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We show that pharmacological inactivation
2022-02-15

We show that pharmacological inactivation of GSTP1 over a sustained period does not show any observable toxicity, and not only prevents breast tumor growth but even slows established breast tumor growth in mice. A highly potent GSTP1 inhibitor, ezatiostat (developed by Telik Inc.) has passed phase I
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br Introduction Depressive disorder is a syndrome characteri
2022-02-14

Introduction Depressive disorder is a syndrome characterized by a group of heterogeneous symptoms that affect more than 350 million people worldwide, 4% of world population (WHO, 2012). The WHO estimates depression will be the leading global cause of disability in 2020, with tremendous economic c
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While the S site has been implicated in binding
2022-02-14

While the S2 site has been implicated in binding, it rvx is unclear whether the S2 site plays a role in the substrate transport process. Crystal structures have revealed that different drugs and detergents can bind to the S2 site of SERT [8] and LeuT [[13], [14], [15]]. However, there are no crysta
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br Introduction Atherothrombosis is associated with the pres
2022-02-14

Introduction Atherothrombosis is associated with the presence of a low-grade, subclinical smoldering inflammatory response [1]. Several inflammatory markers, among them high-sensitive C-reactive protein (hs-CRP) [2], the erythrocyte sedimentation rate (ESR) [3], fibrinogen concentrations [4], int
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Due to the versatility of the ghrelin
2022-02-14

Due to the versatility of the ghrelin system and its multiple functions, dysregulation in some of the components of the ghrelin system, such as ghrelin, GOAT, and GHSR, might lead to pathogenesis of many endocrine-related diseases, including obesity, short stature, cancer, inflammatory, and cardiova
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Herein we describe the development of second generation GSM
2022-02-14

Herein, we describe the development of second generation GSM compounds aimed at improving critical physicochemical properties while maintaining the potent activity of the parent AGSM. Ligand design focused on identifying heterocyclic replacements for the hydrophobic D-ring as a means to improve ADME
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br Conclusion In the present
2022-02-14

Conclusion In the present study, we found that the majority of commercially available antibodies and antibody-based tools against galanin and its receptors that we tested do not meet validation requirements. Therefore, critical validation of these tools by the user is essential before being used
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Among sensitizers tested in the
2022-02-14

Among 22 sensitizers tested in the previous study, six test chemicals were pre- or pro-haptens (Nepal et al., 2018a). Among 6 chemicals, hydroquinone and 2-aminophenol, strong sensitizers, were falsely classified as non-sensitizers due to the lack of metabolic activation (Nepal et al., 2018a). Liter
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In recent years it was discovered in animals
2022-02-14

In recent years, it was discovered in animals that certain types of non-apoptotic cell death are strictly dependent on iron and ROS. The term ‘ferroptosis’, derived from the Greek word ‘ptosis’ (falling) and the Latin word ‘ferrum’ (iron), is coined to describe such cell death phenomena. Cytoplasmic
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br Rationale The present study was motivated
2022-02-14

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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Glutathione transferases EC also referred to as
2022-02-12

Glutathione transferases (EC 2.5.1.18; also referred to as glutathione S-transferases, GSTs) are ubiquitous and promiscuous enzymes that catalyze various kinds of reactions involving a wide variety of substrates that are toxic and chemically reactive (Angelucci et al., 2005). The primary function of
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The present study chose the fdh gene the homolog
2022-02-12

The present study chose the fdh gene, the homolog of mammalian GSNOR, to generate UAS-fdh and fdh double-stranded RNA interference (ds-RNAi) transgenic Drosophila. These transgenic models were used to study the effect of GSNOR activity modulation on visual learning and memory and to explore the poss
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We also noticed that acetic
2022-02-12

We also noticed that acetic acid by itself (used to induce pain) increased spinal cord levels of KYNA (see Fig. 5). The most rational explanation of this finding is based on the possibility that acetic acid and KYNA share the same transport systems and the finding is therefore not surprising. Altho
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Our data for glucose and insulin
2022-02-12

Our data for glucose and insulin tolerance tests indicate that niacin-induced hyperglycemia is proportional to the degree of insulin resistance induced, implying that there is deterioration in islet function with niacin treatment (McCulloch et al., 1991). In this regard, we have demonstrated, for th
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br Acknowledgments br Introduction Oocyte donation
2022-02-12

Acknowledgments Introduction Oocyte donation has increasingly been used as an option for infertile women with preserved ovarian function but expected poor outcomes, e.g. low responders to standard ovarian stimulation and women who have experienced repeated implantation failure. Transfer of em
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