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The physiological role of lactate induced antilipolytic effe
2022-02-08
The physiological role of lactate-induced antilipolytic effects is less clear. It has been speculated that GPR81 mediates the inhibition of lipolysis during intensive exercise, a condition which results in high systemic lactate plasma concentrations 9, 10. Owing to oxygen shortage resulting from int
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In parallel we were also preparing and evaluating other
2022-02-07
In parallel, we were also preparing and evaluating other piperidine bioisosteres and modifications to – to further access additional novel intellectual property (IP) space. Modeling work suggested that 4-position homologated piperidines, as well as 3-position homologated azetidines overlapped favora
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Solid tumors usually present insufficient supply of oxygen a
2022-02-07
Solid tumors usually present insufficient supply of oxygen, activating the hypoxia inducible factor-1 (HIF-1) pathway, which prompts an adaptive response on genes that regulate glycolytic metabolism, promoting glucose uptake through the transcription of GLUTs [54]. Increasing evidence indicates that
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Type diabetes mellitus is characterised
2022-02-07
Type 2 diabetes mellitus is characterised by two major features: peripheral insulin resistance and impaired insulin secretion from pancreatic beta sgk inhibitor [1]. The condition occurs when the pancreatic beta cells are unable to compensate for increased insulin demand due to insulin resistance i
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The in vivo biological activity
2022-02-07
The in vivo biological activity of the four novel analogues was then systematically assessed in three animal models including normal control, high fat fed and ob/ob mice. As expected from earlier in vitro studies, all four glucagon receptor antagonists had minor effects on glucose or insulin concent
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T0070907 australia All of the abovementioned effects
2022-02-07
All of the abovementioned effects of PUFAs signal their involvement in a cellular phenotype switching phenomenon, which is increasingly recognized as a potential target for future pharmacotherapies of atherosclerosis, especially for individuals who do not respond to the classical lipid-lowering stra
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Finally the optimized leads and
2022-02-05
Finally, the optimized leads (−)- and (−)- were tested in rat model of CIPN (3 and 30 mg/kg, po, qd, administered for 7 days) and the results have been shown in . Under acute set up, after single oral administration at 30 mg/kg, both the compounds exerted significant improvement of the NP condition
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br Acknowledgement This research was supported by Basic Scie
2022-02-05
Acknowledgement This research was supported by Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Education, Science and Technology (NRF-2016R1A2B4012818). Oral GSK2578215A sale is the most popular administration route due to good patien
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br Acknowledgments br Introduction Lung cancer is a
2022-02-05
Acknowledgments Introduction Lung cancer is a common but extremely perilous cancer, with approximately 733,000 new incidences reported annually in China [1]. Lung cancer ranks highest in the causes of tumor-related mortality, accounting for approximately one quarter of all cancer deaths [2]. N
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Most hexokinases are widely expressed but distinct
2022-02-05
Most hexokinases are widely expressed but distinct hexokinases predominate specific tissues (Katzen and Schimke, 1965, Rogers et al., 1975). Hexokinase I is found in all mammalian tissues, but is most abundant in the DAMGO australia and kidney (griffin et al., 1992). Hexokinase II is the primary he
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Interestingly myorelaxation and the stimulation
2022-02-05
Interestingly, myorelaxation and the stimulation of cGMP production are properties also reported for sGC stimulators, such as YC-1 and BAY 41–2272 (i.e., indazole compounds that were discovered in the 1990s) [35]. They relax aortic ring contractions induced by phenylephrine, and their effects are s
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br Mechanism of action of herbs and their
2022-02-05
Mechanism of action of herbs and their active constituents used in hair loss treatment The hair growth cycle consists of 4 stages known as the anagen (active growth phase; takes 2–7years), catagen (involuting or regressing phase; takes approx. 2weeks), telogen (short resting phase; takes approx.
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In summary we have designed and optimized a new series
2022-02-04
In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstr
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One difficulty in studying gp is that it binds
2022-02-04
One difficulty in studying gp120 is that it binds to more than one receptor. Understanding how AM251 respond to gp120 is complex because of this promiscuity. In an attempt to establish the contribution of CXCR4 in the antagonistic effect of gp120 on morphine-induced antinociception, AMD3100 was adm
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Because sleep and metabolism are
2022-02-04
Because sleep and metabolism are intimately linked, the authors next move to study whether Eaat2 also controls metabolic rate. First, we must ask how sleep and metabolism are connected at a functional level. The Ro 48-8071 allocation hypothesis of sleep posits that organisms temporally partition sp
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