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Most human diseases e g cancer
2024-04-24

Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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br Conclusion br References and recommended reading
2024-04-24

Conclusion References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements Introduction Nucleosome, the basic chromatin unit, is composed of DNA and core histones (H2A, H2B, H3 and H4) and organized into
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To elucidate this relationship we developed a spatial model
2024-04-24

To elucidate this relationship, we developed a spatial model of Ca-influx through N-methyl-D-aspartate receptor (NMDAR), CaMKII/PP1 activation, and AMPAR insertion in a realistic spine geometry. Using this model, we show that i) variables in membrane voltage mediated Ca-influx, particularly the numb
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AHR mediated MMP upregulation has been shown
2024-04-24

AHR-mediated MMP1 upregulation has been shown in response to tobacco smoke [32]. Tobacco smoke contains various AHR ligands such as benzo[a]pyrene. Both benzo[a]pyrene [15] and FICZ [13] are high-affinity ligands for AHR and upregulate CYP1A1 and CYP1B1. FICZ is rapidly degraded by CYP1A1 [20], [33]
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br Endoplasmic reticulum protein ERp binds to AdipoR
2024-04-24

Endoplasmic reticulum protein 46 (ERp46) binds to AdipoR1 in HeLa cells ERp46 is localized in the ER and is suggested to act as a chaperone. About 20% of endogenous ERp46 are found at the plasma membrane suggesting that this protein may have additional functions. ERp46 interacts with caged compou
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Since the cloning of ARs in
2024-04-24

Since the cloning of ARs in the beginning of the 1990s, the efforts to characterize them have led to the accumulation of a substantial amount of experimental data. Decades of site-directed mutagenesis (SDM; Box 1) studies, in combination with pharmacological data and computational modeling, have pav
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Compounds were profiled for their
2024-04-24

Compounds – were profiled for their inhibitory activity against dipeptidyl peptidase-IV Activity and/or Structure Homologues (DASH) [e.g. DPP2, DPP8 and DPP9] and non-DASH [eg. post-proline cleaving enzyme (PPCE), neutral endopeptidase (NEP), aminopeptidase P (APP), aminopeptidase N (APN)] enzymes.
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To date more than different mutations in
2024-04-24

To date, more than 50 different mutations in the gene have been described (Human Gene Mutation Database at the Institute of Medical Genetics in Cardiff: SRD5A2 Gene: http://www.hgmd.cf.ac.uk). Most of them are missense mutations but premature stop codons and deletions leading to non-functional or su
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HT modulates cortical and hippocampal pyramidal cell functio
2024-04-24

5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal Sunitinib Malate mg as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leiser
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Despite functional studies demonstrating the role of HT in
2024-04-24

Despite functional studies demonstrating the role of 5-HT in ureteral contractility, the source of endogenous 5-HT in the ureter is unclear. Since 5-HT-containing enterochromaffin cells, which are present in the gastrointestinal tract, could not be found in the ureter (Nocito et al., 2007, Ripoche,
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br Disclaimer br Conflicts of
2024-04-24

Disclaimer Conflicts of interest Role of the Sponsor Acknowledgements Funding/support: This project was supported by a grant from the Department of Surgery (R5129), Western University and by the Institute for Clinical Evaluative Sciences (ICES) Western site. ICES is funded by an annual g
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br Introduction The principal pathways
2024-04-24

Introduction The principal pathways of adrenal and gonadal steroidogenesis have been known for over 50 years (reviewed by Miller and Auchus, 2011). Cholesterol is first converted to pregnenolone via three reactions, 20-hydroxylation, 22-hydroxylation and scission of the 20,22 carbon–carbon bond,
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At first the APC is a kDa
2024-04-23

At first, the APC is a 310kDa protein divided into three domains such as N-terminal, central core and C-terminal domain [102], plays a major role to regulate the Wnt signaling pathway in human cancer by translating β-catenin from the Ac-IETD-pNA to the nucleus [103]. The SIRT1 regulates the Wnt sig
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Loss of virulence in ACL mutants may
2024-04-23

Loss of virulence in ACL mutants may be caused by defect in vegetative growth and conidial germination, and reduced trichothecene production. However, supplement of potassium acetate restored the defects in germination rate and vegetative growth, but not virulence in wheat heads (Table 2, Fig. 2B),
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Wound healing without blastema formation causes partial
2024-04-23

Wound healing without blastema formation causes partial restoration of lost tissue, and gives rise to fibrotic scars. Healing by fibrotic scarring rather than by regeneration leads to tissue dysfunction, and can place a huge burden for the health of the animal [4]. Therefore, understanding the molec
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