104261-03-2Relevant academic research and scientific papers
Activity-based protein profiling reveals GSTO1 as the covalent target of piperlongumine and a promising target for combination therapy for cancer
Li, Li,Zhao, Yue,Cao, Ran,Li, Lin,Cai, Gaihong,Li, Jiaojiao,Qi, Xiangbing,Chen, She,Zhang, Zhiyuan
, p. 4407 - 4410 (2019/04/26)
Through systematic target identification for piperlongumine, a cancer-selective killing molecule, we identified GSTO1 as its major covalent target for cancer cell death induction. We also reveal that GSTO1 inhibition is a promising combination strategy with other anti-cancer agents by drug combination screening in which piperlongumine exhibits broad-spectrum synergistic effects with a large proportion of the tested anti-cancer agents, especially with PI3K/Akt/mTOR pathway inhibitors.
Inter- and intraspecific comparisons of antiherbivore defenses in three species of rainforest understory shrubs
Fincher,Dyer,Dodson,Richards,Tobler,Searcy,Mather,Reid,Rolig,Pidcock
, p. 558 - 574 (2008/09/20)
Plants defend themselves against herbivores and pathogens with a suite of morphological, phenological, biochemical, and biotic defenses, each of which is presumably costly. The best studied are allocation costs that involve trade-offs in investment of resources to defense versus other plant functions. Decreases in growth or reproductive effort are the costs most often associated with antiherbivore defenses, but trade-offs among different defenses may also occur within a single plant species. We examined trade-offs among defenses in closely related tropical rain forest shrubs (Piper cenocladum, P. imperiale, and P. melanocladum) that possess different combinations of three types of defense: ant mutualists, secondary compounds, and leaf toughness. We also examined the effectiveness of different defenses and suites of defenses against the most abundant generalist and specialist Piper herbivores. For all species examined, leaf toughness was the most effective defense, with the toughest species, P. melanocladum, receiving the lowest incidence of total herbivory, and the least tough species, P. imperiale, receiving the highest incidence. Although variation in toughness within each species was substantial, there were no intraspecific relationships between toughness and herbivory. In other Piper studies, chemical and biotic defenses had strong intraspecific negative correlations with herbivory. A wide variety of defensive mechanisms was quantified in the three Piper species studied, ranging from low concentrations of chemical defenses in P. imperiale to a complex suite of defenses in P. cenocladum that includes ant mutualists, secondary metabolites, and moderate toughness. Ecological costs were evident for the array of defensive mechanisms within these Piper species, and the differences in defensive strategies among species may represent evolutionary trade-offs between costly defenses.
Diels-Alder Reaction of the N-Protected 3-Phenylthio-2(1H)-dihydropyridinone Derivatives
Torisawa, Yasuhiro,Nakagawa, Masako,Takami, Hideo,Nagata, Toshiaki,Ali, Mohamed Ayman,et al.
, p. 277 - 292 (2007/10/02)
Efficient methods for the preparation of N-protected 3-phenylthio-2(1H)-dihydropyridinones from 2-piperidone and their Diels-Alder reaction with 2-trimethylsilyloxybutadiene are described.The role of the electron-withdrawing N-protecting group in the dienophiles is rationalized in terms of the lowered energy level in LUMO.
