• br Discussion AhR is a receptor that

  2022-10-31

  

  Discussion AhR is a receptor that binds to a great variety of lipophilic compounds, in particular those containing at least one aromatic ring (Abel and Haarmann-Stemmann, 2010, Guyot et al., 2013, Hahn, 2002). The main known function of this receptor is to induce the metabolism of these compounds

• br Introduction The chronic inflammation is

  2022-10-31

  

  Introduction The chronic inflammation is one of the leading events involved in the aetiology of many chronic-degenerative diseases including diabetes, atherosclerosis, arthritis and cancer (Coussens and Werb, 2002). Monocytes/macrophages lineage plays an important role during inflammation through

• Encouraged by this observation a systematic SAR study on the

  2022-10-31

  

  Encouraged by this observation, a systematic SAR study on the A ring -alkoxy was conducted as summarized in . The A ring methoxy-containing KRCA-0008 was proven an optimal substituent in terms of potency after all and its bigger size derivatives were detrimental in both biochemical and H3122 cellul

• Acknowledgments br P c is

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  Acknowledgments P450c17 is expressed in several steroidogenic tissues, including the adrenal cortex, the ovary, and the testes (). Thus, 17α-hydroxylase/17,20-lyase is a key enzyme required for the production of both cortisol and sex steroids. This enzyme defect blocks the synthesis of cortisol,

• In considering the roles of these enzymes in normal

  2022-10-31

  

  In considering the roles of these enzymes in normal physiology, given the importance of GLUT4-dependent glucose uptake and glucose-dependent fatty R788 disodium synthesis synthesis for systemic metabolic homeostasis (Herman and Kahn, 2006, Herman et al., 2012), deletion of Acly in adipocytes result

• To evaluate the ability of both sets of compounds to

  2022-10-31

  

  To evaluate the ability of both sets of compounds to inhibit the activity of 15-LOX an initial screen was performed, whose results are shown in . The comparison of inhibition values would seem to indicate that, in the HYD series, an electron donor group at the position increases and an electron at

• To further investigate the role of cholesterol

  2022-10-31

  

  To further investigate the role of cholesterol in the Rh2-induced cytotoxicity, we then focused on the U937 cell line, which is cholesterol auxotroph and considered as a valuable model to study the importance of cholesterol in membrane structure and function (Billheimer et al., 1987), and used the e

• br Conclusion br Competing interests br Funding The

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  Conclusion Competing interests Funding The Bolger Prostate Cancer Research Fund (no grant number), the National Institute of General Medical Sciences of the National Institutes of Health (1-R01-GM58553, G. B. Bolger, principal investigator), and the National Cancer Institute of the NIH to t

• br Conflict of Interest br

  2022-10-27

  

  Conflict of Interest Transparency Document Introduction Mitoxantrone (MXT) is an androstenedione chemotherapeutic agent that is used to treat acute nonlymphocytic leukemia, acute lymphoblastic leukemia, prostate cancer, metastatic breast cancer, and non-Hodgkin’s lymphoma [13], [14]. It is

• A c and CD are expressed in a small

  2022-10-27

  

  A2c and CD73 are expressed in a small population of OSNs with pear-shaped morphology. In spite of the expression of molecular markers of ciliated OSNs such as Golf, ACIII, and OMP [1, 17], these OSNs have an extremely short dendrite and are located in the superficial layer of OE. In addition to the

• Similarly Dilma et al tried to assess the diagnostic

  2022-10-27

  

  Similarly Dilmaç et al. [16] tried to assess the diagnostic value of adenosine deaminase activity in sputum of patients with pulmonary tuberculosis, their aim was to determine and compare sputum ADA activity in pulmonary tuberculosis, lung cancer and chronic obstructive pulmonary disease (COPD) pati

• br Introduction Adenosine deaminase ADA

  2022-10-27

  

  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

• Compounds were profiled for their inhibitory activity

  2022-10-27

  

  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.

• br Conclusion There have been multiple clinical trials and p

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  Conclusion There have been multiple clinical trials and pre-clinical studies that have tested the utility of 5ARIs in treating prostate disease, as summarized in Fig. 1. Inhibiting androgen action through the use of finasteride and dutasteride has been established as a valuable resource for physi

• br Conclusion In summary screening a small compound library

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  Conclusion In summary, screening a small compound library based on the 3-aminopyridin-2-one motif in a target-blind manner against a 26-kinase panel, representative of the kinome, identified hits that possess good activity and excellent ligand efficiency against MPS1, Aurora A and Aurora B. The b

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