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GnRH ant have been designed to obtain pharmacological compou
2022-01-17
GnRH-ant have been designed to obtain pharmacological compounds to block the pituitary–gonadal axis without the undesirable flare effect exerted by GnRH itself or by the GnRH-a (see Section 2.2). GnRH-ant competitively block the binding of GnRH to GnRHRs (Schally, 1999; Tan & Bukulmez, 2011); they p
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Generally replacement of the aryl group
2022-01-17
Generally, replacement of the aryl group was well tolerated, with tetrahydropyran () and hydroxyl () functionality providing potency equivalent to and . These substitutions had no effect on selectivity versus GlyT2 and taurine transporter (TauT)—no activity was observed at micromolar concentrations
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We noticed that the spontaneous openings
2022-01-17
We noticed that the spontaneous openings of the D97R α1 GlyR appeared to be quite similar to those elicited by a maximally-effective glycine concentration on wildtype GlyR; both generated similar open and shut dwell-time histograms, both exhibited openings grouped into clusters with Popen values gre
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br NMDA receptor LBDs The study of GluA was
2022-01-17
NMDA receptor LBDs The study of GluA2 was later expanded to include NMDA receptors [22]. NMDA receptors are obligate heterotetramers that are composed of two glutamate-binding subunits and two glycine-, or d-serine-, binding subunits. In this study, crystal structures of the NMDA receptor glycine
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br Declaration of interest br Acknowledgments br This
2022-01-17
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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Emodin br Experimental methods br Acknowledgments We thank a
2022-01-17
Experimental methods Acknowledgments We thank all members of the Hermanson lab, especially Ana Teixeira, Shirin Ilkhanizadeh and Karolina Wallenborg, for assistance and discussions, Peter Löw for anti-synaptotagmin antibody, and Lars Björklund, Ole Isacson, Christer Höög, Claes Wahlestedt and
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Previous research has suggested that differences
2022-01-17
Previous research has suggested that differences in spatiotemporal regulation of intracellular signaling pathways can confer specificity to cellular responses (Marshall, 1995). Conventional approaches based on gain- or loss-of-function genetic manipulations or small-molecule inhibitors, however, lac
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In terms of cytotoxicity studies under
2022-01-17
In terms of cytotoxicity studies under two-dimensional cell culture conditions, only two of the above-mentioned publications with liposomal formulations of tyrosine kinase inhibitors reported viability data as compared to respective free drugs. On the one hand, liposomal gefitinib exerted strongly r
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Another TKI used in cancer
2022-01-17
Another TKI used in cancer therapy is the Abl inhibitor imatinib mesilate which has also a beneficial effect on glucose homeostasis in diabetic humans [39], [40], [41]. Imatinib has a clear impact on NFκB activation and anti-apoptotic preconditioning of β-cells [39], attenuating islet inflammation [
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br Conclusion br Acknowledgements This work was supported by
2022-01-17
Conclusion Acknowledgements This work was supported by R01 HL127386 (Niklason) and 1R01 HL128406-01A1 (Dardik), and by an unrestricted research gift from Humacyte Inc. KLL was supported by F30HL143880. KLL and EQ were supported by T32 GM007205. LEN is a founder and shareholder in Humacyte, Inc
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In conclusion we have shown that the
2022-01-15
In conclusion, we have shown that the brain penetrating ability of heteroaryl piperazine and piperadine ureas can be modulated through small structural changes to the heteroarenes, the piperazine or piperidine core, and the biaryl ether tail. Compounds exhibiting / ratios ranging as high as 4.2:1 to
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Myelination by oligodendrocytes is required for
2022-01-15
Myelination by oligodendrocytes is required for saltatory nerve impulse conduction and proper CNS function (Bercury and Macklin, 2015). Defects in myelination and remyelination impair saltatory nerve conduction and functional connectivity leading to cognitive, behavioral, and motor deficits in neuro
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br Cellular directionality To obtain
2022-01-15
Cellular directionality To obtain a comprehensive understanding of cell migration, it is essential to understand how cues from the cell’s external environment are relayed to the Moxidectin cytoskeleton, so the cell can migrate towards the cue; a process herein referred to as cellular directional
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br Rho protein networks in malignancy It has long been
2022-01-15
Rho protein networks in malignancy It has long been recognized that Rho activity and expression are frequently elevated in tumors (Fritz et al., 1999, Orgaz et al., 2014). In this chapter we will introduce the most prominent Rho proteins, their regulators and effectors and provide an overview of
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A general synthetic pathway to these
2022-01-15
A general synthetic pathway to these tricyclic structures is described in (detailed procedures can be accessed in the patent application WO 2011/014520 A2). Benzylation of the appropriate ketoester using KHMDS, followed by treatment with DMF-dimethyl acetal yielded the racemic (dimethylamino)-methyl
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