Preclinical activity and a pilot phase I study of pacritinib, an oral JAK2/FLT3 inhibitor, and chemotherapy in FLT3-ITD-positive AML [0.03%]
帕克利替尼（一种口服JAK2/FLT3抑制剂）和化疗在FLT3-ITD阳性AML中的临床前活性及I期试点研究
Jae Yoon Jeon,Qiuhong Zhao,Daelynn R Buelow et al.
Jae Yoon Jeon et al.
Activating FLT3 internal tandem duplication (FLT3-ITD) mutations in acute myeloid leukemia (AML) associate with inferior outcomes. We determined that pacritinib, a JAK2/FLT3 inhibitor, has in vitro activity against FLT3-ITD and tyrosine kin...
Cardamonin, a natural chalcone, reduces 5-fluorouracil resistance of gastric cancer cells through targeting Wnt/β-catenin signal pathway [0.03%]
姜黄素类似物 cardamonin通过作用于Wnt/β-连环蛋白信号通路降低胃癌细胞对氟尿嘧啶的耐药性
Gaochao Hou,Xiang Yuan,Yi Li et al.
Gaochao Hou et al.
Objectives Cardamonin (CD), an active chalconoid, has been extensively studied in a wide variety of human tumors. However, the effects and underlying mechanism of cardamonin on 5-fluorouracil (5-FU)-resistant gastric cancer (GC) remain larg...
Zelnorm, an agonist of 5-Hydroxytryptamine 4-receptor, acts as a potential antitumor drug by targeting JAK/STAT3 signaling [0.03%]
5-羟色胺4受体激动剂替加色罗通过靶向JAK/STAT3信号通路发挥潜在的抗肿瘤作用
Lei Zhang,Qiaoling Song,Xinxin Zhang et al.
Lei Zhang et al.
The Janus kinase (JAK)/signal transducer and activator of transcription 3 (STAT3) signaling pathway plays central roles in cancer cell growth and survival. Drug repurposing strategies have provided a valuable approach for developing antitum...
Expression of the PTEN/FOXO3a/PLZF signalling pathway in pancreatic cancer and its significance in tumourigenesis and progression [0.03%]
PTEN/FOXO3a/PLZF信号通路在胰腺癌中的表达及其在肿瘤发生发展中的意义
Qiubo Zhang,Xuanna Li,Yaqing Li et al.
Qiubo Zhang et al.
Pancreatic cancer (PC) is one of the most lethal gastrointestinal malignancies. The PTEN/AKT signalling pathway is closely related to the tumourigenesis and progression of PC. The downstream effectors, FOXO3a, PLZF and VEGF, are reported to...
Identification of a 3,3-difluorinated tetrahydropyridinol compound as a novel antitumor agent for hepatocellular carcinoma acting via cell cycle arrest through disturbing CDK7-mediated phosphorylation of Cdc2 [0.03%]
一种新的肝癌抗肿瘤药物的鉴定：通过干扰CDK7介导的Cdc2磷酸化作用，使细胞周期停滞在3,3-二氟四氢吡啶化合物中
Wu Bi,Ji-Chang Xiao,Rui-Jie Liu et al.
Wu Bi et al.
Tetrahydropyridinol derivatives were recently reported to exhibit good biological activities, and the incorporation of fluorine into organic molecules may have profound effects on their physical and biological properties. Therefore, we inve...
Pam3CSK4, a TLR2 ligand, induces differentiation of glioblastoma stem cells and confers susceptibility to temozolomide [0.03%]
TLR2配体 Pam3CSK4诱导胶质母细胞瘤干细胞分化并使其对替莫唑胺敏感
Javier Megías,Alba Martínez,Teresa San-Miguel et al.
Javier Megías et al.
Glioblastoma multiforme (GBM) is the most aggressive human brain tumor, and GBM stem cells (GSC) may be responsible for its recurrence and therapeutic resistance. Toll-like receptors (TLRs), which recognize multiple ligands (endogenous and ...
A phase Ib study of GSK3052230, an FGF ligand trap in combination with pemetrexed and cisplatin in patients with malignant pleural mesothelioma [0.03%]
戈舍瑞林(FGFR配体陷阱)联合培美曲塞和顺铂治疗恶性胸膜间皮瘤的Ib期临床研究
Emilie M J van Brummelen,Evgeny Levchenko,Manuel Dómine et al.
Emilie M J van Brummelen et al.
Background Fibroblast growth factors (FGFs) have a fundamental role in cancer. Sequestering FGFs with GSK3052230 (FP-1039) blocks their ability to activate FGFRs while avoiding toxicities associated with small molecule inhibitors of FGFR, i...
A phase 1 study of oral ASP5878, a selective small-molecule inhibitor of fibroblast growth factor receptors 1-4, as a single dose and multiple doses in patients with solid malignancies [0.03%]
一项关于选择性成纤维细胞生长因子受体1-4抑制剂ASP5878口服单剂量及多剂量的I期临床研究：在实体瘤患者中的药代动力学、安全性及初步疗效试验
Noboru Yamamoto,Baek-Yeol Ryoo,Bhumsuk Keam et al.
Noboru Yamamoto et al.
ASP5878 is a selective small-molecule inhibitor of fibroblast growth factor receptors (FGFRs). This study investigated safety, tolerability, and antitumor effect of single and multiple oral doses of ASP5878 in patients with solid tumors. Th...
Randomized phase II trial of neoadjuvant everolimus in patients with high-risk localized prostate cancer [0.03%]
新辅助治疗依维莫司治疗高危局限性前列腺癌患者的二期随机试验
Vadim S Koshkin,Maria C Mir,Pedro Barata et al.
Vadim S Koshkin et al.
Background Despite definitive local therapy, patients with high-risk prostate cancer have a significant risk for local and distant failure. To date, no systemic therapy given prior to surgery has been shown to improve outcomes. The phosphat...
Correction to: Sphingadienes show therapeutic efficacy in neuroblastoma in vitro and in vivo by targeting the AKT signaling pathway [0.03%]
correction to: 神经酰胺二烯具有体内和体外治疗神经母细胞瘤的效力通过靶向AKT信号通路
Piming Zhao,Ana E Aguilar,Joanna Y Lee et al.
Piming Zhao et al.
The authors would like to note an omission of disclosure in this paper. Author JDS is cofounder, equity-holder, and consultant of GILTRx Therapeutics.
Published Erratum
Investigational new drugs. 2019 Dec;37(6):1309. DOI:10.1007/s10637-019-00772-w 2019