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br Materials and methods br Results br Discussion br Acknowl
2022-09-07
Materials and methods Results Discussion Acknowledgments Introduction As we move into an aging society, there has been a growing interest in neurological disorders [1]. Neurodegenerative diseases such as Parkinson’s disease (PD) and Alzheimer’s disease (AD) cause cognitive malfunctio
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In the course of our synthetic
2022-09-07
In the course of our synthetic studies, we also discovered an unprecedented application of Burgess reagent. Instead of generating an olefin by an intramolecular syn-elimination, the product resulting from the treatment of spirocyclic alcohols 11 and 12 with Burgess reagent led to the expansion of th
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br Conflict of interest statement br Acknowledgements br Int
2022-09-07
Conflict of interest statement Acknowledgements Introduction Galanin is a multi-functional neuropeptide that is widely distributed in the neuroendocrine system and peripheral tissues of various species. This 29-amino-acid peptide (30 in humans) is proteolytically processed from its precurso
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br Results and discussion The synthesis
2022-09-07
Results and discussion The synthesis of core aldehyde building block 2 commenced with known aldehyde 5. The Horner–Wadsworth-Emmons olefination of the latter (using commercially available 6) gave cinnamate ester 7. Facile hydrogenation of the double bond in 7 was achieved over Raney nickel withou
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We tested formyl MYVKWPWYVWL which we had previously shown
2022-09-07
We tested formyl-MYVKWPWYVWL, which we had previously shown to have essentially identical Kis for W190/N192, R190/K192 and R190/N190 [8] of 130 nM, for its ability to downregulate surface receptor (Fig. 5A). R190/K192 exhibited the lowest EC50 of 44±4 nM about 3 fold below the observed Ki and a maxi
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Distribution of histamine receptors in the intestines varies
2022-09-07
Distribution of histamine receptors in the intestines varies among species, but our findings are similar to those previously reported in humans and guinea pigs (Thurmond, 2010, Thurmond, 2015). H1 receptors were located mainly in the gastric mucosa, smooth muscle, and lymphoid tissue, corresponding
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YAP TAZ nuclear function is also influenced by
2022-09-07
YAP/TAZ nuclear function is also influenced by interaction with the TEAD family of transcription factors [96, 97, 98, 99, 100, 101]. The RAC1 Cy3 hydrazide exchange factor protein TIAM1 has recently been linked to YAP/TAZ regulation in the nucleus and cytoplasm. Nuclear TIAM1 inhibits YAP/TAZ bindin
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Lactate LA the end product of aerobic glycolysis has been
2022-09-06
Lactate (LA), the end product of aerobic glycolysis, has been long neglected and seen as a byproduct until recently the findings for its important role in global gene transcription, cancer progression, functional polarisation of immune TMN 355 and the sustenance of stem cells [[7], [8], [9]]. Lacta
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IC is a rat mAb specifically binding
2022-09-06
IC2 is a rat mAb specifically binding to insulin granula [127,128]. Although this mAb was discovered 30 years ago, it has only recently been used for β-cell imaging in vivo. Moore et al. used this mAb for β-cell imaging in 2001 [129]. After DTPA conjugation, IC2 was labeled with 111In. Both in vitro
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To apply the recently developed GPR ligands to CNS disorders
2022-09-06
To apply the recently developed GPR35 ligands to CNS disorders, it is necessary to understand whether GPR35 is expressed by any identified cell types in the GSK2578215A and whether activation or blockade of this receptor has any consequence on the activity of the neuronal circuitry. To this end, th
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For some agonists these stable GPR responses were resistant
2022-09-06
For some agonists, these stable GPR119 responses were resistant to washing. Thus, sustained activation could continue, for at least a number of hours, even after removal of free agonist. These data are consistent with reports for other GPCR systems that do not desensitize (Calebiro et al., 2009, Fer
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In addition to gonadotropes GnRHRs have
2022-09-05
In addition to gonadotropes, GnRHRs have also been detected on somatotropes, lactotropes, thyrotropes, melanotropes, somatolactin (SL) cells, and/or corticotropes using immunohistochemical, radioligand-binding, or mRNA expression approaches across species; including fishes, rats, and humans (La Rosa
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NEIL interacts with many DNA replication proteins including
2022-09-03
NEIL1 interacts with many DNA replication proteins including flap-endonuclease 1 (FEN-1), proliferating cell nuclear antigen (PCNA), and Werner RecQ helicase (WRN) through its disordered C-terminal part. One study showed that in in vitro condition, NEIL1 binds to the damaged epz in an RPA-coated si
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Taking into account abovementioned vitamin D deficiency
2022-09-03
Taking into account abovementioned, vitamin D3 deficiency effects on synaptic neurotransmission can be considered as targeting both Ca2+-independent and Ca2+-dependent processes. Ca2+-independent action of vitamin D3 deficiency is associated with a decrease in the expression of glutamate and GABA tr
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br Introduction Opioids have long been used in pain manageme
2022-09-03
Introduction Opioids have long been used in pain management [1]. However, their non-medical use has grown rapidly in the last few years. Hydrocodone (HYD) is one of the most widely used short-acting opioids; with over 136.7 million prescriptions in 2011 [2]. HYD is a semi-synthetic opioid used fo
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