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In clinical studies BA has
2024-09-12

In clinical studies, BA has been reported to promote dose-dependent LDL-C lowering effects of up to 30% as monotherapy, and up to an additional 24% when added in combination with stable statin therapy, or approximately 50% when combined with ezetimibe 109, 110, 111, 112. These effects were accompani
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Crystal structures were obtained of sulfonamide and amide
2024-09-12

Crystal structures were obtained of sulfonamide 18 and amide 19 as a derivative of amide 36 (Fig. 7A and B). The precise rotameric orientation of amide 36 was of significant interest to understand the compound's interaction with the protein. As it would be difficult to assign the rotomer of 36, the
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Molecular docking quantitative structure activity
2024-09-12

Molecular docking, quantitative structure–activity relationship (QSAR) and high-throughput virtual screening (HTVS) studies have a very widespread use in computer-assisted drug design.25, 26, 27, 28 Suvannang et al. used the published X-ray crystallographic data to examine known aromatase inhibitors
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Several strategies have been employed to
2024-09-11

Several strategies have been employed to design and engineer peptide biosensors of kinase activity, which are quite different from the strategies developed to generate genetically encoded KARs. In all cases, PF-670462 induces changes in the spectral properties of the fluorophore(s) incorporated int
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Various antiangiogenic drugs have been analyzed over the las
2024-09-11

Various antiangiogenic drugs have been analyzed over the last few years; noteworthy, bevacizumab, a monoclonal antibody against VEGF-A, alone or in combination with cytotoxic agents showed interesting results in terms of radiographic response rates and progression-free survival in initial phase 2 st
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br Materials and methods br Results br Discussion
2024-09-11

Materials and methods Results Discussion Our results revealed that LPS injection in rats impaired fear memory in the PA task. This results are in agreement with the most of previous studies reported that following acute [23,24,39,[45], [46], [47]] or chronic systemic genotyping mice buy [30
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The association of male gender
2024-09-11

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., 200
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A straightforward synthetic pathway was
2024-09-11

A straightforward synthetic pathway was adopted to synthesize the target compounds as outlined in . The starting chloromethylquinazolinones (–) were synthesized from anthranilic bromodomain in two steps following reported procedures., , , The first step involves chloroacetylation of anthranilic ac
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Within the PARP family TIPARP is most evolutionarily conserv
2024-09-11

Within the PARP family, TIPARP is most evolutionarily conserved with PARP12 (ARTD12) and PARP13 (ARTD13) [27,28,41]. All three proteins contain at least one RNA-type CCCH zinc finger domain, a poly-ADP-ribose binding WWE domain and a PARP catalytic domain (Fig. 1). PARP13 is catalytically inactive,
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br Materials and methods br Discussion Few studies have
2024-09-11

Materials and methods Discussion Few studies have examined peripheral PACAP levels in migraineurs, and no reports have described PACAP levels in blood samples from patients with CM. Here, we demonstrated that plasma PACAP concentrations were lower in patients with interictal migraine (in both
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br Conclusions Several lines of evidence have
2024-09-11

Conclusions Several lines of evidence have been established, which support the adenosine kinase hypothesis of epileptogenesis, which is based on a sequence of events leading from acute 8351 injury to initial downregulation of ADK, rise in extracellular adenosine, changes in astrocytic adenosine r
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Introduction Pyometra is relatively common in intact bitches
2024-09-11

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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In the olfactory bulb expression was especially
2024-09-11

In the olfactory bulb, expression was especially prominent in the mitral cell layer from embryonic stages to adult tissues (Figs. 1D–G). By E14–E16, Ack1 signal was remarkably intense in the proliferative ventricular zone (Fig. 1D). From E18 to adult, expression was also observed in glomerular and g
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br In patients with spina bifida and spinal
2024-09-11

In patients with spina bifida and spinal cord injury, fecal incontinence is a serious issue that can impair activities of daily living and patient self-esteem. To address this Malone et al. first described the Antegrade Continence Enema (ACE) procedure in 1990 [1], which achieves continence by all
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Thirty six of the analogs
2024-09-10

Thirty-six of the analogs synthesized showed ATX inhibition greater than 50% at 10μM with FS-3, twelve of which had improved potency over the lead (Fig. 5). Of these, 22 was sub-micromolar (IC50 670nM). The 3,5-dichlorophenoxy ring of 22 is reminiscent of the 3,5-dichlorophenylthiourea ring in Hoegl
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