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Despite the emerging success of multi-targeted protein tyrosine kinase (PTK) inhibitors in cancer therapy, significant side effects and resistance concerns seems to be avoided unlikely. The aim of the present study was to identify novel multi-targeting PTK inhibitors. The kinase enzymatic activities were measured by enzyme-linked immunosorbent assay(More)
We report here the discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase by adopting a strategy integrating focused combinatorial library design, virtual screening, chemical synthesis, and bioassay. Thirty two compounds were selected and synthesized. All compounds showed potent inhibitory activity(More)
The IκB kinase complex (IKK) is a key regulator of immune responses, inflammation, cell survival, and tumorigenesis. The prosurvival function of IKK centers on activation of the transcription factor NF-κB, whose target gene products inhibit caspases and prevent prolonged JNK activation. Here, we report that inactivation of the BH3-only protein BAD by IKK(More)
Quercetin-3-O-amino acid-esters, a new type of quercetin derivatives, were successfully prepared for the first time. Different from quercetin, the novel compounds show higher selectivity as inhibitors against Src tyrosine kinase (IC(50) values ranging from 3.2 microM to 9.9 microM) than against EGFR tyrosine kinase. Molecular docking reveals that both(More)
We demonstrate a noncollinear optical parametric chirped-pulse amplification scheme for generating high-peak-power tunable mid-infrared (IR) pulses. The high-gain LiNbO(3)-based noncollinear parametric amplifier, seeded by a tunable femtosecond optical parametric amplifier, provides a wide wavelength tuning range from 3.3 to 3.95 μm and a large saturated(More)
Real-time pulse-contrast observation with a high dynamic range is a prerequisite to tackle the contrast challenge in ultra-high peak-power lasers. However, the commonly used delay-scanning cross-correlator (DSCC) can only provide the time-consumed measurements for repetitive lasers. Single-shot cross-correlator (SSCC) becomes essential in optimizing laser(More)
Optical noise, the core of the pulse-contrast challenge for ultra-high peak power femtosecond lasers, exhibits spatiotemporal (ST) coupling induced by angular dispersion. Full characterization of such ST noise requires two-dimensional measurements in the ST domain. Thus far, all noise measurements have been made only in the temporal domain. Here we report(More)
We experimentally study a new kind of parametric noise that is initiated from signal scattering and enhanced through optical parametric amplification. Such scattering-initiated parametric noise behaves similarly to parametric super-fluorescence in the spatial domain, yet is typically much stronger. In the time domain it inherits the chirp of signal pulses(More)
We propose a novel single-shot pulse-contrast measurement approach based on high-order quasi-phase-matching (QPM) cross correlation. It supports perfect contrast measurement with features of no artifacts, high resolution, and large temporal window. The prototype experiment based on the noncollinear third QPM with a beam crossing angle of 90 deg, using(More)
We report a method for filtering out the noises produced in optical parametric chirped-pulse amplifiers by dressing the seed beam with spatial chirp. After dechirping the amplified signal with a compressor, the noises experience a spatiotemporal coupling, making themselves highly distinguishable from the compressed signal in space, and hence supporting(More)