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Search results for: MODULATORS
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Tannins as Hemostasis Modulators
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Potential allosteric modulators of the proteasome activity
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Synthetic genistein derivatives as modulators of glycosaminoglycan storage
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Modified Peptide Molecules As Potential Modulators of Shelterin Protein Functions; TRF1
PublicationIn this work, we present studies on relatively new and still not well-explored potential anticancer targets which are shelterin proteins, in particular the TRF1 protein can be blocked by in silico designed "peptidomimetic" molecules. TRF1 interacts directly with the TIN2 protein, and this protein-protein interaction is crucial for the proper functioning of telomere, which could be blocked by our novel modified peptide molecules....
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Novel Quaternary TlGaSn2Se6 Single Crystal as Promising Material for Laser Operated Infrared Nonlinear Optical Modulators
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Efflux Pump Blockers in Gram-Negative Bacteria: The New Generation of Hydantoin Based-Modulators to Improve Antibiotic Activity
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Search for ABCB1 Modulators Among 2-Amine-5-Arylideneimidazolones as a New Perspective to Overcome Cancer Multidrug Resistance
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Evaluation and cellular responses of modulators of TRF1/TRF2 protein’s function as potential anticancer drugs interfering with telomeric shelterin’s function
PublicationA number of proteins that interact with telomeres have been identified in human cells, indicating the high plasticity of human nucleoprotein complex organization. The most important complex is the "shelterin" complex, which consists of six proteins: TRF1, TRF2, TIN2, POT1, TPP1. The TRF1 and TRF2 directly bind to telomeric double-stranded DNA and the TIN2 protein. The TIN2 protein also binds to the TPP1 protein, stabilizing the...
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The Effect of Physical Activity and Repeated Whole-Body Cryotherapy on the Expression of Modulators of the Inflammatory Response in Mononuclear Blood Cells among Young Men
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Morphology control through the synthesis of metal-organic frameworks
PublicationDesignable morphology and predictable properties are the most challenging goals in material engineering. Features such as shape, size, porosity, agglomeration ratio significantly affect the final properties of metal- organic frameworks (MOFs) and can be regulated throughout synthesis parameters but require a deep under- standing of the mechanisms of MOFs formation. Herein, we systematically summarize the effects of the indi- vidual...
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Polarization-dependent optical absorption in phosphorene flakes
PublicationThe interest of 2D materials is constantly increasing because of their very attractive mechanical, electrical and optical parameters. They have been used in many applications, e.g. photodetectors, sensors, modulators, insulators. One of the recently discovered 2D materials is phosphorene. In contrast to graphene, phosphorene has a direct bandgap tuned by numbers of layers in the 2D structure. The phosphorene flakes are strongly...
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FPGA-Based System for Electromagnetic Interference Evaluation in Random Modulated DC/DC Converters
PublicationField-Programmable Gate Array (FPGA) provides the possibility to design new “electromagnetic compatibility (EMC) friendly” control techniques for power electronic converters. Such control techniques use pseudo-random modulators (RanM) to control the converter switches. However, some issues connected with the FPGA-based design of RanM, such as matching the range of fixed-point numbers, might be challenging. The modern programming...
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Two-Dimensional Gas Chromatography Coupled With Mass Spectrometry in Food Analysis
PublicationThe development of instrumental analytical techniques provided the opportunity for in-depth characterization of many food matrices. In particular, the use of gas chromatography coupled with mass spectrometry gives impressive results in terms of quality and authenticity testing, conducting food freshness evaluations and contamination assessments. A new variant of gas chromatography, namely two-dimensional gas chromatography (GC...
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Optimization of Chemical Functionalities of Indole-2-carboxamides To Improve Allosteric Parameters for the Cannabinoid Receptor 1 (CB1)
Publication5-Chloro-3-ethyl-N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide (1; ORG27569) is a prototypical allosteric modulator for the cannabinoid type 1 receptor (CB1). Here, we reveal key structural requirements of indole-2-carboxamides for allosteric modulation of CB1: a critical chain length at the C3-position, an electron withdrawing group at the C5-position, the length of the linker between the amide bond and the phenyl ring...
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Discovery of small-molecule regenerative drugs using a model of complex tissue injury in mice. Transcriptomic responses of neurodevelopmental genes during pharmacologically induced regeneration
PublicationDespite significant development in regenerative medicine, there is a deficit of effective therapies for wound healing and tissue regeneration. Research performed using animal wound models allows for a better understanding of this complex process, searching for compounds with pro-regenerative properties, and assessing their efficacy and safety. Unfortunately, the lack of adequate preclinical models proves to be an issue as no animal...
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In vivoevaluation of the CB1allosteric modulator LDK1258 reveals CB1-receptor independent behavioral effects
PublicationIn the present study, we examined whether LDK1258, which produces strong CB1receptor allosteric effects ininvitroassays, would elicitin vivoeffects consistent with allosteric activity. In initial studies, LDK1258 reducedfood consumption and elicited delayed antinociceptive effects in the chronic constrictive injury of the sciaticnerve (CCI) model of neuropathic pain, which unexpectedly emerged 4 h post-injection. UPLC-MS/MS analysisquantified...