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At the outset of targeting the two Gln
2023-07-26

At the outset of targeting the two Gln756 side-chain rotamers, it was unclear which rotational isomer would lead to more potent ASK1 inhibitors. While such a preference might have been anticipated, the cohort of ASK1 inhibitors in Table 3 did not provide any guidance regarding which of the Gln756 am
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Despite their different effects on cell
2023-07-26

Despite their different effects on cell survival, the functions of autophagy and apoptosis are not completely independent. Additionally, Cho et al. (2009) suggested that the mediation of caspase-3 links the apoptotic and autophagic signaling pathways. Consequently, to illuminate the correlation, exc
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The relationship between the apelinergic
2023-07-26

The relationship between the apelinergic and opioid systems has been previously reported (Lv et al., 2011, Yang et al., 2010). Lv and colleagues showed that naloxone has a suppressive effect on apelin-induced depression-like behavior in mice (Lv et al., 2012a). Furthermore, heterodimerization of GPC
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br Results br Discussion AP a heterodimeric transcription
2023-07-26

Results Discussion AP-1, a heterodimeric transcription factor comprising various combinations of FOS, JUN, MAF, ATF, and CREB family proteins, has been known to play a pivotal role in leukocyte development for decades (Liebermann et al., 1998; Valledor et al., 1998). However, its participation
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br HIF Blockade in AA Therapy In lieu
2023-07-26

HIF-α Blockade in AA Therapy In lieu of the evidence supporting a central role for HIF-α signaling in tumor angiogenesis and CC pathobiology, significant efforts have focused on the discovery of small-molecule HIF-α inhibitors (for exhaustive compendia, see [28,44,45]). In brief, inhibitors vary
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d-glucose br Small molecule homoisoflavonoid in combination
2023-07-26

Small molecule homoisoflavonoid in combination with anti-VEGF therapy Basavarajappa et al. [11] reported a new synthetic homoisoflavonoid compound, SH-11037 by modifying the structure of naturally occurring homoisoflavonoid cremastranone. SH-11037 exhibited promising inhibition of human retinal m
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Introduction Cardiovascular disease is the principal cause
2023-07-26

Introduction Cardiovascular disease is the principal cause of morbidity and mortality in patients with AZD8931 (1). Comprehensive management of these patients includes not only adequate glycemic control but also attention to additional recognized risk factors. Hypertension is a cardiovascular risk
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In light of several reports
2023-07-26

In light of several reports of defects in memory-related tasks for the dysbindin-deficient mice (Cox et al., 2009, Takao et al., 2008), it was rather unexpected that an enhancement of CA3–CA1 LTP was observed in our investigation as well as in another independent study (T.T. Tang et al., 2009). The
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We found evidence of the interaction between AR and
2023-07-26

We found evidence of the interaction between AR and hemiacetals by evaluating the effect of glucose on l-idose reduction. l-idose was recently proposed as the best AR substrate able to mimic glucose [38]. This aldose is structurally very closely related to d-glucose, from which it differs only in th
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Among all the compounds the
2023-07-26

Among all the compounds, the novel L-748,337 derivative (23d) showed the potent human β3-AR antagonist activity and high lipolysis inhibitory activity in vitro. The vx 765 23d displayed 23-fold more potent β3-AR antagonist activity (EC50 = 0.5117 nM) than that of L-748,337 (EC50 = 11.91 nM) and hig
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Additionally regulation of GPCR heteromerization by specific
2023-07-26

Additionally, regulation of GPCR heteromerization by specific ligands may depend not only on the affinity of ligands for receptors, but also on presence of different interacting proteins co-localizing with the receptors in the specific cell, which may induce some conformational changes and contribut
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50 dub br Adenosine and tumor microenvironment In the majori
2023-07-26

Adenosine and tumor microenvironment In the majority of carcinogenic processes a proinflammatory state is generated [36], [37]. In addition, a tumor hypoxic environment is generally due to inadequate perfusion of oxygen to the tumor [38]. Immunomodulators are molecules that regulate the immune r
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br Material and methods br Results br Discussion
2023-07-26

Material and methods Results Discussion To develop a novel regenerative and/or neuroprotective therapy for optic neuropathy, including glaucoma, numerous studies have tested new candidates favorable to RGC survival and axon regeneration. Among the many candidate drugs, AdoR modulators are o
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Two patients developed diffuse mesangio proliferative glomer
2023-07-26

Two patients developed diffuse mesangio-proliferative glomerulonephritis (DMPG) postoperatively, presenting as nephrotic syndrome and benign haematuria, respectively. DMPG has been reported in an adult patient with thymomatous MG following thymectomy [35], and various types of glomerulonephritis hav
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In this study an in vitro AChE inhibition assay
2023-07-26

In this study, an in vitro AChE inhibition assay combined with UF-HPLC-ESI-Q-TOF/MS method was developed for rapid screening and identification of AChEI from the roots of C. chinensis Franch. Five compounds was found with AChE inhibitory activity and identified by the on-line DAD-ESI-Q-TOF/MS compar
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