Eduard A. Sergienko

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Visual-perceptual, attentional, and visual-motor skills were examined in a group of 16 school-age children, born at 27-32 gestational weeks, who had performed normally on pediatric screening tests. Compared with 16 matched full-term controls, the preterms performed poorly on only two measures: they took longer to point to the missing arc of an annulus(More)
Herein we present the outcome of a high throughput screening (HTS) campaign-based strategy for the rapid identification and optimization of selective and general chemotypes for both kappa (κ) opioid receptor (KOR) activation and inhibition. In this program, we have developed potent antagonists (IC(50) < 120 nM) or agonists of high binding affinity (K(i) < 3(More)
Quiescin sulfhydryl oxidase 1 (QSOX1) is a highly conserved disulfide bond-generating enzyme that is overexpressed in diverse tumor types. Its enzymatic activity promotes the growth and invasion of tumor cells and alters extracellular matrix composition. In a nude mouse-human tumor xenograft model, tumors containing shRNA for QSOX1 grew significantly more(More)
A high throughput screen for compounds that induce TRAIL-mediated apoptosis identified ML100 as an active chemical probe, which potentiated TRAIL activity in prostate carcinoma PPC-1 and melanoma MDA-MB-435 cells. Follow-up in silico modeling and profiling in cell-based assays allowed us to identify NSC130362, pharmacophore analog of ML100 that induced(More)
Binding of leukocyte specific integrin CD11b/CD18 to its physiologic ligands is important for the development of normal immune response in vivo. Integrin CD11b/CD18 is also a key cellular effector of various inflammatory and autoimmune diseases. However, small molecules selectively inhibiting the function of integrin CD11b/CD18 are currently lacking. We(More)
BACKGROUND Intracellular proteases constitute a class of promising drug discovery targets. Methods for high throughput screening against these targets are generally limited to in vitro biochemical assays that can suffer many technical limitations, as well as failing to capture the biological context of proteases within the cellular pathways that lead to(More)
Late effects of early visual deprivation on state control in sleep were studied in 23 infants with bilateral congenital cataract before and after surgery (usually, on the 6th month of life). In the course of three years 67 observations were performed. Laboratory assessments included videotaping infant sleep behaviour, recording EEG, EOG, ECG, galvanic skin(More)
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