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br Conflict of Interest Both GM and
2021-12-14
Conflict of Interest Both GM and BDH are shareholders in Caldan Therapeutics, a company exploring potential novel treatments for type 2 diabetes. Acknowledgments Work described herein was supported by Biotechnology and Biological Sciences Research Council [grant BB/K019864/1)] (to GM) and [gr
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In recent years several DPP IV inhibitors have
2021-12-14
In recent years, several DPP-IV inhibitors have already been approved, such as sitagliptin, vildagliptin, saxagliptin, tenegliptin, alogliptin and linagliptin, etc. Among them, linagliptin (1, Fig. 1) is a non-peptide mimetic Posaconazole with a unique xanthine scaffold developed through high-throu
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PPACK Dihydrochloride mg Introduction Substantial body of ev
2021-12-14
Introduction Substantial body of evidence supports the notion that GABA, the dominant inhibitory neurotransmitter in the hypothalamus of mammals, affects GnRH release by two classes of membrane receptors: GABAA (GABAAR) [1] and GABAB (GABAB R) [2]. Studies in rodents and sheep have documented that
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Based on the role of NMDA
2021-12-14
Based on the role of NMDA receptors in initiation and propagation of epileptic seizures and on potentiation of NMDA function by glycine, it has been hypothesized that glycine will have proconvulsant activity (Foster and Kemp, 1989). Indeed, there is some evidence that human epileptogenic foci, remov
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To maintain low Glu concentrations in the
2021-12-14
To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino rilpivirine is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of perisynaptic astrocytes, and
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In our study we observed elevation of
2021-12-14
In our study, we observed elevation of the fluorescent intensity in the layers without synaptic contacts (OS, ONL, INL, and GCL). In the enzyme-linked fluorescence assay system, released glutamate is catalyzed by the enzyme on the surface of a quartz glass. Therefore, the diffusion of glutamate onto
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To maintain low Glu concentrations in the synaptic cleft bel
2021-12-14
To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino geldanamycin is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of perisynaptic astrocytes, and
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Transient forebrain ischemia in rodents
2021-12-14
Transient forebrain ischemia in rodents induces a reduction in expression of mRNA encoding the AMPA receptor subunit GluR265, 66, 67, 68, 69 (Fig. 3). gluR2 mRNA expression is markedly reduced in the CA1 region (the saha inhibitor region most vulnerable to ischemia-induced damage), but not in the CA
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Fig demonstrates placental amino acid transporter protein co
2021-12-14
Fig. 7 demonstrates placental amino cathepsin inhibitors transporter protein concentrations. While no change in the placental SNAT2 is effected in response to a high-fat diet in wt, a trend toward a reduction was seen in glut3 mice in response to a high-fat vs. chow diet (Fig. 7A and B). A high-fat
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The widespread involvement of HH GLI in
2021-12-14
The widespread involvement of HH/GLI in human malignancies has initiated a remarkable effort to identify selective HPIs. As shown in Table 2.1, most of these small molecule inhibitors target the essential effector protein SMO, which should lead to pathway abrogation by eventually decreasing the GLIA
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br Rationale The present study
2021-12-14
Rationale The present study was motivated to get further insight into the molecular recognition processes of 2-alkyl(amino)ethyl-1,1-bisphosphonates taking compounds 12–14 as reference structures. We have recently demonstrated that TcFPPS inhibitors 12 and 13 bind to the allylic site of the enzym
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Adipocytes play diverse roles in energy homeostasis by contr
2021-12-13
Adipocytes play diverse roles in energy homeostasis by controlling energy consumption [8] and function as a source of proteins and cytokines, which mediate numerous physiological functions [9]. Excessive accumulation of adipocytes, as well as an increase in either their size or number, causes obesit
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As evidenced by SARs and
2021-12-13
As evidenced by SARs and crystallographic data, HO-1 has at least three main crucial regions for inhibitor binding. The most crucial area, the so-called eastern region, is able to allocate the azole ring that represents the first anchoring point by establishing a coordination binding to the heme fer
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The vessel wall protein collagen
2021-12-13
The vessel wall protein collagen, which becomes exposed to circulating platelets after vascular injuries, is a very strong platelet agonist. It stimulates all relevant platelet activation steps predominantly via the GPVI/FcRγ-chain receptor complex through an immunoreceptor tyrosine-based activation
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In vertebrates three cognate receptors or receptor like sequ
2021-12-13
In vertebrates, three cognate receptors or receptor-like sequences have been identified with distinct distributions and functions (Millar, 2005, Neill et al., 2001). Only two types of GnRHR occur in mammals, though (Morgan and Millar, 2004). The mammalian type I GnRHR shares over 80% amino Artemisin
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