13036-02-7Relevant articles and documents
Targeting Tumor Associated Phosphatidylserine with New Zinc Dipicolylamine-Based Drug Conjugates
Liu, Yu-Wei,Shia, Kak-Shan,Wu, Chien-Huang,Liu, Kuan-Liang,Yeh, Yu-Cheng,Lo, Chen-Fu,Chen, Chiung-Tong,Chen, Yun-Yu,Yeh, Teng-Kuang,Chen, Wei-Han,Jan, Jiing-Jyh,Huang, Yu-Chen,Huang, Chen-Lung,Fang, Ming-Yu,Gray, Brian D.,Pak, Koon Y.,Hsu, Tsu-An,Huang, Kuan-Hsun,Tsou, Lun K.
, p. 1878 - 1892 (2017)
A series of zinc(II) dipicolylamine (ZnDPA)-based drug conjugates have been synthesized to probe the potential of phosphatidylserine (PS) as a new antigen for small molecule drug conjugate (SMDC) development. Using in vitro cytotoxicity and plasma stability studies, PS-binding assay, in vivo pharmacokinetic studies, and maximum tolerated dose profiles, we provided a roadmap and the key parameters required for the development of the ZnDPA based drug conjugate. In particular, conjugate 24 induced tumor regression in the COLO 205 xenograft model and exhibited a more potent antitumor effect with a 70% reduction of cytotoxic payload compared to that of the marketed irinotecan when dosed at the same regimen. In addition to the validation of PS as an effective pharmacodelivery target for SMDC, our work also provided the foundation that, if applicable, a variety of therapeutic agents could be conjugated in the same manner to treat other PS-associated diseases.
Mechanical Properties of a Metal-Organic Framework formed by Covalent Cross-Linking of Metal-Organic Polyhedra
Lal, Garima,Derakhshandeh, Maziar,Akhtar, Farid,Spasyuk, Denis M.,Lin, Jian-Bin,Trifkovic, Milana,Shimizu, George K. H.
, p. 1045 - 1053 (2019)
Overcoming the brittleness of metal-organic frameworks (MOFs) is a challenge for industrial applications. To increase the mechanical strength, MOFs have been blended with polymers to form composites. However, this also brings challenges, such as integration and integrity of MOF in the composite, which can hamper the selectivity of gas separations. In this report, an "all MOF" material with mechanical flexibility has been prepared by covalent cross-linking of metal-organic polyhedra (MOPs). The ubiquitous Cu24 isophthalate MOP has been decorated with a long alkyl chain having terminal alkene functionalities so that MOPs can be cross-linked via olefin metathesis using Grubbs second generation catalyst. Different degrees of cross-linked MOP materials have been obtained by varying the amount of catalyst in the reaction. Rheology of these structures with varying number of cross-links was performed to assess the cross-link density and its homogeneity throughout the sample. The mechanical properties were further investigated by the nanoindentation method, which showed increasing hardness with higher cross-link density. Thus, this strategy of cross-linking MOPs with covalent flexible units allows us to create MOFs of increasing mechanical strength while retaining the MOP cavities.
All solution-processed red organic light-emitting diode based on a new thermally cross-linked heteroleptic Ir(iii) complex
Cho, Woosum,Reddy, Saripally Sudhaker,Kim, Junyoung,Cho, Young-Rae,Jin, Sung-Ho
, p. 11714 - 11721 (2018)
A novel cross-linkable red iridium(iii) complex and electron transport material were designed and synthesized for use in the fabrication of solution-processed phosphorescent organic light-emitting diodes (PHOLEDs). The newly cross-linkable red Ir(iii) complex was successfully thermal cross-linked with a cross-linkable host in the emitting layer (EML). After cross-linking, the EML was found not to be damaged by organic solvents. A maximum external quantum efficiency (EQE) of 4.64% (2.77 cd A-1) was achieved for deep-red PHOLEDs after rinsing, which was similar to the EQE of 4.59% (2.52 cd A-1) after rinsing the deep-red PHOLEDs with thermal cross-linking.
