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Thiazole heterocycles constitute an interesting class of
2025-02-27
Thiazole heterocycles constitute an interesting class of molecules, which exhibit a broad spectrum of biological activity, including antifungal properties [[16], [17], [18], [19]]. Encouraged by our previous study that describes the activity of hydrazine-thiazole derivatives against C. gattii and C
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Exemestane Sorafenib was the first small RTK inhibitor
2025-02-27
Sorafenib was the first small RTK inhibitor drug to be developed and was initially approved against renal cell carcinoma, then against hepatocellular carcinoma (HCC) and more recently for differentiated thyroid treatment [111]. Sunitinib soon followed, being approved for gastrointestinal stromal tum
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The association of male gender with increased atherosclerosi
2025-02-27
The association of male gender with increased atherosclerosis has stimulated interest in the role of androgen signalling in this condition. Androgens act (Fig. 2) by direct activation of androgen receptor (AR), a nuclear receptor that acts as a ligand-regulated transcription factor (Gao et al., 2005
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br Acetaldehyde One of the most common http
2025-02-26
Acetaldehyde One of the most common environmental aldehydes is acetaldehyde (CH2CHO). Acetaldehyde, which is highly volatile, has been classified as a Group I human carcinogen by the International Agency for Research on Cancer [30]. Aldehydes can form DNA adducts, including ring-open forms of cro
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NLX a k a F or befiradol exhibits nanomolar
2025-02-26
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in BMS-345541 to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally, it ha
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Introduction Adenosine monophosphate cAMP is a general purpo
2025-02-26
Introduction Adenosine 3′,5′-monophosphate (cAMP) is a general-purpose signaling molecule present in most branches of life. Intracellular cAMP levels control diverse cellular functions. In bacteria, cAMP regulates metabolism by activation of the catabolite activator protein (CAP), also known as cAM
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Neural progenitor cells NPCs are self renewing multipotent c
2025-02-26
Neural progenitor cells (NPCs) are self-renewing, multipotent cells that are capable of differentiating into neurons, astrocytes and oligodendrocytes. NPCs are activated in response to a variety of pathological states in neurodegenerative diseases such as Parkinson’s disease and multiple sclerosis,
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where is the breaking force In the following the
2025-02-26
where is the breaking force. In the following, the details of the simulation are presented and subsequently, the results are discussed. The initial atomic structure is extracted from the crystal structure of single AF (PDB identification 3G37) which consist 12 monomers. As aforementioned 4 monomer
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br Conflicts of interest br Acknowledgments br Significance
2025-02-26
Conflicts of interest Acknowledgments Significance Introduction Androgen receptor (AR) plays a paramount role in the onset and progression of prostate cancer (PC) (Burnstein, 2005, Lonergan and Tindall, 2011, Watson et al., 2015). This very facet underlies androgen deprivation therapy (A
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Because serum ATX activity and plasma LPA are well correlate
2025-02-26
Because serum ATX activity and azidothymidine LPA are well correlated with liver fibrosis stage histologically, both of these parameters merit consideration as novel markers of fibrosis. However, serum ATX activity may be a more useful test from a clinical laboratory perspective. First, LPA can incr
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Compound was docked into the
2025-02-26
Compound was docked into the active site of Aurora B kinase using Tripos sybyl-X ver. 2.1.1. The crystal structure of human Aurora B kinase cocrystallized with its potent inhibitor VX-680 was used for the docking analysis (PDB ID: ). The most likely binding conformations were selected based on the
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In response to DSB the lesion recognition factor
2025-02-26
In response to DSB, the lesion recognition factor Mre11-Rad50-Nbs1 (MRN) complex helps the recruitment of ATM to the damage site and its activation by phosphorylation [29]. However, whether UV-damage recognition factors directly influence ATR and ATM recruitment and their phosphorylation is not clea
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Chromatin proteins play important roles in gene expression a
2025-02-26
Chromatin proteins play important roles in gene expression and DNA repair. The importance of chromatin composition on gene expression is exemplified by X-inactivation, where one of the two X chromosomes in female mammalian ABT 724 trihydrochloride is transcriptionally silenced by heterochromatin ,
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In recent years the higher lipophilicity thus better
2025-02-25
In recent years, the ‘higher lipophilicity’-thus-‘better performance’ tenet, derived from the polar paradox theory applied to micro-structured media, was challenged by novel and unexpected experimental results. In particular, the synthesis of many complete series of fatty T16Ainh - A01 esters of na
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ERAP has been crystallized in two different
2025-02-25
ERAP1 has been crystallized in two different conformations, wherein the C-terminal domain IV is either closely interacting with domains I/II and enclosing the active site (termed ‘closed’), or is rotated away in a hinge motion which exposes the active site (‘open’). This large motion correlates with