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With the identification of small
2022-09-09
With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-methy
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While earlier reports on ferroptosis did not clarify
2022-09-09
While earlier reports on ferroptosis did not clarify mitochondrial damage and consequent death signaling in this paradigm of oxidative death, evidence from recent studies in neuronal systems strongly suggested a mechanistic link between enhanced lipid peroxide formation and loss of mitochondrial int
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It has been reported that the FDP
2022-09-09
It has been reported that the FDP synthase in Hevea latex has a major role to produce the starter substrate FPP for the prenyl chain elongation in natural rubber biosynthesis (Takaya et al., 2003). Accumulation of HbFDP mRNA transcripts in different tissue types including latex (natural rubber) prod
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Following the discovery of diketo compounds S
2022-09-08
Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent Z DEVD FMK based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase. Bio
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Management of HIV treatment with HIV PIs
2022-09-08
Management of HIV-1 treatment with HIV PIs can be complicated due to wide inter-patient variability in CA 074 levels. In certain scenarios, therapeutic drug monitoring (TDM) has been recommended as a useful approach to individualize therapy for HIV-infected patients [[9], [10], [11], [12]]. Several
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Histamine receptors were largely linked with allergic
2022-09-08
Histamine receptors were largely linked with allergic and inflammatory reactions before the recognition of the histamine H3R in 1983 that proved its function as auto- as well as heteroreceptor at pre- and postsynaptic membranes and demonstrated its intense regulating influence on release of numerous
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br Introduction Hexokinase HK is an enzyme that catalyses
2022-09-08
Introduction Hexokinase (HK) is an enzyme that catalyses the transfer of phosphate from ATP to glucose in the first step of glucose metabolism (Wilson, 1995, Wilson, 2003). In mammalian, HK has four important isozymes which are designated as HK1, HK2, HK3 and HK4 (Wilson, 1995, Wilson, 2003). HK1
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Finally worth of mention are few
2022-09-08
Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a Neuromedin B library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development of the first serie
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In the Hedgehog signaling pathway cholesterol
2022-09-08
In the Hedgehog signaling pathway, cholesterol is required to activate SMO (Cooper et al., 2003), the downstream target of PTCH1. A previous study (Bidet et al., 2011) reported that Patched expression in yeast XL-888 increased extrusion of a fluorescent boron dipyromethanene sterol derivative (BODI
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br GSK The GSK family is highly
2022-09-08
GSK-3 The GSK-3 family is highly conserved throughout evolution and is encoded by two genes, GSK-3α and GSK-3β, which are located in chromosomes 19q13.2 and 3q13.3 in human, respectively. Both GSK-3α and GSK-3β proteins exist in a variety of tissues with the highest levels found in Cystamine dihy
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Approximately mammalian genes encoding family A or rhodopsin
2022-09-08
Approximately 250 mammalian genes encoding family A (or rhodopsin-like) GPCRs have been cloned (Lee et al., 2001a). As yet, the total number of cloned GPCRs reported in the literature including the secretin and metabotropic glutamate-like families of GPCRs falls short of the projected 616 GPCR-encod
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The discovery that the physiological functions
2022-09-08
The discovery that the physiological functions of LPI are associated with the activation of specific GPR55 membrane receptor [4] has launched a new era of research on this lysophospholipid. However, the activation of membrane receptors by lysophospholipids is extremely complex due to the multitude o
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SBI-0206965 br Conflict of Interest Both
2022-09-08
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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Glycine regulates several brain functions and
2022-09-08
Glycine regulates several brain functions and glycine transporters significantly contribute in such processes. In previous work we reported calpain sensitive regions in N-terminal domains of GlyT1a and GlyT1b (Baliova and Jursky, 2005). Here we show that distal part of glycine transporter GlyT1C-ter
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br Dysregulation of glutamate transporter expression and fun
2022-09-07
Dysregulation of glutamate transporter expression and function Aberrant glutamate transporter function and expression are associated with various neurological disorders. Therefore, understanding the underlying mechanisms of EAAT1/2 expression may provide therapeutic targets for treating neurologi
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