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One effective approach to fine tuning
2022-06-05

One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic Methotrexate scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as well as A
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br FAAH regulation of ECB signaling ECBs are
2022-06-02

FAAH regulation of ECB signaling ECBs are fatty AGK 2 synthesis amides and monoacylglyerols functioning as neuromodulator lipids that exhibit rapid (within seconds) on-demand biosynthesis in response to neuronal activation, and are subsequently degraded by specialized catabolic enzymes. There ar
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br Expression and Purification of LSD Proteins br
2022-06-02

Expression and Purification of LSD1 Proteins In Vitro Enzymatic Assays Analysis of LSD1 Demethylase Activity Acknowledgments Conflict of Interest Statement: Y.S. is a cofounder of Constellation Pharmaceuticals, Inc. and is a member of its scientific advisory board. Y.S. is also a consu
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Consideration must be given to both the tissues themselves
2022-06-02

Consideration must be given to both the tissues themselves and to infiltrating immune cells. As highlighted by Maxwell and Eckardt [88], clinical trials of compounds targeting these pathways will require large numbers of participants and prolonged follow-up to identify rare and late complications or
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Thermal analysis of the NQ peptide
2022-06-02

Thermal analysis of the NQ21 peptide was performed with the Solar CM2203 spectrofluorometer. We prepared three 1 μg/mL peptide solutions with different Methylprednisolone levels (5.0, 7.4, 8.5) in 0.01 M phosphate buffers. Each solution was slowly heated up from 28 °C to 54 °C with a step of 1 °C.
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The mD plasmid containing CD domain gene under the control
2022-06-02

The mD1.2 plasmid containing CD4 domain 1 gene under the control of a promoter was obtained as a gift from Dr. Dimiter S. Dimitrov. The mD1.2 plasmid was digested using restriction endonuclease I (New England BioLabs, USA) to release the mD1.2 gene. The gene encoding the mD1.2 protein was elongated
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One of the possible disadvantages of
2022-06-02

One of the possible disadvantages of this methodology is a possible cytotoxic effect resulting from either adenoviral vector injection or to Cre recombinase expression. Adenovirus has previously been used to efficiently mediate transgene expression in mouse MK-4827 hydrochloride (Thomas et al., 2000
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Also considered very rare is
2022-06-01

Also considered very rare is progressive encephalomyelitis with rigidity and myoclonus (PERM); sometimes called Stiff Person Syndrome Plus (SPS Plus) and with antibodies to glutamic kh7 decarboxylase (GAD). However, PERM is now increasingly found with glycine receptor antibodies (GlyR-Ab), in adult
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There are also data showing potential beneficial effects of
2022-06-01

There are also data showing potential beneficial effects of SGLT2i on non-alcoholic fatty liver disease (NAFLD) [[14], [15], [16], [17]], a hepatic manifestation of the metabolic syndrome that has been linked to type 2 diabetes mellitus (T2DM) development and increased cardiovascular (CV) as well as
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equol Similarly Somavarapu and Kepp constructed a PS homolog
2022-06-01

Similarly, Somavarapu and Kepp [29] constructed a PS1 homology model using 4HYG as a template, plus modeling the TM6-TM7 intracellular segment (amino acids 273 to 374). In this study, the authors considered for the first time the mature and immature (not autoproteolyzed) forms of PS1 component, sinc
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br Results br Discussion Immune mediated chronic
2022-06-01

Results Discussion Immune-mediated chronic inflammatory diseases (e.g. rheumatoid arthritis, psoriasis, multiple sclerosis, and inflammatory bowel disease) are characterized by a dysregulated migration of leukocytes from blood vessels into inflamed tissues. To date, several new targets and inh
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Type II diabetes is characterized by an inability to maintai
2022-06-01

Type II diabetes is characterized by an inability to maintain glucose homeostasis due to insulin desensitization and/or insufficient insulin secretion. GPR40, also known as free fatty pyruvate dehydrogenase kinase receptor 1 (FFAR1), is a member of the G-protein-coupled lipid-activated family of re
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In human cancers it has been identified that FOXC AS
2022-06-01

In human cancers, it has been identified that FOXC2-AS1 functions as an oncogenic RNA. For instance, in osteosarcoma, FOXC2-AS1 regulates the expression of FOXC2 at the transcription and post-transcription levels to promote doxorubicin resistance by facilitating ABCB1 expression (C.L. Zhang et al.,
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The ETB receptor has been
2022-06-01

The ETB receptor has been shown to decrease sodium transport in the renal medullary collecting duct and medullary thick ascending limb of Henle10, 11, 12, 13, 18. However, both inhibitory and stimulatory effects of endothelin have been reported in the proximal tubule16, 47, 48, 49. In the rat, endot
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The finding that a peptide consisting
2022-06-01

The finding that a peptide consisting of d-amino acids binds to LSD1-CoREST1 with equal affinity as the l-amino cudc ligand indicates that the assays detect a generally non-specific association between two highly charged molecules. Nonetheless, p53-CTD is an effective inhibitor of LSD1 and its bind
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