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Generally replacement of the aryl
2022-05-30

Generally, replacement of the aryl group was well tolerated, with tetrahydropyran () and hydroxyl () functionality providing potency equivalent to and . These substitutions had no effect on selectivity versus GlyT2 and taurine transporter (TauT)—no activity was observed at micromolar concentrations
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Based on work from our labs with mGlu NAMs and
2022-05-30

Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]
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br Methods br Results and
2022-05-27

Methods Results and discussion Conclusions A third example of a hexokinase using polyphosphate exclusively as a phosphoryl donor has been identified, this time in mammalian tissues. This is the first polyphosphate utilizing enzyme activity demonstrated in mammalian SKF38393 HCl mg as far a
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br Some general considerations on anterior pituitary cell ty
2022-05-27

Some general considerations on anterior pituitary cell type, models, sex and drugs Historically, real-time analysis of native endocrine anterior pituitary cell excitability has been somewhat limited and thus much of the pioneering work on anterior pituitary cell excitability and stimulus-secretio
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Amongst oxidants that we have studied
2022-05-27

Amongst oxidants that we have studied, PMS is unique in having a greater effect in deoxygenated cells. The resulting phenotype shows some similarities with the increased cation permeability shown by deoxygenated sickle PX 866 [27]. It is interesting to consider why PMS has this effect. PMS functions
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Photoincorporation of pTFDBzox AP occurred predominantly in
2022-05-27

Photoincorporation of 21-pTFDBzox-AP occurred predominantly in the β3 subunit, very modestly in the α1 subunit and not at all in the γ2 subunit. These observations taken together with the sensitivity of 21-pTFDBzox-AP enhancement of GABA currents to the α1 M1 mutation Q242 W4 suggest that the 21-pTF
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Target regulated the formation of G
2022-05-27

Target-regulated the formation of G-quadruplex was used here to “kill two Histamine Phosphate with one stone” for the detection of melamine and I− with one probe DNA. G-quadruplexes are higher-order structures formed from G-rich oligonucleotides through the stacking of planar G-tetrads [43,44]. The
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Compound and several additional FPR antagonists identified
2022-05-27

Compound 10 and several additional FPR1 antagonists identified here specifically blocked fMLF-induced responses mediated via FPR1 in FPR1-HL60 Berberine Sulfate and human neutrophils, but not responses mediated via FPR2 or FPR3 (in human neutrophils and transfected HL60 cells) or Fpr1 (murine neutr
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Koumine br Conflicts of interest br Acknowledgment br Introd
2022-05-27

Conflicts of interest Acknowledgment Introduction The Koumine growth factor receptors (FGFRs) are a family members of receptor tyrosine kinase (RTK) that represent attractive therapeutic targets for anti-cancer therapy gaining more and more attention in recent years [1], [2]. This family me
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br Materials and methods br Results The immunoblot analysis
2022-05-27

Materials and methods Results The immunoblot analysis demonstrated the presence of similar immunoreactivity by liver FBPase in hepatic and renal extracts. These results indicate that FBPase is present in a similar amount in both tissues. Moreover, the analysis revealed that the antibody detect
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br PEPCK This enzyme decarboxylates
2022-05-27

PEPCK This enzyme decarboxylates and then phosphorylates oxaloacetate to form phosphoenolpyruvate (PEP) in the second step of gluconeogenesis after the carboxylation of pyruvate catalyzed by PC. PEPCK1 (PEPCK-C, encoded by the PCK1 gene) and PEPCK2 (PEPCK-M, encoded by the PCK2 gene) are two isof
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br Introduction Migraine is a
2022-05-27

Introduction Migraine is a chronic neurological disorder characterized by recurrent episodes of headache. It affects more than 10% of the population worldwide, resulting in a staggering amount of episodic disability, a substantial decrease in the quality of life and a concomitant loss in producti
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Neuropathic pain NP is a chronic
2022-05-27

Neuropathic pain (NP) is a chronic pain caused by lesion or disease affecting any part of the nervous system leading to clinical conditions ranging from painful neuropathy to poststroke central pain. Anticonvulsant drugs, Gabapentin and Pregabalin, acting on αδ subunit-containing voltage-dependent c
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br Conclusion The histamine H receptor has been the focus
2022-05-27

Conclusion The histamine H3 receptor has been the focus of a great deal of research over the past four decades and in this context, substantial progress has been made in developing H3R-related ligands. The involvement of H3Rs in many neurological disorders has been documented by several lines of
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br Materials and methods br Results
2022-05-27

Materials and methods Results Discussion It was previously shown that heterologous DNA vaccines composed of fused cDNA fragments encoding chimeric NH2-terminal human HER2 and COOH-terminal rat neu sequences stimulated stronger antibody responses and protective antitumor immunity than either
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