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An alternative to the agonist or antagonist potential in
2023-01-13
An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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br ARIs in the prevention of
2023-01-13
5ARIs in the prevention of prostate cancer Prostate cancer continues to be a leading cause of male deaths worldwide. In 2009, it was estimated there would be 192,280 new cases of prostate cancer with a predicted 27,360 deaths [25]. Because androgens, and specifically DHT, play a large role in bot
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br Funding br Introduction The interest in the
2023-01-13
Funding Introduction The interest in the effects of endocrine disrupting chemicals (EDCs) in the aquatic environment continues to increase over the past decade, specifically those that act on steroidogenic pathways. EDCs that include synthetic androgenic and estrogenic compounds can severely a
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Furthermore new strategies to achieve a total
2023-01-13
Furthermore, new strategies to achieve a total androgen deprivation namely by blocking either androgen biosynthesis as well as AR are being considered and should be a relevant topic in the near future. A successful example of this approach is galeterone (159), which not only inhibits the CYP17 enzym
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ATM dependent initiation of radiation induced G M checkpoint
2023-01-13
ATM-dependent initiation of radiation-induced G2/M checkpoint arrest is well established [11], [34], [35]. However, the ATR pathway may also be involved [36], [37]. Brown and Baltimore generated Cre/lox-conditional cell lines or Fmoc-Tyr(tBu)-OH with a kinase inactive allele of ATR (ATRkd) to evalu
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br Conclusion In conclusion the arginase from P
2023-01-13
Conclusion In conclusion, the arginase from P. aeruginosa IH2 was purified with electrophoretic homogeneity. Purified enzyme was homo-dimer and showed significant activity and catalytic stability near to the pH of circulating system and temperature of human body. The prolonged serum and proteolyt
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br The role of apelin in respiratory diseases At
2023-01-12
The role of apelin in respiratory diseases At present, several scientific studies have suggested that the apelin/APJ system may play an important role in the development of pulmonary diseases (Table 4). For example, in an experiment on rats suffering from acute lung injury, apelin-13 decreases th
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Expression of Twist and the AR are increased by oxidative
2023-01-10
Expression of Twist1 and the AR are increased by oxidative stress, but the change in the receptor (mRNA/protein) is lost after treatment with siRNAs that target Twist 1 (Shiota et al., 2010). Twist 1 was found to bind to E-boxes, 5′-CANNTG-3′, in the proximal promoter (−442 to +51 bp) and upstream r
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A requirement for active PKA signaling during LTD induction
2023-01-10
A requirement for active PKA signaling during LTD induction was proposed in studies characterizing AKAP150 D36mice (Lu et al., 2008), but linking impaired LTD in D36 mice to PKA signaling deficits was complicated by subsequent work showing substantial increases in the number of dendritic spines and
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Introduction Pyometra is relatively common in intact bitches
2023-01-10
Introduction Pyometra is relatively common in intact bitches and its diagnosis is aided by ultrasonography (Bigliardi et al., 2004), along with measurement of acute phase proteins and leucocyte (white blood cell, WBC) counts; assessment of these parameters during recovery may be helpful for monitor
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prolyl hydroxylase br Funding This work was supported by Are
2023-01-10
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 role for YAP in mediating resistance to EGFR inhibition
2023-01-10
A role for YAP in mediating resistance to EGFR inhibition has also been described [28], [29]. In line with these evidences, we observed increased YAP activation in all the generated EGFR TKI–resistant cells, testified by decreased phosphorylation on the inhibitory serine 127, enhanced nuclear locali
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(-)-Bicuculline methiodide The following are the supplementa
2023-01-10
The following are the supplementary data related to this article. Funding Work in Dr. Rosell's laboratory is partially supported by a grant from La Caixa Foundation, and an Instituto de Salud Carlos III grant (RESPONSE, PIE16/00011). Work in Dr. Cao's laboratory is partially supported by the Maj
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Whole body loss of ACLY is early embryonic
2023-01-10
Whole-body loss of ACLY is early embryonic lethal, indicating that it serves non-redundant roles during development (Beigneux et al., 2004). Silencing or inhibition of ACLY suppresses the proliferation of many cancer cell lines and impairs tumor growth (Bauer et al., 2005, Hanai et al., 2012, Hatziv
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The interaction of ATR ATRIP
2023-01-10
The interaction of ATR-ATRIP with RPA-coated ssDNA is sufficient for ATR-ATRIP recruitment to DNA lesions, but it is not sufficient to fully activate ATR. In response to DNA damage, the heterotrimeric ring-shaped complex 9-1-1 (RAD9-RAD1-HUS1 in humans; Ddc1-Rad17-Mec3 in S. cerevisiae) is loaded at
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