- Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγInverse Agonist for Treatment of Castration-Resistant Prostate Cancer
-
We report the design, optimization, and biological evaluation of nuclear receptor RORγinverse agonists as therapeutic agents for prostate cancer treatment. The most potent compound 27 (designated as XY101) exhibited cellular activity with an IC50/su
- Zhang, Yan,Wu, Xishan,Xue, Xiaoqian,Li, Chenchang,Wang, Junjian,Wang, Rui,Zhang, Cheng,Wang, Chao,Shi, Yudan,Zou, Lingjiao,Li, Qiu,Huang, Zenghong,Hao, Xiaojuan,Loomes, Kerry,Wu, Donghai,Chen, Hong-Wu,Xu, Jinxin,Xu, Yong
-
p. 4716 - 4730
(2019/05/08)
-
- Designed to dissolve: Suppression of colloidal aggregation of Cu(I)-selective fluorescent probes in aqueous buffer and in-gel detection of a metallochaperone
-
Due to the lipophilicity of the metal-ion receptor, previously reported Cu(I)-selective fluorescent probes form colloidal aggregates, as revealed by dynamic light scattering. To address this problem, we have developed a hydrophilic triarylpyrazoline-based fluorescent probe, CTAP-2, that dissolves directly in water and shows a rapid, reversible, and highly selective 65-fold fluorescence turn-on response to Cu(I) in aqueous solution. CTAP-2 proved to be sufficiently sensitive for direct in-gel detection of Cu(I) bound to the metallochaperone Atox1, demonstrating the potential for cation-selective fluorescent probes to serve as tools in metalloproteomics for identifying proteins with readily accessible metal-binding sites.
- Morgan, M. Thomas,Bagchi, Pritha,Fahrni, Christoph J.
-
p. 15906 - 15909
(2011/11/12)
-
- Methods for the use of inhibitors of cytosolic phospholipase A2 in the treatment of thrombosis
-
This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds in the treating or preventing thrombosis in a mammal, or preventing progression of symptoms of thrombosis.
- -
-
Page/Page column 21-22
(2010/11/29)
-
- Process for making an aldehyde
-
A process for making an aromatic aldehyde in which a sulfoxide is reacted with a dihalogenated aromatic compound in the absence of an effective amount of an activating reagent. The aldehyde may then be used to make other compounds, such as a compound that acts as a cPLA inhibitor.
- -
-
-