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In mice the Tfm mutation
2024-11-11

In mice, the Tfm mutation increased the anxiety-state assessed in the novel object and in light/dark box tests, whereas no changes were detected in the open field or elevated plus maze tasks (Zuloaga et al., 2008). As for Tfm rats, this seemed to be related to an increased HPA response to stress. Th
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br Acknowledgements br Introduction Microbial enzymes have g
2024-11-11

Acknowledgements Introduction Microbial enzymes have gained interest for their widespread uses in industries and medicine owing to their stability, catalytic activity, and ease of production and optimization than plant and animal enzymes (Singh et al., 2016). Microbial aminopeptidases (amino-a
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AKT activity is also self limiting
2024-11-11

AKT activity is also self-limiting through its substrate GSK3β; the kinase activity of which is negatively regulated by AKT phosphorylation (Fig. 3; Li, Liu, & Gao, 2009). GSK3β activation results in phosphorylation and subsequent ubiquitin mediated degradation of PHLPP (Li et al., 2009). AKT activa
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br Experimental procedure br Introduction Migraine is
2024-11-09

Experimental procedure Introduction Migraine is a debilitating neurovascular disorder characterized by recurring unilateral pulsating headaches of moderate to severe intensity, associated with nausea, photophobia and/or phonophobia, lasting from 4 to 72 h (Headache Classification Committee of
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Synthesis pharmacological evaluation for the binding at hA h
2024-11-09

Synthesis, pharmacological evaluation for the binding at hA, hA and hA ARs, and efficacy at hA subtype of the synthesized compounds, together with the assessment of their theoretical ADME properties were the guidelines in this preliminary drug discovery investigation. The synthetic pathways which y
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map3k8 br Introduction Adenosine deaminase ADA also known
2024-11-09

Introduction Adenosine deaminase (ADA), also known as adenosine aminohydrolase, is a key enzyme involved in the purine metabolism that converts adenosine to inosine irreversibly (Lupidi et al., 1997). It is a zinc containing metalloenzyme present in both prokaryotes and eukaryotes. In humans ADA
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A key step in the ADAR reaction is the formation
2024-11-09

A key step in the ADAR reaction is the formation of the adenosine covalent hydrate with a tetrahedral center at C6. The nucleoside analog 8-azanebularine (box in Fig. 6), with its relatively high propensity to form a covalent hydrate, is useful as an adenosine replacement in ADAR2 substrates to trap
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The role of DHT in
2024-11-09

The role of DHT in early teleost embryogenesis is not entirely clear or established, however additional studies that treat fish embryos to DHT or to specific srd5a inhibitors at critical stages of development (i.e. prior to sex differentiation) will shed light on the early functions of this androgen
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br Funding This work was supported by
2024-11-09

Funding This work was supported by Arena Pharmaceuticals, Inc, San Diego, CA, USA. Introduction 5-hydroxytryptamine 1B (5-HT1B) receptors are widely distributed in the central nervous system (CNS); they have various modulatory functions in drug reinforcement, appetitive behaviors, stress, moo
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A rational approach for the design of new
2024-11-09

A rational approach for the design of new steroid compounds as possible competitive inhibitors of CYP17 include chemical modification at C17 of the enzyme's natural substrates, pregnenolone (1) and progesterone (2), introducing groups with moderate to strong dipole properties at C20, such as oxime a
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br Disclosure br Acknowledgement br Introduction CYP A is
2024-11-09

Disclosure Acknowledgement Introduction CYP17A1 is a multifunctional enzyme with both 17α-hydroxylase and 17,20-lyase activities and is essential for the biosynthesis of steroidal gen antibiotic in male testes and adrenal glands. The 17α-hydroxylase activity of CYP17A1 is involved in the co
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Jesus et al discovered a new series of azaindole as
2024-11-09

Jesus et al. discovered a new series of azaindole as Aurora inhibitors through various modification of GSK1070916 (47). They synthesized series from modification of the GSK1070916 and evaluated for in-vitro Aurora-B/INCENP and Aurora-A/TPX2 inhibition assays. Modified PI3K Akt mTOR Compound Library
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In this study significant reduction in the
2024-11-09

In this study, significant reduction in the HCO3− content in sham-operated and testosterone-treated rats following bafilomycin A1 administration suggested that V-ATPase could be involved in mediating the decrease in vas deferens fluid HCO3− content, most probably due to the increase in H+ secretion
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It is well known that
2024-11-09

It is well-known that neurosteroids such as testosterone and their metabolites endogenously modulate neural excitability in animals and humans. Testosterone has protective effects against seizures induced by KA and PTZ (Frye et al., 2001b; Reddy, 2004b). Estrogens, on the other hand, have proconvuls
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Patients with cardiovascular disorders typically have lower
2024-11-09

Patients with cardiovascular disorders typically have lower plasma apelin levels than matched healthy controls. For example, plasma apelin levels are reduced in patients with coronary artery disease (CAD), and among CAD patients with unstable angina or acute myocardial infraction there is a further
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