Multifunctional Fullerene Derivative for Interface Engineering in Perovskite Solar Cells
Li, Yaowen,Zhao, Yue,Chen, Qi,Yang, Yang (Michael),Liu, Yongsheng,Hong, Ziruo,Liu, Zonghao,Hsieh, Yao-Tsung,Meng, Lei,Li, Yongfang,Yang, Yang
, p. 15540 - 15547 (2015)
In perovskite based planar heterojunction solar cells, the interface between the TiO2 compact layer and the perovskite film is critical for high photovoltaic performance. The deep trap states on the TiO2 surface induce several challenging issues, such as charge recombination loss and poor stability etc. To solve the problems, we synthesized a triblock fullerene derivative (PCBB-2CN-2C8) via rational molecular design for interface engineering in the perovskite solar cells. Modifying the TiO2 surface with the compound significantly improves charge extraction from the perovskite layer. Together with its uplifted surface work function, open circuit voltage and fill factor are dramatically increased from 0.99 to 1.06 V, and from 72.2percent to 79.1percent, respectively, resulting in 20.7percent improvement in power conversion efficiency for the best performing devices. Scrutinizing the electrical properties of this modified interfacial layer strongly suggests that PCBB-2CN-2C8 passivates the TiO2 surface and thus reduces charge recombination loss caused by the deep trap states of TiO2. The passivation effect is further proven by stability testing of the perovskite solar cells with shelf lifetime under ambient conditions improved by a factor of more than 4, from ～40 h to ～200 h, using PCBB-2CN-2C8 as the TiO2 modification layer. This work offers not only a promising material for cathode interface engineering, but also provides a viable approach to address the challenges of deep trap states on TiO2 surface in planar perovskite solar cells.
Molecular Scaffolds as Double-Targeting Agents For the Diagnosis and Treatment of Neuroblastoma
Villaverde, Gonzalo,Alfranca, Arantzazu,Gonzalez-Murillo, áfrica,Melen, Gustavo J.,Castillo, Rafael R.,Ramírez, Manuel,Baeza, Alejandro,Vallet-Regí, María
supporting information, p. 3067 - 3072 (2019/01/14)
The selective delivery of therapeutic and imaging agents to tumoral cells has been postulated as one of the most important challenges in the nanomedicine field. Meta-iodobenzilguanidine (MIBG) is widely used for the diagnosis of neuroblastoma (NB) due to its strong affinity for the norepinephrine transporter (NET), usually overexpressed on the membrane of malignant cells. Herein, a family of novel Y-shaped scaffolds has been synthesized, which have structural analogues of MIBG covalently attached at each end of the Y-structure. The cellular uptake capacity of these double-targeting ligands has been evaluated in vitro and in vivo, yielding one specific Y-shaped structure that is able to be engulfed by the malignant cells, and accumulates in the tumoral tissue, at significantly higher levels than the structure containing only one single targeting agent. This Y-shaped ligand can provide a powerful tool for the current treatment and diagnosis of this disease.
Molecular Swings as Highly Active Ion Transporters
Ren, Changliang,Chen, Feng,Ye, Ruijuan,Ong, Yong Siang,Lu, Hongfang,Lee, Su Seong,Ying, Jackie Y.,Zeng, Huaqiang
supporting information, p. 8034 - 8038 (2019/05/16)
Ions are transported across membrane mostly via carrier or channel mechanisms. Herein, a unique class of molecular-machine-inspired membrane transporters, termed molecular swings is reported that utilize a previously unexplored swing mechanism for promoting ion transport in a highly efficient manner. In particular, the molecular swing, which carries a 15-crown-5 unit as the ion-binding and transporting unit, exhibits extremely high ion-transport activities with EC50 values of 46 nm (a channel:lipid molar ratio of 1:4800 or 0.021 mol % relative to lipid) and 110 nm for K+ and Na+ ions, respectively. Remarkably, such ion transport activities remain high in a cholesterol-rich environment, with EC50 values of 130 (0.045 mol % relative to lipid/cholesterol) and 326 nm for K+ and Na+ ions, respectively.
