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With an ever increasing incidence rate of type diabetes
2022-08-17
With an ever-increasing incidence rate of type 2 diabetes and obesity, it is imperative to develop new therapeutic regimes that may provide a benefit both in terms of efficacy and tolerability. The existing portfolio of drugs for the treatment of metabolic disorders, primarily type 2 diabetes and ob
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The mechanisms by which NEIL and NEIL excise bulky
2022-08-17
The mechanisms by which NEIL1 and NEIL3 excise bulky adducts and unhook ICLs are unclear. Structures of NEIL1 are available only in complex with DNA containing small lesions 79., 80., 81., and the single available structure of NEIL3 lacks DNA (Figure 5D,E) [73]. Nonetheless, comparison of the two st
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br Conclusion br Conflict of interest statement br
2022-08-17
Conclusion Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as Introduction Over the past decade, more than a hundred new biopharmaceutical products have been approved and market
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br Author s contributions br Conflict of interest
2022-08-17
Author's contributions Conflict of interest Acknowledgements This work was supported in part by a grant from Department of Biotechnology (DBT), Government of India (Sanction Order No.: BT/563/NE/U-Excel/2016). MC, PDG and SKM acknowledge the Ministry of Human Resource and Development (MHRD)
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atm kinase inhibitor The general synthetic routes leading to
2022-08-17
The general synthetic routes, leading to aspartate and 2,3-diaminopropionate analogs, are shown in . As outlined in , aspartic atm kinase inhibitor analogs – were synthesized through standard carbodiimide-mediated coupling between an amine and an appropriately protected aspartic acid. It is worth m
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Further explorations at the ortho and meta positions of
2022-08-17
Further explorations at the ortho- and meta-positions of the phenyl in the tail proceeded on the basis of the preliminary results. First, we investigated the fluorine group at the meta- (13p) and ortho-positions (13q) of the phenyl group, with both compounds being slightly less potent than 13o. Surp
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In spite of the similarities of caffeine
2022-08-17
In spite of the similarities of caffeine's effects in L929 cells and erythrocytes, a major difference can be identified in the magnitude of inhibition (35% versus 90%). It initially seems reasonable to conclude from this finding that the reduced magnitude of caffeine inhibition in L929 cells is simp
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br The concept of the axo myelin synapse Axons can
2022-08-17
The concept of the axo-myelin ‘synapse’ Axons can release glutamate in a Ca+-dependent and independent manner (reviewed in [13,69]). Glutamate released from axons activates GluRs located in myelin, a feature that gave rise to the idea of the axo-myelin ‘synapse’ by analogy with classical synaptic
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br Acknowledgments This work was supported by a grant CIHR
2022-08-17
Acknowledgments This work was supported by a grant CIHR-NSFC China-Canada Joint Health Research from the National Science Foundation of China (Grant Number 81061120525) and the Canadian Institutes for Health Research (Grant number CCI-109605). The authors thank two anonymous reviewers for helpful
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Ketamine has recently been found
2022-08-17
Ketamine has recently been found to exert rapid and sustained antidepressant effect. Single dose ketamine can have an efficacy of up to 1 week [20]. Furthermore, ketamine is an effective drug against refractory depression [21,22]. The antidepressant mechanism of ketamine is still unclear. Whether CO
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Importantly bioelectric circuits in tissues Fig
2022-08-16
(4) Importantly, bioelectric circuits in tissues (Fig. 2A) have a capacity to store long-term patterning information. An example is planarian anterior-posterior patterning: during regeneration, each fragment cut from a worm needs to build a head and tail at their correct ends. This process is regula
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Tranilast Sodium Clinical data showed TAK was rapidly absorb
2022-08-16
Clinical data showed TAK-875 was rapidly absorbed with a half-life of 28-30h and clearance primarily through glucouronidation in the liver with minimal urinary clearance [30]. TAK-875 made the glycosylated hemoglobin (HbA1c) levels fall significantly from baseline after 24-week administration in onc
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L-α-Aminoadipic Acid br Conclusions and perspectives In
2022-08-16
Conclusions and perspectives In conclusion, offering duly validated and highly performing assays for measuring DiXaIs in plasma is a step, but not the final issue. More dedicated and individual assays will continue this innovative development, which witnesses the need for collaboration between co
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Evidence suggests that phosphorylation increases synaptotagm
2022-08-16
Evidence suggests that phosphorylation increases synaptotagmin affinity for the SNARE complex [15], [128]. It is, however, unclear how this might affect release. Synaptotagmin has been identified as part of the minimal vesicle docking machinery in chromaffin nisoldipine [129]. Thus, phosphorylation
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The histamine H receptor H R amino acids
2022-08-16
The histamine H3 receptor (H3R; 326–445 amino-acids) is located on histaminergic neuron somata, dendrites and axon varicosities, as well as on the axon varicosities and somata of other neurons, providing negative feedback to inhibit histamine synthesis and the release of histamine or other transmitt
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