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br Funding sources This work was supported
2021-11-12

Funding sources This work was supported, in part, by NIH GM115388 to BGM. Acknowledgements Introduction Glucokinase (GCK) plays a central role in the regulation of glucose metabolism. Its activity is restricted to ana 2 with important roles in whole-body glucose homeostasis [1]. In pancre
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Despite the potential promise of
2021-11-12

Despite the potential promise of both of these peptides, such compounds are still susceptible to efficient renal filtration (Emmanouel et al., 1978, Holst, 1991, Deacon et al., 1996). However, numerous studies have demonstrated that fatty mcc950 synthesis dervatisation of related regulatory peptides
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br Acknowledgments br Introduction Postmenopausal
2021-11-12

Acknowledgments Introduction Postmenopausal osteoporosis, which is primarily caused by PLX3397 deficiency, has been a worldwide health problem and threatens postmenopausal women of all races. An estimated 80% of osteoporosis patients in the United States are women, and approximately 30% of po
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Cys loop GABA receptors are well studied targets
2021-11-12

Cys-loop GABA receptors are well-studied targets for insecticides and also play an important role in nematode biology. These receptors are also targets for the anthelmintic piperizine (Accardi et al., 2012). The nematode GABA receptor most studied is the UNC-49 receptor which plays a role in muscle
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br Author contributions br Conflict of
2021-11-12

Author contributions Conflict of interests Acknowledgements This work was supported by NIH grant DK098730 to NHM. Free fatty acids play important roles in biological processes contributing to both health and disease. As essential nutritional components, free fatty acids are utilized as b
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Akt mTOR signaling pathway is
2021-11-12

Akt/mTOR signaling pathway is a major negative regulator of autophagy, via modulating ULK1 complex. It is well established that Inhibition of mTOR by deprivation of nutrients or growth factors, led to dephosphorylation of ULK1, ULK2, and Atg13 in human cells, which is a key step for ULK1 complex ass
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The pharmacokinetic properties of were amenable
2021-11-12

The pharmacokinetic properties of 12 were amenable to oral dosing allowing in vivo comparison to 6. Compared to a maximum efficacious dose of 6 (60mg/kg), 12 demonstrated improved glycemic control during OGTT in high-fat fed/STZ treated (HF/STZ) and BDF/diet-induced obesity (DIO) mouse models of typ
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In the Medicines for Malaria Venture MMV distributed the
2021-11-12

In 2011 the Medicines for Malaria Venture (MMV) distributed the Open-Access Malaria Box to accelerate antimalarial drug discovery (Spangenberg et al., 2013). The Malaria Box consists of 400 structurally diverse compounds, curated from >20,000 hits generated from large-scale screens, that inhibit the
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Factor Xa FXa has emerged as
2021-11-12

Factor Xa (FXa) has emerged as a particularly promising target for the development of effective anticoagulant drugs because FXa acts at the convergence point of the extrinsic and intrinsic coagulation pathways. It efficiently catalyzes the conversion of prothrombin to thrombin with one molecule of F
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br Concluding remarks Several orphan GPCRs have expression p
2021-11-11

Concluding remarks Several orphan GPCRs have expression profiles that indicate they are worthy of consideration as therapeutic targets. This view can be supported via various transgenic techniques, and it would be interesting to have wide-ranging phenotypic information on GPR35 knockout mice. Bas
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The mechanisms by which NEIL and
2021-11-11

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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In respect of clinical development
2021-11-11

In respect of clinical development Takeda has pioneered the field with the GPR40 agonist TAK-875 or fasiglifam (Figure 2A), which in phase-II studies decreased HbA1c as efficiently as sulfonylurea without signs of hypoglycemia [24]. This was obtained with surprisingly little effect on systemic insul
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br Funding sources This work
2021-11-11

Funding sources This work was supported, in part, by NIH GM115388 to BGM. Acknowledgements Introduction Glucokinase (GCK) plays a central role in the regulation of glucose metabolism. Its activity is restricted to PKM2 inhibitor mg with important roles in whole-body glucose homeostasis [1
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Statins are recognized by their nephroprotective effect Chmi
2021-11-11

Statins are recognized by their nephroprotective effect (Chmielewski et al., 2002). The hepato- and nephroprotective effects of silymarin are also well studied (Alqasoumi, 2014, Mohamed et al., 2018). Several studies documented increasing Exendin-3 (9-39) amide sale of FXR by statins (Byun et al.,
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It is noted that knee swelling was milder and
2021-11-11

It is noted that knee swelling was milder and the intensity of IL-4 staining (MFI) in the vehicle-treated group was lower in the second (Fig. 7a and d) than the first (Figs. 1a and 3f) AIA experiment. The variation in joint swelling between the two studies is most likely due to the models being perf
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