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br Acknowledgments The authors gratefully
2022-06-16
Acknowledgments The authors gratefully acknowledge the financial support of this study by STCU Project 6052 “Enzyme multibiosensor system for renal dysfunction diagnosis and hemodialysis control”. Furthermore, this study was supported by NASU in the frame of Scientific and Technical Program “Sens
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Anti apoptotic Bcl proteins have
2022-06-16
Anti-apoptotic Bcl-2 proteins have become attractive targets for anti-cancer agents development, because they are associated with progression of a wide variety of human cancers., , The small-molecular Bcl-2 inhibitor venetoclax (ABT-199) () has been approved recently for the treatment of patients wi
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Numerous strategies of cardiomyocyte protection are effectiv
2022-06-16
Numerous strategies of cardiomyocyte protection are effective in preclinical, animal models and in small clinical trials. However, most have disappointed in large clinical trials [4,5]. Failures of cyclosporine and post-conditioning to mitigate reperfusion injury are recent examples [[6], [7], [8]].
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Under increased drug pressure more
2022-06-16
Under increased drug pressure, more protease variants with more than one substitution will likely become clinically relevant. The accumulation of additional substitutions can allow RAS variants to emerge that alone are not viable, but in combination can rescue the viral fitness. We previously demons
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An interesting question is why RhoF has such the slow
2022-06-16
An interesting question is why RhoF has such the slow rate of GDP dissociation. The amino DMPO mutations in a presumable GDP-binding site of RhoF had only moderate effects on the GDP dissociation (Fig. 3C), which suggests a mechanism involving the global amino acid sequence of RhoF, rather than the
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Considering its role in regulating
2022-06-16
Considering its role in regulating cytoskeletal dynamics, the Rho kinase effector ROCK has been particularly implicated in tumor metastasis. The ROCK inhibitors Y27632 and fasudil have been extensively studied in cancer and beneficial effects have been observed in many types of cancers (Kale et al.,
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Calcein acetoxymethyl ester In order to elucidate the mechan
2022-06-16
In order to elucidate the mechanisms behind the observed changes in metabolic activity in the cardiomyoblasts we investigated changes in gene and protein expression subsequent to treatment with PSN632408 with or without concurrent exposure to palmitate. Activating GPR119 in basal and high palmitate
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Indeed it was shown further in VSV
2022-06-16
Indeed, it was shown further in VSV G that the H80A mutation, and the E123L and D121L double mutation, which both abolish VSV G fusion properties, were rescued by the same compensatory Q112P mutation. In a single FD, residue 112 is located on the opposite side of the three-stranded β-sheet and is fa
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Heterocysts provide the required microoxic environment for t
2022-06-16
Heterocysts provide the required microoxic environment for the oxygen-sensitive N2-fixing nitrogenase enzyme complex. This environment is formed during heterocyst development. Developing heterocysts inactivate photosystem II and degrade antenna pigments, thereby decreasing oxygenic photosynthesis (F
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br Results and discussion A diverse set of compounds were
2022-06-16
Results and discussion A diverse set of compounds were synthesized to improve the PK and physicochemical properties of 2. Compounds' agonist effects on hGPR40 were assessed by calcium mobilization assay using hGPR40-HEK293 cell line which stably expressed human GPR40. Preliminary explorations fo
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Experiments show that CSD propagation can
2022-06-15
Experiments show that CSD propagation can be slowed or interrupted by pre-existing lesions or areas of high astrocytic density (Chen et al., 2006), and reduced expression of astrocytic gap junctions significantly increases the size of ischemic infarcts (Nakase et al., 2003). By decreasing the gap ju
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Two intermediate compounds A and
2022-06-15
Two intermediate compounds (A and B in Fig. 1) were tested for both Aβ40 and CYP3A4 inhibition activity. Potential hydrolysis of structures I and IIin vivo may produce A which is a strong CYP3A4 inhibitor. Cyclopropanol group is a suspected liability, because NIBR189 B without it has a clean CYP3A4
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Mallory stained sections showed significant increase in coll
2022-06-15
Mallory stained sections showed significant increase in collagen fiber deposition around the hepatic nodules together with significant increase in positive immune-reaction to α-SMA in TAA-treated group. This was in accordance with previous studies which reported that myofibroblasts which were develo
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The objective of this study is to
2022-06-15
The objective of this study is to design and synthesize drug-like molecules with agonistic activity on both receptors; PPARγ and FFAR1. These agents would act as insulin sensitizers and insulin secretagogues through their action on PPARγ and FFAR1, respectively. The design of drugs with dual mode of
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The presence of FBP in nuclei seems to accompany
2022-06-15
The presence of FBP2 in nuclei seems to accompany the cells' potential to divide as it has been shown that during differentiation of the satellite cells (myogenic progenitor cells) the amount of nuclear FBP2 decreases and in differentiated myotubes, the localisation of FBP2 is restricted to cytoplas
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