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To date attention has been directed
2022-11-02

To date, attention has been directed towards new molecular targets in luminal phenotype (ER-positive), such as CDK4/6 and, to a lesser extent, androgen receptor (AR) pathways [8]. While the role of CDK4/6 has been elucidated and their inhibitors have shown a benefit in luminal BC, the role of AR in
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Based on structure activity relationship of several SARM tem
2022-11-01

Based on structure activity relationship of several SARM templates, Ligand Pharmaceuticals chose LGD2226 as their first clinical candidate (Miner et al., 2007). Although LGD2226 demonstrated myo- and osteo-anabolic activity and maintenance of sexual function in various preclinical models, the develo
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We have recently begun to demonstrate this concept by
2022-11-01

We have recently begun to demonstrate this concept by reporting a novel class of β-hairpin peptidomimetics, built on a piperidine-pyrrolidine semi-rigid β-turn inducer [12] and bearing two recognition pentapeptide sequences, designed on oligomeric and fibril structures of Aβ1-42 (compound 1, Fig. 1)
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The evidence points toward a role for LO
2022-11-01

The evidence points toward a role for 12/15-LO activity in WAT in modulating chronic local inflammation and subsequent systemic metabolic decline in the obese state. However, little is known as to the role of 12- and 15-LOs in BAT. Indeed, in addition to WAT, platelet- and leukocyte-type 12-LO are e
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br Endoplasmic reticulum protein ERp binds to AdipoR
2022-11-01

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 XL184 austra
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However although in vitro studies in heterologous
2022-11-01

However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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br Introduction Epilepsy is characterized by spontaneous rec
2022-11-01

Introduction Epilepsy is characterized by spontaneous recurrent seizures and represents one of the most frequent neurological diseases affecting about 60 million people worldwide (McNamara, 1999). It is estimated that up to 50% of all cases are triggered by “initial precipitating injuries”, such
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ADA catalyzes the deamination of adenosine and deoxyadenosin
2022-11-01

ADA catalyzes the deamination of adenosine and deoxyadenosine into their respective inosine nucleoside (Cristalli et al., 2001). This conversion is an initial step in a series of reactions responsible for lymphocyte proliferation and differentiation. Moreover, ADA is considered an indicator of cellu
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br Introduction Adenosine deaminase ADA
2022-11-01

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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br Results and discussion br Conclusion A series of
2022-11-01

Results and discussion Conclusion A series of aminobenzothiazole derivatives were investigated as possible Aurora B kinase inhibitors. Bioisosteric replacement of the heterocyclic core of the lead compound was performed regarding the docking analysis. Replacement of the oxygen Rosiglitazone o
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The apoptosis promoting Bcl family
2022-11-01

The apoptosis-promoting Bcl-2 family includes BH3-only proteins (e.g., Bim, Bid and Bad) and multiple-domain proteins (e.g., Bax and Bak). At the time of apoptosis stimulation (e.g., DNA damage), only the BH3-only protein is activated, directly or indirectly promoting Bax/Bak oligomerization, changi
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br Acknowledgments This study is a
2022-11-01

Acknowledgments This study is a part of a MSc thesis and supported by Scientific Research Projects Coordination Unit of Akdeniz University (grant number: 2011.02.0122.007). Introduction Apelin receptor (putative receptor protein related to the angiotensin receptor AT1, APJ) belongs to the G-p
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50 dub synthesis Obesity is associated with chronic low grad
2022-11-01

Obesity is associated with chronic low-grade 50 dub synthesis resulting from increased M1 macrophage infiltration into adipose tissue, which can subsequently lead to the development of insulin resistance. Previously, we reported that LFE and FSB both reduced body weight gain in high fat diet-induce
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br Prostate cancer and resistance to
2022-10-31

Prostate cancer and resistance to AR targeting treatment The AR plays a pivotal role in the development, differentiation, homeostasis and secretory function of the normal prostate (Wilson, 2011). The AR is also a key player in many phases of prostate carcinogenesis (Huggins et al., 1941, Scher an
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br AR mediated actions in cells of the vascular wall
2022-10-31

AR-mediated actions in EZ Cap Reagent AG of the vascular wall Sex hormones may influence the size and composition of atherosclerotic lesions indirectly by modifying systemic cardiovascular risk factors such as plasma lipids profiles and insulin sensitivity; this aspect of their action is discusse
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