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One important discovery of our study is the identification
2021-12-17

One important discovery of our study is the identification of a pharmacological mechanism for the macrolide antibiotic erythromycin (EM) in promoting joint health. EM is a commonly used antibiotic that directly binds bacterial ribosomes to inhibit protein synthesis [66]. Although EM-like macrolide M
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Analysis of published albumin X ray structures
2021-12-16

Analysis of published albumin X-ray structures had suggested that an allosteric link may exist, but could not establish whether Zn2+ prevented FFA binding or vice versa. This question was answered through competition experiments monitored by isothermal titration calorimetry (ITC; Fig. 3) for BSA [55
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br Clinical development of FGFR inhibitors in breast cancer
2021-12-16

Clinical development of FGFR inhibitors in breast cancer The rationale to explore the role of FGFR inhibitors in patients with breast cancer comes from a variety of sources. These include genomic aberrations frequently identified in the FGF/FGFR pathway in breast cancer, the increased sensitivity
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br Declaration of interest br
2021-12-16

Declaration of interest Acknowledgments This work was supported by grants from the Polish National Science Centre (PRELUDIUM grant no. 2013/11/N/NZ5/00270) and the European Commission FP7 Project Beta-JUDO (grant number 279 153), European Union EIT Health project DeTecT2D, Swedish Diabetes A
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Sirolimus rapamycin and everolimus both of which
2021-12-16

Sirolimus (rapamycin) and everolimus, both of which are mTOR inhibitors, are released by commonly used first- and second-generation DES. Considering the relatively high rates of the target vessel failure with currently available DES [12,14,16,45,46], there is a need for a novel drug strategy that pr
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Integrin engagement triggers activation of
2021-12-16

Integrin engagement triggers activation of several signaling pathway including Fak, which is recognized as the key signal transduction factor in the integrin signaling pathway that functions by activating downstream signaling in focal adhesion plaques. Whether changes in integrin-FAK signaling pathw
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BQ-788 sodium salt The synthesis of substituted pyrimidinone
2021-12-16

The synthesis of 2-substituted pyrimidinone carboxamides – is outlined in , . Treatment of readily accessible nitriles with N-methylhydroxylamine hydrochloride in the presence of BQ-788 sodium salt provided the adducts , which were subsequently reacted with diethyl acetylenedicarboxylate to afford i
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Over the last years numerous studies gave
2021-12-16

Over the last 15 years, numerous studies gave insights into sGC activation and binding of activators: Photoaffinity labelling studies with cinaciguat suggested the N-terminus of the β1 subunit as target region for this new drug [17]. Schmidt et al. identified the amino acids tyrosine 135, serine 137
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Furthermore increased plasma levels of endoglin have been as
2021-12-16

Furthermore, increased plasma levels of endoglin have been associated with diabetic complications (Valbuena-Diez et al., 2012). The involvement of soluble endoglin in a number of widespread pathologies demonstrates that endoglin is not only marker of endothelial integrity but also a causative factor
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ampk inhibitor The study of TcMYH protein is a
2021-12-16

The study of TcMYH protein is a step forward for the characterization of a GO system in T. cruzi. The complete system appears to be present and our findings demonstrate that is important to maintain DNA stability of the nuclear and mitochondrial genomes, particularly in the presence of oxidative str
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MC 1568 br Introduction Maintaining blood glucose within
2021-12-16

Introduction Maintaining blood glucose within an appropriate range is crucial for survival. In diabetes, those who suffer episodes of severe hypoglycemia have an increased risk of death [1], [2]. The MC 1568 is especially dependent on an adequate, continuous supply of circulating glucose to fuel
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br Regulation of GCK by intrinsic conformational dynamics
2021-12-16

Regulation of GCK by intrinsic conformational dynamics GCK is a 465-residue, 52-kDa enzyme comprised of two domains, hereafter referred to as the large domain and the small domain, that are separated by a flexible hinge region. As with other proteins that adopt the hexokinase fold, substrates bin
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The present study demonstrates that
2021-12-16

The present study demonstrates that SNAP 37889 exhibits a toxic effect to these specific cell types, which is independent of endogenous expression of GAL receptor subtypes and leads to apoptosis. This conclusion is based on our findings that, although HMCB, HL-60 and SH-SY5Y cell lines differ in GAL
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br Conclusion br Acknowledgement br Introduction Biogenic am
2021-12-15

Conclusion Acknowledgement Introduction Biogenic amine histamine is synthesized from L-histidine by histidine decarboxylase (HDC). Histamine is involved in a wide variety of pathological and physiological processes including allergic reactions, inflammation, immune responses, gastric secret
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Hh signaling pathway plays an
2021-12-15

Hh signaling pathway plays an essential role in the regulation of invertebrate and vertebrate tissue development and metabolic homeostasis. Components of Hh signaling pathway have been identified in succession, including Hh ligands, membrane protein receptors, cytoplasmic components and transcriptio
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