80410-57-7Relevant articles and documents
Probing the Intracellular Dynamics of Nitric Oxide and Hydrogen Sulfide Using an Activatable NIR II Fluorescence Reporter
Zhu, Tianli,Ren, Ning,Liu, Xia,Dong, Yan,Wang, Rongchen,Gao, Jinzhu,Sun, Jie,Zhu, Ying,Wang, Lihua,Fan, Chunhai,Tian, He,Li, Jiang,Zhao, Chunchang
supporting information, p. 8450 - 8454 (2021/03/08)
Understanding the complex interplay among gasotransmitters is of great significance but remains technically challenging. In this study, we present the design and synthesis of a dually responsive BOD-NH-SC reporter for probing the dynamic and alternating existence of NO and H2S in living cells. This designed reporter can repeatedly cycle S-nitrosation and transnitrosation reactions when successively treated with NO and H2S, thus affording the interchange of NIR fluorescence at 645 nm (NO) and NIR II fluorescence at 936 nm (H2S). In light of this unique fluorescence alternation between two colors, we synthesized water-soluble BOD-NH-SC dots to visualize the intracellular dynamics of NO and H2S. These molecular probes thus provide a toolbox to elucidate the interplaying roles of NO and H2S in the complex interaction networks of various signal transduction pathways.
Affinity-Driven Covalent Modulator of the Glyceraldehyde-3-Phosphate Dehydrogenase (GAPDH) Cascade
Chern, Jeffy,Lu, Chun-Ping,Fang, Zhanxiong,Chang, Ching-Ming,Hua, Kuo-Feng,Chen, Yi-Ting,Ng, Cheng Yang,Chen, Yi-Lin Sophia,Lam, Yulin,Wu, Shih-Hsiung
supporting information, p. 7040 - 7045 (2018/05/29)
Traditional medicines provide a fertile ground to explore potent lead compounds, yet their transformation into modern drugs is fraught with challenges in deciphering the target that is mechanistically valid for its biological activity. Herein we reveal that (Z)-(+)-isochaihulactone (1) exhibited significant inhibition against multiple-drug-resistant (MDR) cancer cell lines and mice xenografts. NMR spectroscopy showed that 1 resisted an off-target thiolate, thus indicating that 1 was a target covalent inhibitor (TCI). By identifying the pharmacophore of 1 (α,β-unsaturated moiety), a probe derived from 1 was designed and synthesized for TCI-oriented activity-based proteome profiling. By MS/MS and computer-guided molecular biology approaches, an affinity-driven Michael addition of the noncatalytic C247 residue of GAPDH was found to control the “ON/OFF” switch of apoptosis through non-canonically nuclear GAPDH translocation, which bypasses the common apoptosis-resistant route of MDR cancers.
PISTON FOR AN INTERNAL COMBUSTION ENGINE AND METHOD FOR PRODUCING THE PISTON FOR AN INTERNAL COMBUSTION ENGINE
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, (2018/08/03)
The present invention relates to compounds of general formula (I), wherein A represents an optionally substituted heterocycle group, B represents an aryl or heteroaryl group and wherein X, R1, R2, R3, R4 and R5 are as defined in the description. Compounds of formula (I) are useful to destroy, inhibit, or prevent the growth or spread of cells, especially malignant cells, into surrounding tissues implicated in a variety of human and animal diseases.