抑癌因子p53可以通过影响溶质载体家族7成员11、亚精胺/精胺N1-乙酰转移酶1、谷氨酰胺酶2、二肽基肽酶4和细胞周期蛋白依赖性激酶抑制剂1A来促进或抑制铁死亡,进而影响HCC的进展,通过调控铁死亡通路治疗HCC具有很大的应用前景。关键词:铁死亡;癌,肝细胞;肿瘤抑制蛋白质p53 基金项目:国家...
Lain et al (2008) Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator. Cancer Cell 13 454. PMID: 18455128.Lain, S., J.J. Hollick, J. Campbell, O.D. Staples, M. Higgins, M. Aoubala, A. McCarthy, V. Appleyard, K.E. Murray, L. Baker, et ...
Mutant p53 in cancer: from molecular mechanism to therapeutic modulation Introduction The tumor suppressor geneTP53is the most frequently mutated gene in human tumors.1,2The process of tumor development is strongly related to the dysfunctions caused byTP53mutations.3,4p53 protein functions primarily a...
Despite its well demonstrated role in control of p53 function, the mechanism of action of PPM1D is not well defined. It has been shown that PPM1D removes phosphate groups from both p53 and MDM210,11 and that it can also dephosphorylate key mediators of the DNA-damage response such as ATM...
At the same time, given that many aspects of p53 regulation have been studied, we envisaged that identifying testable hypotheses relating to the mechanism of action of hit compounds in cells was achievable. Here, we describe the discovery and characterization of a bioactive small-molecule activator...
Two, phase Ib/II clinical trials with APR-246 have been concluded so far. Both studies were designed to recruit patients withTP53gene mutations based on the primary mechanism of action of the drug. One study, for the safety and efficacy of APR-246 in combination with azacitidine and to asse...
Cancer-selective therapy of the future: apoptin and its mechanism of action. Classical chemotherapy, that specifically targets rapidly proliferating cells, has been in existence for over eighty years and has proven to be fully succe... S Maddika,FJ Mendoza,K Hauff,... - 《Cancer Biology & Th...
Although p53 is thought to suppress cancer by inducing growth arrest or apoptosis in response to cellular stress signals, its molecular mechanism of action in tumor suppression has remained unclear. p53 is a transcriptional activator that can induce numerous target genes, but it also displays other ...
m Schematic representation of mechanism of action of two antitumor drugs, KuDOS (KU-55933) and etoposide, and their effects on the activation of ATM serine/threonine kinase and p53 protein. n, o D2 mRNA expression was measured by Real-Time PCR in SCC011 (n) and SCC13 (o) cells, ...
The particularly offensive, and often even life-threatening and difficult to restrain side effects, significantly degrade the quality of life of patients and are often responsible for the cessation of therapy. This is the result of a non-specific mechanism of action and the low selectivity of ...