Design, synthesis and pharmacological characterization of analogs of 2-aminoethyl diphenylborinate (2-APB), a known store-operated calcium channel blocker, for inhibition of TRPV6-mediated calcium transport

2-Aminoethyl diphenylborinate (2-APB) is a known modulator of the IP3 receptor, the calcium ATPase SERCA, the calcium release-activated calcium channel Orai and TRP channels. More recently, it was shown that 2-APB is an efficient inhibitor of the epithelial calcium channel TRPV6 which is overexpressed in prostate cancer. We have conducted a structure-activity relationship study of 2-APB congeners to understand their inhibitory mode of action on TRPV6. Whereas modifying the aminoethyl moiety did not significantly change TRPV6 inhibition, substitution of the phenyl rings of 2-APB did. Our data show that the diaryl borinate moiety is required for biological activity and that the substitution pattern of the aryl rings can influence TRPV6 versus SOCE inhibition. We have also discovered that 2-APB is hydrolyzed and transesterified within minutes in solution.

Network Store: Exploring Slicing in Future 5G Networks

In this paper, we present a revolutionary vision of 5G networks, in which SDN programs wireless network functions, and where Mobile Network Operators (MNO), Enterprises, and Over-The-Top (OTT) third parties are provided with NFV-ready Network Store. The proposed Network Store serves as a digital distribution platform of programmable Virtualized Network Functions (VNFs) that enable 5G application use-cases. Currently existing application stores, such as Apple's App Store for iOS applications, Google's Play Store for Android, or Ubuntu's Software Center, deliver applications to user specific software platforms. Our vision is to provide a digital marketplace, gathering 5G enabling Network Applications and Network Functions, written to run on top of commodity cloud infrastructures, connected to remote radio heads (RRH). The 5G Network Store will be the same to the cloud as the application store is currently to a software platform.