 inhibitor, plus pembrolizumab: Phase 2 study in adults and children with various solid tumors.新型MDM2-p53抑制剂APG-115联合帕博利珠单抗治疗成人及儿童实体瘤患者的最新II期临床...
【6】Chang, Yong S. , et al. "Stapledα-helical peptide drugdevelopment: a potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy."Proceedings of the National Academy of Sciences of the United States of America110.36(2013). ...
图二MDM2-p53 inhibitor 7 (MI-1061)及PROTAC 8 (MD-224) 后续的体外、体内研究显示,相对于原有药物(MI-1061) ,PROTAC(MD-224)的功效大大提高,且在有效剂量下(25 mg/kg(Q2D))未表现出任何毒性副作用,具有巨大的药物应用潜力。 小结 显然,新型PROTAC技术给MDM2-p53抑制剂的开发带来了新的契机,相对于传...
Newly updated activity results of alrizomadlin (APG-115), a novel MDM2/p53 inhibitor, plus pembrolizumab: Phase 2 study in adults and children with various solid tumors. 新型MDM2-p53抑制剂APG-115联合帕博利珠单抗治疗成人及儿童实体瘤患者的最新II期临床数据 ...
Newly updated activity results of alrizomadlin (APG-115), a novel MDM2/p53 inhibitor, plus pembrolizumab: Phase 2 study in adults and children with various solid tumors. 新型MDM2-p53抑制剂APG-115联合帕博利珠单抗治疗成人及儿童实体瘤患者的最新II期临床数据 ...
英文原题:Discovery of Novel p53-MDM2 Inhibitor (RG7388)-Conjugated PlatinumIVComplexes as Potent Antitumor Agents 通讯作者:王胜正(空军军医大学药学系) 作者:Wei Liu, Yi Ma, Youyou He, Yanhong Liu, Zhongjie Guo, Jin He, Xiaodong Han, Yujiao Hu, Muqiong Li, Ru Jiang, and Shengzheng Wang*...